Microneedles(MNs)have been extensively investigated for transdermal delivery of large-sized drugs,including proteins,nucleic acids,and even extracellular vesicles(EVs).However,for their sufficient skin penetration,con...Microneedles(MNs)have been extensively investigated for transdermal delivery of large-sized drugs,including proteins,nucleic acids,and even extracellular vesicles(EVs).However,for their sufficient skin penetration,conventional MNs employ long needles(≥600μm),leading to pain and skin irritation.Moreover,it is critical to stably apply MNs against complex skin surfaces for uniform nanoscale drug delivery.Herein,a dually amplified transdermal patch(MN@EV/SC)is developed as the stem cell-derived EV delivery platform by hierarchically integrating an octopusinspired suction cup(SC)with short MNs(≤300μm).While leveraging the suction effect to induce nanoscale deformation of the stratum corneum,MN@EV/SC minimizes skin damage and enhances the adhesion of MNs,allowing EV to penetrate deeper into the dermis.When MNs of various lengths are applied to mouse skin,the short MNs can elicit comparable corticosterone release to chemical adhesives,whereas long MNs induce a prompt stress response.MN@EV/SC can achieve a remarkable penetration depth(290μm)for EV,compared to that of MN alone(111μm).Consequently,MN@EV/SC facilitates the revitalization of fibroblasts and enhances collagen synthesis in middle-aged mice.Overall,MN@EV/SC exhibits the potential for skin regeneration by modulating the dermal microenvironment and ensuring patient comfort.展开更多
Candida albicans is one of the most common pathogens causing invasive fungal infections,with a mortality rate of up to 20%-50%.Amphotericin B(AmB),a biopharmaceutics classification system(BCS)IV drug,significantly inh...Candida albicans is one of the most common pathogens causing invasive fungal infections,with a mortality rate of up to 20%-50%.Amphotericin B(AmB),a biopharmaceutics classification system(BCS)IV drug,significantly inhibits Candida albicans.AmB is primarily administered via oral and intravenous infusion,but severe infusion adverse effects,nephrotoxicity,and potential hepatotoxicity limit its clinical application.Deep eutectic solvents(DESs),with excellent solubilization ability and skin permeability,are attractive for transdermal delivery.Herein,we used DESs to deliver AmB for antifungal therapy transdermally.We first prepared and characterized DESs with different stoichiometric ratios of choline(Ch)and geranate(Ge).DESs increased the solubility of AmB by a thousand-fold.In vitro and in vivo,skin permeation studies indicated that DES_(1:2)(Ch and Ge in 1:2 ratio)had the most outstanding penetration and delivered fluorescence dye to the dermis layer.Then,DES_(1:2)-AmB was prepared and in vitro antifungal tests demonstrated that DES_(1:2)-AmB had superior antifungal effects compared to AmB and DES_(1:2).Furthermore,DES_(1:2)-AmB was skin-irritating and biocompatible.In conclusion,DES-AmB provides a new and effective therapeutic solution for fungal infections.展开更多
Microneedle(MN)patches could be a promising treatment for diabetic foot ulcers that plague thousands of people worldwide.While reducing skin resistance or increasing driving force can accelerate the efficiency of tran...Microneedle(MN)patches could be a promising treatment for diabetic foot ulcers that plague thousands of people worldwide.While reducing skin resistance or increasing driving force can accelerate the efficiency of transdermal drug delivery with conventional MN patches,it can create toxic chemical residues or require the help of additional devices.Herein,a thermo-responsive microneedles patch(TMN)with high biocompatibility without additional equipment is proposed.The TMN consisted of a bilayer microneedles composed of sodium alginate(SA)-g-poly(N-isopropylacrylamide)layer(SA-g-PNIPAM)loaded with sucrose octasulfate sodium salt(SOS)and hyaluronic acid layer and a polycaprolactone/chitosan nanofiber membrane loading with tetracycline hydrochloride(TH)and SOS.PNIPAM accelerates drug release by extruding the drug through a volumetric phase transition in response to temperature changes,and TH and SOS promote wound healing by inhibiting bacterial growth and promoting vascular regeneration and epithelial formation.The results showed that the drug release of TMN was significantly faster,with the drug release rate of more than 80% in the 10th h,and the antibacterial rate of TMN could reach 800%.In addition,TMN had good biocompatibility and good healing effects in vivo,which may be helpful for the design of multifunctional dressings in the future.展开更多
Diabetic pressure ulcers(DPU)are non-healing due to vascular dysfunction and bacterial infection.Early intervention can delay ulcer progression,such as preventing the formation of full-thickness skin defects.Local adm...Diabetic pressure ulcers(DPU)are non-healing due to vascular dysfunction and bacterial infection.Early intervention can delay ulcer progression,such as preventing the formation of full-thickness skin defects.Local administration of deferoxamine(DFO)at wound sites has been shown to promote neovascularization and enhance wound healing.However,since DPU skin wounds are not full-thickness defects and DFO is hydrophilic,enhancing its transdermal delivery is crucial for effective treatment.Photothermal ablation of stratum corneum,generated by copper sulfide nanoparticles(Cu S NPs)under near-infrared(NIR)light irradiation,is a promising method to improve transdermal drug delivery.Meanwhile,Cu S NPs-induced photothermal therapy offers excellent antibacterial performance.In this study,DFO and Cu S NPs were incorporated into a matrix metalloproteinase(MMPs)-sensitive hydrogel.This hydrogel promotes cell adhesion and is degraded by cell-secreted MMPs,a process crucial for the controlled release of encapsulated DFO and Cu S NPs.Under NIR irradiation,the stratum corneum is disrupted,facilitating transdermal DFO delivery and simultaneously eliminating infected bacteria.As a result,the essential requirements for DPU treatment,“facilitating transdermal DFO delivery,promoting angiogenesis,and inhibiting bacterial infection”,were achieved simultaneously.展开更多
Ionic liquids (ILs) have been proven to be an effective technology for enhancing drug transdermal absorption. However, due to the unique structural components of ILs, the design of efficient ILs and elucidation of act...Ionic liquids (ILs) have been proven to be an effective technology for enhancing drug transdermal absorption. However, due to the unique structural components of ILs, the design of efficient ILs and elucidation of action mechanisms remain to be explored. In this review, basic design principles of ideal ILs for transdermal drug delivery system (TDDS) are discussed considering melting point, skin permeability, and toxicity, which depend on the molar ratios, types, functional groups of ions and inter-ionic interactions. Secondly, the contributions of ILs to the development of TDDS through different roles are described: as novel skin penetration enhancers for enhancing transdermal absorption of drugs;as novel solvents for improving the solubility of drugs in carriers;as novel active pharmaceutical ingredients (API-ILs) for regulating skin permeability, solubility, release, and pharmacokinetic behaviors of drugs;and as novel polymers for the development of smart medical materials. Moreover, diverse action mechanisms, mainly including the interactions among ILs, drugs, polymers, and skin components, are summarized. Finally, future challenges related to ILs are discussed, including underlying quantitative structure-activity relationships, complex interaction forces between anions, drugs, polymers and skin microenvironment, long-term stability, and in vivo safety issues. In summary, this article will promote the development of TDDS based on ILs.展开更多
