Naturally degradable capsule provides a platform for sustained fragrance release.However,practical challenges such as low encapsulation efficiency and difficulty in sustained release are still limited in using fragran...Naturally degradable capsule provides a platform for sustained fragrance release.However,practical challenges such as low encapsulation efficiency and difficulty in sustained release are still limited in using fragranceloaded capsules.In this work,the natural materials sodium alginate and gelatine are dissolved and act as the aqueous phase,lavender is dissolved in caprylic/capric triglyceride(GTCC)as the oil phase,and SiO_(2) nanoparticles with neutralwettability as a solid emulsifier to form O/W Pickering emulsions simultaneously.Finally,multi-core capsules are prepared using the drop injection method with emulsions as templates.The results show that the capsules have been successfully prepared with a spherical morphology and multi-core structure,and the encapsulation rate of multi-core capsules can reach up to 99.6%.In addition,the multi-core capsules possess desirable sustained release performance,the cumulative sustained release rate of fragrance at 25℃over 49 days is only 32.5%.It is attributed to the significant protection of multi-core structure,Pickering emulsion nanoparticle membranes,and hydrogel network shell for encapsulated fragrance.This study is designed to deliver a new strategy for using sustained-release technology with fragrance in food,cosmetics,textiles,and other fields.展开更多
H_(2)O_(2)is an environmentally friendly oxidizing agent with minimal secondary pollution;however,its application has always been constrained by factors such as storage and transportation.In this study,we propose an i...H_(2)O_(2)is an environmentally friendly oxidizing agent with minimal secondary pollution;however,its application has always been constrained by factors such as storage and transportation.In this study,we propose an innovative method for storing and releasing H_(2)O_(2)using hydrogels.Commercial hydrogels(sodium polyacrylate)can undergo swelling and absorb H_(2)O_(2)in aqueous solutions,and the swollen hydrogel can continuously release H_(2)O_(2)under osmotic pressure.And the characteristics of osmotic pressure drive ensure the recyclability of hydrogel for H_(2)O_(2)storage.Experimental results demonstrate that H_(2)O_(2)can stably exist within the hydrogel for an extended period,and this strategy helps to avoid explosion the risk and potential environmental hazards during the transportation of H_(2)O_(2).Finally,experiments confirm that the hydrogel controlled sustained release of H_(2)O_(2)is effective in both Fenton reactions and the process of bacterial inactivation.This work introduces new ideas for the storage of H_(2)O_(2),and the sustained release of H_(2)O_(2)may have significant implications in the fields of healthcare,environmental science,catalysis,and beyond.展开更多
Aim To prepare the sustained release melatonin tablet with HPMC matrix and study its pharmacokinetics and bioavailatility. Methods HPMC was used as matrix to formulate the sustained release tablet. The influences of t...Aim To prepare the sustained release melatonin tablet with HPMC matrix and study its pharmacokinetics and bioavailatility. Methods HPMC was used as matrix to formulate the sustained release tablet. The influences of the size of melatonin, type and amount of HPMC, drug loading, type and amount of additives, and compressing pressure were investigated. Plasma concentration of melatonin in dogs after intravenous injection of two doses and oral administration of sustained release tablets and unmodified release capsules was detected by HPLC using fluorescence detector. Results The drug release from sustained release tablets was influenced by the size of melatonin, type and amount of HPMC, drug loading, and type and amount of additives. Melatonin was found to fit two compartment model after intravenous injection, AUC was proportional to doses, and t(1/2β) of two doses has no significant difference. Relative bioavailability of melatonin sustained release tablet to normal capsule was 83.8%, and absolute bioavailability was 3.75% for sustained release tablet and 4.49% for capsule. Conclusion The melatonin sustained release tablet was well formulated. The absolute bioavilability for oral administration of either sustained release tablet or unmodified release capsule of melatonin was less than 5%. The bioavailability of melatonin sustained release tablet was lower than that of unmodified release capsule, but MRT of sustained release tablet was significantly longer than that of capsule.展开更多