Atopic dermatitis(AD) is a chronic inflammatory skin condition. Natural products have gained traction in AD treatment due to their accessibility, low toxicity, and favorable pharmacological properties. However, their ...Atopic dermatitis(AD) is a chronic inflammatory skin condition. Natural products have gained traction in AD treatment due to their accessibility, low toxicity, and favorable pharmacological properties. However, their application is primarily constrained by poor solubility, instability, and limited permeability. The transdermal drug delivery system(TDDS) offers potential solutions for transdermal delivery, enhanced penetration, improved efficacy, and reduced toxicity of natural drugs, aligning with the requirements of modern AD treatment. This review examines the application of hydrogels, microneedles(MNs), liposomes, nanoemulsions, and other TDDS-carrying natural products in AD treatment, with a primary focus on their effects on penetration and accumulation in the skin. The aim is to provide valuable insights into the treatment of AD and other dermatological conditions.展开更多
Melanoma is one of the most malignant skin tumors, whose high invasion is generally associated with BRAF gene mutation. Although new chemotherapeutic drugs, such as vemurafenib, have been developed to inhibit the grow...Melanoma is one of the most malignant skin tumors, whose high invasion is generally associated with BRAF gene mutation. Although new chemotherapeutic drugs, such as vemurafenib, have been developed to inhibit the growth of melanoma, these drugs are usually administered intravenously or orally, resulting in toxic side effects on major tissues and organs. Tetrahedral framework nucleic acids(tFNAs) are a novel type of DNA nanostructures with excellent biocompatibility and versatility which have been proven to penetrate through skin barrier with ease. In this study, we prepared t FNAs with vemurafenib and connected DNA aptamer AS1411 at the apex of t FNAs(AS1411-tFNAs/vemurafenib). On one hand, AS1411-tFNAs/vemurafenib could kill melanoma cells by blocking the mutated BRAF gene in vitro. Compared with free vemurafenib, AS1411-tFNAs/vemurafenib had no obvious toxicity to normal cells. On the other hand,AS1411-tFNAs could transfer vemurafenib to cross through the skin barrier and permeate into tumor tissues. In vivo, transdermal delivery of AS1411-t FNAs/vemurafenib could inhibit the growth of human A375melanoma, whose inhibiting effect was stronger than intravenous administration of vemurafenib. These results demonstrated the application prospects of tFNAs combined with chemotherapeutic drugs in skin tumors.展开更多
Three-dimensional(3D)printing is an innovative manufacturingmethod with the potential to revolutionize topical and transdermal dosage forms.Nowadays,it is established that Vatbased photopolymerization(VP)3D printing t...Three-dimensional(3D)printing is an innovative manufacturingmethod with the potential to revolutionize topical and transdermal dosage forms.Nowadays,it is established that Vatbased photopolymerization(VP)3D printing technologies offer superior printing efficiency and versatility compared to other 3D printing technologies available on the market.However,there are some limitations that impair their full application in pharmaceutical contexts,such as the lack of a range of biocompatiblematerials for topical and transdermal applications.This reviewarticle explores all types of VP-based 3D printing and discusses the relevance of implementing this kind of technology.We start with a detailed description of the printing process,focusing on the commercial materials available and lab-made resins proposed by different authors.We also review recent studies in this field,which mainly focus on the fabrication of transdermal devices based on microneedle arrays.In the future,it is expected that the manufacturers of 3D printers invest in modifications to the printing apparatus to allow the simultaneous printing of different resins and/or compound types,which will open frontiers to the personalization of treatment approaches.展开更多
Plasma-enhanced transdermal drug delivery(TDD) presents advantages over traditional methods,including painless application, minimal skin damage, and rapid recovery of permeability. To harness its clinical potential, f...Plasma-enhanced transdermal drug delivery(TDD) presents advantages over traditional methods,including painless application, minimal skin damage, and rapid recovery of permeability. To harness its clinical potential, factors related to plasma’s unique properties, such as reactive species and electric fields, must be carefully considered.This review provides a concise summary of conventional TDD methods and subsequently offers a comprehensive examination of the current state-of-the-art in plasma-enhanced TDD. This includes an analysis of the impact of plasma on HaCaT human keratinocyte cells, ex vivo/in vivo studies, and clinical research on plasma-assisted TDD. Moreover, the review explores the effects of plasma on skin physical characteristics such as microhole formation, transepidermal water loss(TEWL), molecular structure of the stratum corneum(SC), and skin resistance. Additionally, it discusses the involvement of various reactive agents in plasma-enhanced TDD, encompassing electric fields,charged particles, UV/VUV radiation, heat, and reactive species. Lastly, the review briefly addresses the temporal behavior of the skin after plasma treatment, safety considerations, and potential risks associated with plasma-enhanced TDD.展开更多
Objective:To find a viable alternative to reduce the number of doses required for the patients with post-traumatic stress disorder(PTSD),and to improve efficacy and patient compliance.Methods: In this study,we used gi...Objective:To find a viable alternative to reduce the number of doses required for the patients with post-traumatic stress disorder(PTSD),and to improve efficacy and patient compliance.Methods: In this study,we used ginger oil,a phytochemical with potential therapeutic properties,to prepare ginger oil patches.High-performance liquid chromatography(HPLC)was used to quantify the main active component of ginger oil,6-gingerol.Transdermal absorption experiments were conducted to optimize the various pressure-sensitive adhesives and permeation enhancers,including their type and concentration.Subsequently,the ginger oil patches were optimized and subjected to content determination and property evaluations.A PTSD mouse model was established using the foot-shock method.The therapeutic effect of ginger oil patches on PTSD was assessed through pathological sections,behavioral tests,and the evaluation of biomarkers such as tumor necrosis factor-α(TNF-α),interleukin-6(IL-6),brain-derived neurotrophic factor(BDNF),and melatonin(MT).Results: The results demonstrated that ginger oil patches exerted therapeutic effects against PTSD by inhibiting inflammatory responses and modulating MT and BDNF levels.Pharmacokinetic experiments revealed that ginger oil patches maintained a stable blood drug concentration for at least one day,addressing the rapid metabolism drawback of 6-gingerol and enhancing its therapeutic efficacy.Conclusions: Ginger oil can be prepared as a transdermal drug patch that meets these requirements,and the bioavailability of the prepared patch is better than that of oral administration.It can improve PTSD with good patient compliance and ease of administration.Therefore,it is a promising therapeutic formulation for the treatment of PTSD.展开更多
Transdermal medications are an useful yet underutilized tool in the field of psychiatry.Despite numerous advantages of using this route of medication delivery,transdermal medications remain less popular compared to ot...Transdermal medications are an useful yet underutilized tool in the field of psychiatry.Despite numerous advantages of using this route of medication delivery,transdermal medications remain less popular compared to other routes of medication administration such as oral and intramuscular routes in the management of various psychiatric conditions.In this editorial,we examine the advantages of transdermal medications with a brief overview of transdermal being used in psychiatry and other medical specialties.We discuss the factors that play a role in their limited usage in psychiatry.We highlight certain patient categories who can specifically benefit from them and discuss potential solutions that can broaden the perspective of treating clinicians making this an intriguing avenue in the field of psychiatry.展开更多
Transdermal drug delivery offers a promising alternative to traditional cancer therapies by providing a non-invasive,controlled,and targeted delivery of therapeutic agents.This paper explores the advancements,benefits...Transdermal drug delivery offers a promising alternative to traditional cancer therapies by providing a non-invasive,controlled,and targeted delivery of therapeutic agents.This paper explores the advancements,benefits,and challenges associated with transdermal drug delivery systems(TDDS)in cancer treatment.It highlights the mechanisms of action,key technologies,and the potential impact on patient outcomes.By examining recent studies and clinical trials,this paper aims to provide a comprehensive overview of the efficacy,safety,and prospects of transdermal drug delivery in oncology.展开更多
Aim To prepare triamcinolone-acetonide-acetate (TAA)-loaded solid lipidnanoparticles (SLN) carbomer gel with tripalmitin glyceride (TPG), and investigate theircharacteristics and transdermal drug delivery. Methods SLN...Aim To prepare triamcinolone-acetonide-acetate (TAA)-loaded solid lipidnanoparticles (SLN) carbomer gel with tripalmitin glyceride (TPG), and investigate theircharacteristics and transdermal drug delivery. Methods SLN suspension was prepared by high-pressurehomogenization technique, and then mixed with carbomer gel matrix to get SLN gel. The morphology,particle size with polydispersi-ty index (PI) and zeta potential were examined by atomic forcemicroscopy (AFM) and photon correlation spectroscopy (PCS). The entrapment efficiency, stability andin vitro drug release were also studied. The transdermal drug delivery through porcine ear skin wasevaluated using modified Franz diffusion cells. Results The SLN had a spherical shape with theaverage size of (95.5 - 186.2) nm, the zeta potential of (-26.3- -15.7) mV and the entrapmentefficiency of 67.4%-90.3% for different TAA encapsulated compounds. TAA-SLN carbomer gel had goodstability, the release profile in vitro fitted Higuchi equation. In comparison with conventionalhydrogels, TAA-SLN carbomer gel resulted in higher drug permeation amount and drug deposition withinporcine ear skin after 24 h penetration experiment. Conclusion TAA-SLN carbomer gel is preparedwith stable physicochemical properties. The release profile and improved drug permeation into skinmake it be a promising vehicle for transdermal drug delivery.展开更多
Objective: Objective: To assess the effect and adverse effects of transdermal fentanyl for elderly patients with cancer pain in China. Methods: A total of 1664 elderly patients (aged 65-90 with mean age of 72.6) with ...Objective: Objective: To assess the effect and adverse effects of transdermal fentanyl for elderly patients with cancer pain in China. Methods: A total of 1664 elderly patients (aged 65-90 with mean age of 72.6) with cancer pain enrolled in the multicenter study from 136 institutes in China. Of them, 408 (28.8%) patients were 75 years old or older. All patients received transdermal fentanyl for the management of cancer pain. The patients were asked to record the attacks of pain, quality of life, and any side effects of the treatment. Results: Baseline mean of pain intensity was 7.34. On day 1, 3, 6, 9 15, and 30, the pain mean scores were decreased to 3.82, 2.80, 2.43, 2.11, 1.83, 1.64 (P=0.000). The effective rate was 97.18%. The mean doses of fentanyl was 31.34 g/h (25-150 g/h) initially, and 40.59 g/h and 47.50 g/h (25-200 g/h) at day 15 and day 30. At treatment day 15, the dose of fentanyl was ranger from 25 to 50 g/h in 91.8% of patients, 75 to 100 g/h in 7.5% patients, and 125 to 200 g/h only in 0.8% patients. The fine quality of life was in 25.4% patients before treatment, and was 71.15% and 73.04% at day 15 and day 30 respectively (P=0.0000). The common side effects were constipation (10.70%), nausea (11.96%), dizzy (6.85%), vomiting (3.85%), sedation (2.40%), Respiratory depression (0.12%). 86.2% patients preferred continue treated by transdermal fentanyl. Conclusions: Transdermal fentanyl for the elderly with cancer pain is effective, safe, convenient, and can improve the quality of life. Transdermal fentanyl can be recommended as a first-line drug for the treatment of elderly patients with moderate to severe cancer pain, and the initial doses is recommended as 25 g/h.展开更多
One major problem encountered in transdermal drug delivery is the low permeability of drugs through the skin barrier. In the present study, we developed a surfactant-ethanolic liposomal system to improve the transderm...One major problem encountered in transdermal drug delivery is the low permeability of drugs through the skin barrier. In the present study, we developed a surfactant-ethanolic liposomal system to improve the transdermal delivery of docetaxel （DTX）, a model drug for high molecular weight and poorly water-soluble drugs. Surfactant-ethanolic liposomes （SEL） were composed of phospholipids, ethanol, sodium cholate, DTX and PBS which were prepared by thin film dispersion method. The developed formulations were characterized by determining the vesicle shape and surface morphology, size and size distribution, entrapment efficiency and drug loading capacity. The effects of the developed formulations on the permeation of DTX across rat skin in vitro were investigated using the modified Franz diffusion cell under both occlusive and non-occlusive application condi- tions. The DTX SELs with optimum composition （phospholipid-surfactant, 85：15, w/w） provided a significantly higher steadystate amount of flux and cumulative permeation, compared to the tranditional liposomes, surfactant liposomes and ethanolic liposomes. The optimal SELs exhibited stable vesicle size, morphology and drug loading capacity. Our results indicated that SELs were promising carriers to enhance the transdermal delivery of DTX.展开更多
The objective of the present study is to examine cardiovascular protective action of a newly developed transdermal patch by incorporating bisoprolol and isosorbide dinitrate in spontaneously hypertensive rats. As the ...The objective of the present study is to examine cardiovascular protective action of a newly developed transdermal patch by incorporating bisoprolol and isosorbide dinitrate in spontaneously hypertensive rats. As the combination therapy with these two synergistic drugs at low doses through a suitable form of administration could provide optimal therapeutic benefit, we further evaluated the effects of a 42 d period of anti-hypertensive treatment in spontaneously hypertensive rats. Rats were divided into the following five groups： control （blank patch）, bisoprolol fumarate tablets （BP-FT, 20.0 mg/kg, i.g.）, bisoprolol transdermal patch （BP-TP, 20.0 mg/kg）, isosorbide dinitrate transdermal patch （ISDN-TP, 20.0 mg/kg）, and the combination of BP and ISDN in a transdermal patch at low doses （8 and 12 mg/kg, respectively）. The effects of treatment were evaluated via biochemical indicators related to cardiovascular protection, structure and function. The combination therapy had synergistic anti-hypertensive effects and significantly reduced blood pressure with the benefit of controlling blood pressure variability compared to BP-FT and BP-TP. The combined treatment also reduced heart rate as well as BP-FT and BP-TP, while ISDN-TP had no evident effects on blood pressure, heart rate, and cardiovascular protection. Combination therapy was superior to BP-TP and BP-FT at increasing blood atrial natriuretic peptide and nitric oxide, while also reducing cardiac hydroxyproline and endothelin-1 with no difference in blood endothelin-1 and cardiac malondialdehyde levels. Cardiovascular remodeling differed among the groups, with the combination therapy reducing cardiac hypertrophy and the aortic media/lumen ratio. The consequential improvements in relaxation in response to cumulative concentrations of acetylcholine may explain the associated improvement in endothelial function. Combi- nation treatment with a transdermal patch exhibited a synergistic therapeutic effect. Such favorable cardiovascular effects with nitric oxide donors and β-blockade combination through a transdermal patch may provide long-term cardiovascular protection during anti-hypertensive treatment.展开更多
Chronic pain lasting more than 3 mo,or even several years can lead to disability.Treating chronic pain safely and effectively is a critical challenge faced by clinicians.Because administration of analgesics through or...Chronic pain lasting more than 3 mo,or even several years can lead to disability.Treating chronic pain safely and effectively is a critical challenge faced by clinicians.Because administration of analgesics through oral,intravenous or intramuscular routes is not satisfactory,research toward percutaneous delivery has gained interest.The transdermal patch is one such percutaneous delivery system that can deliver drugs through the skin and capillaries at a certain rate to achieve a systemic or local therapeutic effect in the affected area.It has many advantages including ease of administration and hepatic first pass metabolism avoidance as well as controlling drug delivery,which reduces the dose frequency and side effects.If not required,then the patch can be removed from the skin immediately.The scopolamine patch was the first transdermal patch to be approved for the treatment of motion sickness by the Food and Drug Administration in 1979.From then on,the transdermal patch has been widely used to treat many diseases.To date,no guidelines or consensus are available on the use of analgesic drugs through transdermal delivery.The pain branch of the Chinese Medical Association,after meeting and discussing with experts and based on clinical evidence,developed a consensus for promoting and regulating standard use of transdermal patches containing analgesic drugs.展开更多
The purpose of this study was to investigate the effects of vehicles and organic acids on the in vitro permeation of letrozole across rat skin. Permeation experiments were carried out with 2-chamber diffusion cells th...The purpose of this study was to investigate the effects of vehicles and organic acids on the in vitro permeation of letrozole across rat skin. Permeation experiments were carried out with 2-chamber diffusion cells through rat skin. The binary solvent mixture of ethanol and isopropyl myristate （IPM） could markedly enhance the cumulative penetrated amount of letrozole after 8 h （Qs） compared with IPM alone, especially the IPM system containing 20% （w/w） ethanol. Surprisingly, the use of complexation with organic acids facilitated skin permeation of letrozole in the IPM--ethanol （20%, w/w） system. Due to different structures of tested organic acids, their effects on the penetration of letrozole were different. This study showed that the addition of an organic acid in the IPM-cthanol （20%, w/w） system was a promising approach to enhance the skin permeability of letrozole.展开更多
Aim To study the influence of electric field direction on the in vitro enhanced transdermal delivery of caffeine by eleetroporation. Methods Using side-by-side compartment diffusion cells method and Ag-Ag/AgCl electro...Aim To study the influence of electric field direction on the in vitro enhanced transdermal delivery of caffeine by eleetroporation. Methods Using side-by-side compartment diffusion cells method and Ag-Ag/AgCl electrodes, the transport of caffeine through human cadaver skin by electroporation （exponentially decaying pulse, pulse voltage = 350 V, pulse frequency = 4 pulses· min^-1, capacity = 22 μF, pulse length = 7 ms, 25 pulses） with different electric field directions was carried out and compared with passive diffusion and iontophoresis （0.25 mA·cm^ - 2, lasted for 4 h）. Results （i） The cumulative quantity and flux of caffeine through human skin were increased significantly by eleetroporation or iontophoresis. （ii） The transport of caffeine by positive iontophoresis （ with electric field from donor to receptor compartment） was significantly greater than that by negative iontophoresis （with electric field from receptor to donor compartment）. （iii） The transport of caffeine by positive eleetroporation （with electric field from donor to receptor compartment） was similar to that by negative eleetroporation （with electric field from receptor to donor compartment）. （iv） The enhancing effect of positive iontophoresis on the transdermal delivery of caffeine was significantly greater than that of electroporation （positive or negative）. Conclusion Electric field direction significantly influences the enhancing effect of iontophoresis on the transdermal delivery of caffeine, but does not influence the enhancing effect of eleetroporation.展开更多
With the development of pharmaceutics and other disciplines theories and advanced technologies, the application of many new drug delivery systems has gradually increased in clinical veterinary. Among the many drug del...With the development of pharmaceutics and other disciplines theories and advanced technologies, the application of many new drug delivery systems has gradually increased in clinical veterinary. Among the many drug delivery systems, transdermal patch can maintain stable and effective plasma concentration and therapeutic effect in vivo for a long time after skin dressing delivery, which provides a safe and effective drug-delivery way for the therapy and prevention of some chronic diseases and partial analgesia in a simple and convenient way. Veterinary drug transdermal preparations have been developed both at home and abroad, and satisfactory results have been achieved in the experimental application. Based on the study of veterinary transdermal patches at home and abroad, this paper systematically describes the development and characteristics of transdermal patches, the factors affecting skin permeation and the evaluation this type of preparations in veterinary drugs.展开更多
基金supported by National Research Foundation of Korea(NRF)grants funded by the Korean government(MSIT)(No.RS-2023-00256265,RS-2024-00352352,RS-2024-00405818)the Korean Fund for Regenerative Medicine(KFRM)grant funded by the Korea government(the Ministry of Science and ICT,the Ministry of Health&Welfare).(No.25A0102L1)support from the Market-led K-sensor technology program(RS-2022-00154781,Development of large-area wafer-level flexible/stretchable hybrid sensor platform technology for form factor-free highly integrated convergence sensor),funded By the Ministry of Trade,Industry&Energy(MOTIE,Korea).
文摘Microneedles(MNs)have been extensively investigated for transdermal delivery of large-sized drugs,including proteins,nucleic acids,and even extracellular vesicles(EVs).However,for their sufficient skin penetration,conventional MNs employ long needles(≥600μm),leading to pain and skin irritation.Moreover,it is critical to stably apply MNs against complex skin surfaces for uniform nanoscale drug delivery.Herein,a dually amplified transdermal patch(MN@EV/SC)is developed as the stem cell-derived EV delivery platform by hierarchically integrating an octopusinspired suction cup(SC)with short MNs(≤300μm).While leveraging the suction effect to induce nanoscale deformation of the stratum corneum,MN@EV/SC minimizes skin damage and enhances the adhesion of MNs,allowing EV to penetrate deeper into the dermis.When MNs of various lengths are applied to mouse skin,the short MNs can elicit comparable corticosterone release to chemical adhesives,whereas long MNs induce a prompt stress response.MN@EV/SC can achieve a remarkable penetration depth(290μm)for EV,compared to that of MN alone(111μm).Consequently,MN@EV/SC facilitates the revitalization of fibroblasts and enhances collagen synthesis in middle-aged mice.Overall,MN@EV/SC exhibits the potential for skin regeneration by modulating the dermal microenvironment and ensuring patient comfort.
基金supported by the National Natural Science Foundation of China(Nos.81872823,82073782,and 82241002)the Key R&D Plan of Ganjiang New District of Jiangxi(No.2023010).
文摘Candida albicans is one of the most common pathogens causing invasive fungal infections,with a mortality rate of up to 20%-50%.Amphotericin B(AmB),a biopharmaceutics classification system(BCS)IV drug,significantly inhibits Candida albicans.AmB is primarily administered via oral and intravenous infusion,but severe infusion adverse effects,nephrotoxicity,and potential hepatotoxicity limit its clinical application.Deep eutectic solvents(DESs),with excellent solubilization ability and skin permeability,are attractive for transdermal delivery.Herein,we used DESs to deliver AmB for antifungal therapy transdermally.We first prepared and characterized DESs with different stoichiometric ratios of choline(Ch)and geranate(Ge).DESs increased the solubility of AmB by a thousand-fold.In vitro and in vivo,skin permeation studies indicated that DES_(1:2)(Ch and Ge in 1:2 ratio)had the most outstanding penetration and delivered fluorescence dye to the dermis layer.Then,DES_(1:2)-AmB was prepared and in vitro antifungal tests demonstrated that DES_(1:2)-AmB had superior antifungal effects compared to AmB and DES_(1:2).Furthermore,DES_(1:2)-AmB was skin-irritating and biocompatible.In conclusion,DES-AmB provides a new and effective therapeutic solution for fungal infections.
基金supported by the Joint Funds of National Natural Science Foundation of China(No.U22A20162)the Natural Science Foundation of Hebei Province of China(No.C2021202002)+1 种基金the National Natural Science Foundation of China(No.52271245),the Natural Science Foundation of Tianjin(No.21JCQNJC01280)the financial support from the Danish Council for Independent Research(9040-00219B),European Union’s Horizon 2020 research and innovation program under the Marie Skłodowska-Curie grant agreement ENSIGN(Project ID:101086226),L4DNANO(Project ID:101086227).
文摘Microneedle(MN)patches could be a promising treatment for diabetic foot ulcers that plague thousands of people worldwide.While reducing skin resistance or increasing driving force can accelerate the efficiency of transdermal drug delivery with conventional MN patches,it can create toxic chemical residues or require the help of additional devices.Herein,a thermo-responsive microneedles patch(TMN)with high biocompatibility without additional equipment is proposed.The TMN consisted of a bilayer microneedles composed of sodium alginate(SA)-g-poly(N-isopropylacrylamide)layer(SA-g-PNIPAM)loaded with sucrose octasulfate sodium salt(SOS)and hyaluronic acid layer and a polycaprolactone/chitosan nanofiber membrane loading with tetracycline hydrochloride(TH)and SOS.PNIPAM accelerates drug release by extruding the drug through a volumetric phase transition in response to temperature changes,and TH and SOS promote wound healing by inhibiting bacterial growth and promoting vascular regeneration and epithelial formation.The results showed that the drug release of TMN was significantly faster,with the drug release rate of more than 80% in the 10th h,and the antibacterial rate of TMN could reach 800%.In addition,TMN had good biocompatibility and good healing effects in vivo,which may be helpful for the design of multifunctional dressings in the future.
基金supported by the National Natural Science Foundation of China(No.82072044)the Qing Lan Project of Jiangsu Province of China。
文摘Diabetic pressure ulcers(DPU)are non-healing due to vascular dysfunction and bacterial infection.Early intervention can delay ulcer progression,such as preventing the formation of full-thickness skin defects.Local administration of deferoxamine(DFO)at wound sites has been shown to promote neovascularization and enhance wound healing.However,since DPU skin wounds are not full-thickness defects and DFO is hydrophilic,enhancing its transdermal delivery is crucial for effective treatment.Photothermal ablation of stratum corneum,generated by copper sulfide nanoparticles(Cu S NPs)under near-infrared(NIR)light irradiation,is a promising method to improve transdermal drug delivery.Meanwhile,Cu S NPs-induced photothermal therapy offers excellent antibacterial performance.In this study,DFO and Cu S NPs were incorporated into a matrix metalloproteinase(MMPs)-sensitive hydrogel.This hydrogel promotes cell adhesion and is degraded by cell-secreted MMPs,a process crucial for the controlled release of encapsulated DFO and Cu S NPs.Under NIR irradiation,the stratum corneum is disrupted,facilitating transdermal DFO delivery and simultaneously eliminating infected bacteria.As a result,the essential requirements for DPU treatment,“facilitating transdermal DFO delivery,promoting angiogenesis,and inhibiting bacterial infection”,were achieved simultaneously.
基金funded by the National Natural Science Foundation of China(82273881 and 82304386)Guangdong Basic and Applied Basic Research Foundation(2022A1515110476)+1 种基金the Open Fund of Guangdong Provincial Key Laboratory of Infectious Diseases and Molecular Immunopathology(GDKL202214)SUMC Scientiffc Research Initiation Grant(510858046 and 510858056).
文摘Ionic liquids (ILs) have been proven to be an effective technology for enhancing drug transdermal absorption. However, due to the unique structural components of ILs, the design of efficient ILs and elucidation of action mechanisms remain to be explored. In this review, basic design principles of ideal ILs for transdermal drug delivery system (TDDS) are discussed considering melting point, skin permeability, and toxicity, which depend on the molar ratios, types, functional groups of ions and inter-ionic interactions. Secondly, the contributions of ILs to the development of TDDS through different roles are described: as novel skin penetration enhancers for enhancing transdermal absorption of drugs;as novel solvents for improving the solubility of drugs in carriers;as novel active pharmaceutical ingredients (API-ILs) for regulating skin permeability, solubility, release, and pharmacokinetic behaviors of drugs;and as novel polymers for the development of smart medical materials. Moreover, diverse action mechanisms, mainly including the interactions among ILs, drugs, polymers, and skin components, are summarized. Finally, future challenges related to ILs are discussed, including underlying quantitative structure-activity relationships, complex interaction forces between anions, drugs, polymers and skin microenvironment, long-term stability, and in vivo safety issues. In summary, this article will promote the development of TDDS based on ILs.
基金supported by the NINGBO Medical & Health Leading Academic Discipline Project (No. 2022-ZF02)Ningbo Major Research and Development Plan Project (No.2023Z207)。
文摘Atopic dermatitis(AD) is a chronic inflammatory skin condition. Natural products have gained traction in AD treatment due to their accessibility, low toxicity, and favorable pharmacological properties. However, their application is primarily constrained by poor solubility, instability, and limited permeability. The transdermal drug delivery system(TDDS) offers potential solutions for transdermal delivery, enhanced penetration, improved efficacy, and reduced toxicity of natural drugs, aligning with the requirements of modern AD treatment. This review examines the application of hydrogels, microneedles(MNs), liposomes, nanoemulsions, and other TDDS-carrying natural products in AD treatment, with a primary focus on their effects on penetration and accumulation in the skin. The aim is to provide valuable insights into the treatment of AD and other dermatological conditions.
基金supported by National Key R&D Program of China (No.2019YFA0110600)National Natural Science Foundation of China (No.81970916)+3 种基金Sichuan Science and Technology Program(No.2022NSFSC0002)Sichuan Province Youth Science and Technology Innovation Team (No.2022JDTD0021)Research and Develop ProgramWest China Hospital of Stomatology Sichuan University (No.RD03202302)。
文摘Melanoma is one of the most malignant skin tumors, whose high invasion is generally associated with BRAF gene mutation. Although new chemotherapeutic drugs, such as vemurafenib, have been developed to inhibit the growth of melanoma, these drugs are usually administered intravenously or orally, resulting in toxic side effects on major tissues and organs. Tetrahedral framework nucleic acids(tFNAs) are a novel type of DNA nanostructures with excellent biocompatibility and versatility which have been proven to penetrate through skin barrier with ease. In this study, we prepared t FNAs with vemurafenib and connected DNA aptamer AS1411 at the apex of t FNAs(AS1411-tFNAs/vemurafenib). On one hand, AS1411-tFNAs/vemurafenib could kill melanoma cells by blocking the mutated BRAF gene in vitro. Compared with free vemurafenib, AS1411-tFNAs/vemurafenib had no obvious toxicity to normal cells. On the other hand,AS1411-tFNAs could transfer vemurafenib to cross through the skin barrier and permeate into tumor tissues. In vivo, transdermal delivery of AS1411-t FNAs/vemurafenib could inhibit the growth of human A375melanoma, whose inhibiting effect was stronger than intravenous administration of vemurafenib. These results demonstrated the application prospects of tFNAs combined with chemotherapeutic drugs in skin tumors.
基金funded by the Fundacao para a Ciencia e Tecnologia,Portugal[UIDB/04138/2020 and UIDP/04138/2020 to iMed.ULisboa,CEECINST/00145/2018 to J Marto,fellowship 2020.10138BD to A.Graca and UI/BD/153624/2022 to S.Bom].
文摘Three-dimensional(3D)printing is an innovative manufacturingmethod with the potential to revolutionize topical and transdermal dosage forms.Nowadays,it is established that Vatbased photopolymerization(VP)3D printing technologies offer superior printing efficiency and versatility compared to other 3D printing technologies available on the market.However,there are some limitations that impair their full application in pharmaceutical contexts,such as the lack of a range of biocompatiblematerials for topical and transdermal applications.This reviewarticle explores all types of VP-based 3D printing and discusses the relevance of implementing this kind of technology.We start with a detailed description of the printing process,focusing on the commercial materials available and lab-made resins proposed by different authors.We also review recent studies in this field,which mainly focus on the fabrication of transdermal devices based on microneedle arrays.In the future,it is expected that the manufacturers of 3D printers invest in modifications to the printing apparatus to allow the simultaneous printing of different resins and/or compound types,which will open frontiers to the personalization of treatment approaches.
基金supported by National Natural Science Foundation of China(Nos.52277150,51977096,12005076 and 52130701)the National Key Research and Development Program of China(No.2021YFE0114700)。
文摘Plasma-enhanced transdermal drug delivery(TDD) presents advantages over traditional methods,including painless application, minimal skin damage, and rapid recovery of permeability. To harness its clinical potential, factors related to plasma’s unique properties, such as reactive species and electric fields, must be carefully considered.This review provides a concise summary of conventional TDD methods and subsequently offers a comprehensive examination of the current state-of-the-art in plasma-enhanced TDD. This includes an analysis of the impact of plasma on HaCaT human keratinocyte cells, ex vivo/in vivo studies, and clinical research on plasma-assisted TDD. Moreover, the review explores the effects of plasma on skin physical characteristics such as microhole formation, transepidermal water loss(TEWL), molecular structure of the stratum corneum(SC), and skin resistance. Additionally, it discusses the involvement of various reactive agents in plasma-enhanced TDD, encompassing electric fields,charged particles, UV/VUV radiation, heat, and reactive species. Lastly, the review briefly addresses the temporal behavior of the skin after plasma treatment, safety considerations, and potential risks associated with plasma-enhanced TDD.
基金supported by the National Natural Scientific Foundation(82172186)Beijing Natural Scientific Foundation(L222126).
文摘Objective:To find a viable alternative to reduce the number of doses required for the patients with post-traumatic stress disorder(PTSD),and to improve efficacy and patient compliance.Methods: In this study,we used ginger oil,a phytochemical with potential therapeutic properties,to prepare ginger oil patches.High-performance liquid chromatography(HPLC)was used to quantify the main active component of ginger oil,6-gingerol.Transdermal absorption experiments were conducted to optimize the various pressure-sensitive adhesives and permeation enhancers,including their type and concentration.Subsequently,the ginger oil patches were optimized and subjected to content determination and property evaluations.A PTSD mouse model was established using the foot-shock method.The therapeutic effect of ginger oil patches on PTSD was assessed through pathological sections,behavioral tests,and the evaluation of biomarkers such as tumor necrosis factor-α(TNF-α),interleukin-6(IL-6),brain-derived neurotrophic factor(BDNF),and melatonin(MT).Results: The results demonstrated that ginger oil patches exerted therapeutic effects against PTSD by inhibiting inflammatory responses and modulating MT and BDNF levels.Pharmacokinetic experiments revealed that ginger oil patches maintained a stable blood drug concentration for at least one day,addressing the rapid metabolism drawback of 6-gingerol and enhancing its therapeutic efficacy.Conclusions: Ginger oil can be prepared as a transdermal drug patch that meets these requirements,and the bioavailability of the prepared patch is better than that of oral administration.It can improve PTSD with good patient compliance and ease of administration.Therefore,it is a promising therapeutic formulation for the treatment of PTSD.
文摘Transdermal medications are an useful yet underutilized tool in the field of psychiatry.Despite numerous advantages of using this route of medication delivery,transdermal medications remain less popular compared to other routes of medication administration such as oral and intramuscular routes in the management of various psychiatric conditions.In this editorial,we examine the advantages of transdermal medications with a brief overview of transdermal being used in psychiatry and other medical specialties.We discuss the factors that play a role in their limited usage in psychiatry.We highlight certain patient categories who can specifically benefit from them and discuss potential solutions that can broaden the perspective of treating clinicians making this an intriguing avenue in the field of psychiatry.
文摘Transdermal drug delivery offers a promising alternative to traditional cancer therapies by providing a non-invasive,controlled,and targeted delivery of therapeutic agents.This paper explores the advancements,benefits,and challenges associated with transdermal drug delivery systems(TDDS)in cancer treatment.It highlights the mechanisms of action,key technologies,and the potential impact on patient outcomes.By examining recent studies and clinical trials,this paper aims to provide a comprehensive overview of the efficacy,safety,and prospects of transdermal drug delivery in oncology.
文摘Aim To prepare triamcinolone-acetonide-acetate (TAA)-loaded solid lipidnanoparticles (SLN) carbomer gel with tripalmitin glyceride (TPG), and investigate theircharacteristics and transdermal drug delivery. Methods SLN suspension was prepared by high-pressurehomogenization technique, and then mixed with carbomer gel matrix to get SLN gel. The morphology,particle size with polydispersi-ty index (PI) and zeta potential were examined by atomic forcemicroscopy (AFM) and photon correlation spectroscopy (PCS). The entrapment efficiency, stability andin vitro drug release were also studied. The transdermal drug delivery through porcine ear skin wasevaluated using modified Franz diffusion cells. Results The SLN had a spherical shape with theaverage size of (95.5 - 186.2) nm, the zeta potential of (-26.3- -15.7) mV and the entrapmentefficiency of 67.4%-90.3% for different TAA encapsulated compounds. TAA-SLN carbomer gel had goodstability, the release profile in vitro fitted Higuchi equation. In comparison with conventionalhydrogels, TAA-SLN carbomer gel resulted in higher drug permeation amount and drug deposition withinporcine ear skin after 24 h penetration experiment. Conclusion TAA-SLN carbomer gel is preparedwith stable physicochemical properties. The release profile and improved drug permeation into skinmake it be a promising vehicle for transdermal drug delivery.
文摘Objective: Objective: To assess the effect and adverse effects of transdermal fentanyl for elderly patients with cancer pain in China. Methods: A total of 1664 elderly patients (aged 65-90 with mean age of 72.6) with cancer pain enrolled in the multicenter study from 136 institutes in China. Of them, 408 (28.8%) patients were 75 years old or older. All patients received transdermal fentanyl for the management of cancer pain. The patients were asked to record the attacks of pain, quality of life, and any side effects of the treatment. Results: Baseline mean of pain intensity was 7.34. On day 1, 3, 6, 9 15, and 30, the pain mean scores were decreased to 3.82, 2.80, 2.43, 2.11, 1.83, 1.64 (P=0.000). The effective rate was 97.18%. The mean doses of fentanyl was 31.34 g/h (25-150 g/h) initially, and 40.59 g/h and 47.50 g/h (25-200 g/h) at day 15 and day 30. At treatment day 15, the dose of fentanyl was ranger from 25 to 50 g/h in 91.8% of patients, 75 to 100 g/h in 7.5% patients, and 125 to 200 g/h only in 0.8% patients. The fine quality of life was in 25.4% patients before treatment, and was 71.15% and 73.04% at day 15 and day 30 respectively (P=0.0000). The common side effects were constipation (10.70%), nausea (11.96%), dizzy (6.85%), vomiting (3.85%), sedation (2.40%), Respiratory depression (0.12%). 86.2% patients preferred continue treated by transdermal fentanyl. Conclusions: Transdermal fentanyl for the elderly with cancer pain is effective, safe, convenient, and can improve the quality of life. Transdermal fentanyl can be recommended as a first-line drug for the treatment of elderly patients with moderate to severe cancer pain, and the initial doses is recommended as 25 g/h.
基金The Key Direction Program of Chinese Academy of Sciences(Grant No.kjcx2-sw-h12-01)
文摘One major problem encountered in transdermal drug delivery is the low permeability of drugs through the skin barrier. In the present study, we developed a surfactant-ethanolic liposomal system to improve the transdermal delivery of docetaxel （DTX）, a model drug for high molecular weight and poorly water-soluble drugs. Surfactant-ethanolic liposomes （SEL） were composed of phospholipids, ethanol, sodium cholate, DTX and PBS which were prepared by thin film dispersion method. The developed formulations were characterized by determining the vesicle shape and surface morphology, size and size distribution, entrapment efficiency and drug loading capacity. The effects of the developed formulations on the permeation of DTX across rat skin in vitro were investigated using the modified Franz diffusion cell under both occlusive and non-occlusive application condi- tions. The DTX SELs with optimum composition （phospholipid-surfactant, 85：15, w/w） provided a significantly higher steadystate amount of flux and cumulative permeation, compared to the tranditional liposomes, surfactant liposomes and ethanolic liposomes. The optimal SELs exhibited stable vesicle size, morphology and drug loading capacity. Our results indicated that SELs were promising carriers to enhance the transdermal delivery of DTX.
基金‘863'High Technology R&D Project of Ministry of Science and Technology of China(Grant No.2004AA2Z3073).
文摘The objective of the present study is to examine cardiovascular protective action of a newly developed transdermal patch by incorporating bisoprolol and isosorbide dinitrate in spontaneously hypertensive rats. As the combination therapy with these two synergistic drugs at low doses through a suitable form of administration could provide optimal therapeutic benefit, we further evaluated the effects of a 42 d period of anti-hypertensive treatment in spontaneously hypertensive rats. Rats were divided into the following five groups： control （blank patch）, bisoprolol fumarate tablets （BP-FT, 20.0 mg/kg, i.g.）, bisoprolol transdermal patch （BP-TP, 20.0 mg/kg）, isosorbide dinitrate transdermal patch （ISDN-TP, 20.0 mg/kg）, and the combination of BP and ISDN in a transdermal patch at low doses （8 and 12 mg/kg, respectively）. The effects of treatment were evaluated via biochemical indicators related to cardiovascular protection, structure and function. The combination therapy had synergistic anti-hypertensive effects and significantly reduced blood pressure with the benefit of controlling blood pressure variability compared to BP-FT and BP-TP. The combined treatment also reduced heart rate as well as BP-FT and BP-TP, while ISDN-TP had no evident effects on blood pressure, heart rate, and cardiovascular protection. Combination therapy was superior to BP-TP and BP-FT at increasing blood atrial natriuretic peptide and nitric oxide, while also reducing cardiac hydroxyproline and endothelin-1 with no difference in blood endothelin-1 and cardiac malondialdehyde levels. Cardiovascular remodeling differed among the groups, with the combination therapy reducing cardiac hypertrophy and the aortic media/lumen ratio. The consequential improvements in relaxation in response to cumulative concentrations of acetylcholine may explain the associated improvement in endothelial function. Combi- nation treatment with a transdermal patch exhibited a synergistic therapeutic effect. Such favorable cardiovascular effects with nitric oxide donors and β-blockade combination through a transdermal patch may provide long-term cardiovascular protection during anti-hypertensive treatment.
文摘Chronic pain lasting more than 3 mo,or even several years can lead to disability.Treating chronic pain safely and effectively is a critical challenge faced by clinicians.Because administration of analgesics through oral,intravenous or intramuscular routes is not satisfactory,research toward percutaneous delivery has gained interest.The transdermal patch is one such percutaneous delivery system that can deliver drugs through the skin and capillaries at a certain rate to achieve a systemic or local therapeutic effect in the affected area.It has many advantages including ease of administration and hepatic first pass metabolism avoidance as well as controlling drug delivery,which reduces the dose frequency and side effects.If not required,then the patch can be removed from the skin immediately.The scopolamine patch was the first transdermal patch to be approved for the treatment of motion sickness by the Food and Drug Administration in 1979.From then on,the transdermal patch has been widely used to treat many diseases.To date,no guidelines or consensus are available on the use of analgesic drugs through transdermal delivery.The pain branch of the Chinese Medical Association,after meeting and discussing with experts and based on clinical evidence,developed a consensus for promoting and regulating standard use of transdermal patches containing analgesic drugs.
文摘The purpose of this study was to investigate the effects of vehicles and organic acids on the in vitro permeation of letrozole across rat skin. Permeation experiments were carried out with 2-chamber diffusion cells through rat skin. The binary solvent mixture of ethanol and isopropyl myristate （IPM） could markedly enhance the cumulative penetrated amount of letrozole after 8 h （Qs） compared with IPM alone, especially the IPM system containing 20% （w/w） ethanol. Surprisingly, the use of complexation with organic acids facilitated skin permeation of letrozole in the IPM--ethanol （20%, w/w） system. Due to different structures of tested organic acids, their effects on the penetration of letrozole were different. This study showed that the addition of an organic acid in the IPM-cthanol （20%, w/w） system was a promising approach to enhance the skin permeability of letrozole.
文摘Aim To study the influence of electric field direction on the in vitro enhanced transdermal delivery of caffeine by eleetroporation. Methods Using side-by-side compartment diffusion cells method and Ag-Ag/AgCl electrodes, the transport of caffeine through human cadaver skin by electroporation （exponentially decaying pulse, pulse voltage = 350 V, pulse frequency = 4 pulses· min^-1, capacity = 22 μF, pulse length = 7 ms, 25 pulses） with different electric field directions was carried out and compared with passive diffusion and iontophoresis （0.25 mA·cm^ - 2, lasted for 4 h）. Results （i） The cumulative quantity and flux of caffeine through human skin were increased significantly by eleetroporation or iontophoresis. （ii） The transport of caffeine by positive iontophoresis （ with electric field from donor to receptor compartment） was significantly greater than that by negative iontophoresis （with electric field from receptor to donor compartment）. （iii） The transport of caffeine by positive eleetroporation （with electric field from donor to receptor compartment） was similar to that by negative eleetroporation （with electric field from receptor to donor compartment）. （iv） The enhancing effect of positive iontophoresis on the transdermal delivery of caffeine was significantly greater than that of electroporation （positive or negative）. Conclusion Electric field direction significantly influences the enhancing effect of iontophoresis on the transdermal delivery of caffeine, but does not influence the enhancing effect of eleetroporation.
基金Supported by the Program for Technology Research and Development and Its Demonstration and Popularization of Beijing Vocational College of Agriculture(XY-YF-15-08)~~
文摘With the development of pharmaceutics and other disciplines theories and advanced technologies, the application of many new drug delivery systems has gradually increased in clinical veterinary. Among the many drug delivery systems, transdermal patch can maintain stable and effective plasma concentration and therapeutic effect in vivo for a long time after skin dressing delivery, which provides a safe and effective drug-delivery way for the therapy and prevention of some chronic diseases and partial analgesia in a simple and convenient way. Veterinary drug transdermal preparations have been developed both at home and abroad, and satisfactory results have been achieved in the experimental application. Based on the study of veterinary transdermal patches at home and abroad, this paper systematically describes the development and characteristics of transdermal patches, the factors affecting skin permeation and the evaluation this type of preparations in veterinary drugs.