To investigate the pharmacokinetic characteristics of moclobemide sustainedrelease tablets after multiple oral dose administration in healthy Chinese volunteers. MethodsMoclobemide sustained release tablets were given...To investigate the pharmacokinetic characteristics of moclobemide sustainedrelease tablets after multiple oral dose administration in healthy Chinese volunteers. MethodsMoclobemide sustained release tablets were given as a multiple oral dose regimen of 300 mg oncedaily for five consecutive days to 12 healthy volunteers. The concentrations of moclobemide inplasma were determined by reversed-phase high performance liquid chromatography. The partialpharmacokinetic parameters were calculated using 3p97 pharmacokinetic program. Results Theconcentration-time profile fitted an one-compartment model best. The steady-state pharmacokineticparameters of moclobemide sustained release tablets after multiple oral doses were as follows:C_(max) was (1 950 +- 156) μg· L^(-1), T_(max) was (6.00 +-1.55) h, T_(1/2(kel)) was (3.14 +-0.12)h, AUC_(ss 0-24) was (22 836 +- 1 842) μg·h· L^(-1), MRT was (7.68+-0.36) h, CL/F_((s)) was(20.2+-2.1) L·h^(-1), and V/F_((c)) was (91.4+-9.4) L, respectively. No marked adverse events werenoted during this study. Conclusion The formulation has a sustained-release effect and goodtolerance in the healthy volunteers, which provides useful information for clinical practice.展开更多
Exosomes derived from mesenchymal stem cells are of therapeutic interest because of their important role in intracellular communication and biological regulation.On the basis of previously studied nerve conduits,we de...Exosomes derived from mesenchymal stem cells are of therapeutic interest because of their important role in intracellular communication and biological regulation.On the basis of previously studied nerve conduits,we designed a polydopamine-modified chitin conduit loaded with mesenchymal stem cell-derived exosomes that release the exosomes in a sustained and stable manner.In vitro experiments revealed that rat mesenchymal stem cell-derived exosomes enhanced Schwann cell proliferation and secretion of neurotrophic and growth factors,increased the expression of Jun and Sox2 genes,decreased the expression of Mbp and Krox20 genes in Schwann cells,and reprogrammed Schwann cells to a repair phenotype.Furthermore,mesenchymal stem cell-derived exosomes promoted neurite growth of dorsal root ganglia.The polydopamine-modified chitin conduits loaded with mesenchymal stem cell-derived exosomes were used to bridge 2 mm rat sciatic nerve defects.Sustained release of exosomes greatly accelerated nerve healing and improved nerve function.These findings confirm that sustained release of mesenchymal stem cell-derived exosomes loaded into polydopamine-modified chitin conduits promotes the functional recovery of injured peripheral nerves.展开更多
The purpose of this study was to develop a PLGA microspheres-based donepezil(DP)formulation which was expected to sustain release of DP for one week with high encapsulation efficiency(EE).DP derived from donepezil hyd...The purpose of this study was to develop a PLGA microspheres-based donepezil(DP)formulation which was expected to sustain release of DP for one week with high encapsulation efficiency(EE).DP derived from donepezil hydrochloride was encapsulated in PLGA microspheres by the O/W emulsion-solvent evaporation method.The optimized formulation which avoided the crushing of microspheres during the preparation process was characterized in terms of particle size,morphology,drug loading and EE,physical state of DP in the matrix and in vitro and in vivo release behavior.DP microspheres were prepared successfully with average diameter of 30m,drug loading of 15.92±0.31%and EE up to 78.79±2.56%.Scanning electron microscope image showed it has integrated spherical shape with no drug crystal and porous on its surface.Differential scanning calorimetry and X-ray diffraction results suggested DP was in amorphous state or molecularly dispersed in microspheres.The Tg of PLGA was increased with the addition of DP.The release profile in vitro was characterized with slow but continuous release that lasted for about one week and fitted well with first-order model,which suggested the diffusion governing release mechanism.After single-dose administration of DP microspheres via subcutaneous injection in rats,the plasma concentration of DP reached peak concentration at 0.50 d,and then declined gradually,but was still detectable at 15 d.A good correlation between in vitro and in vivo data was obtained.The results suggest the potential use of DP microspheres for treatment of Alzheimer’s disease over long periods.展开更多
Environmental cleaning is an important aspect of bacteria control.Ethyl cellulose microcapsules containing potassium monopersulfate(PMCM)were prepared by emulsified solvent diffusion method.The chemical structure and ...Environmental cleaning is an important aspect of bacteria control.Ethyl cellulose microcapsules containing potassium monopersulfate(PMCM)were prepared by emulsified solvent diffusion method.The chemical structure and microstructure of the obtained PMCM was characterized by methods of Fourier transform infrared spectroscopy(FT-IR),optical microscopy,scanning electron microscopy and X-ACT energy dispersive X-ray spectroscopy.The SEM micrographs of the PMCM containing 21.6%of C,46.8%of O,10.7%of S and 19.4%of K was relatively smooth.Thermal stability,sustained release performance,and antimicrobial activity of PMCM were investigated.The results showed that the drug loading and encapsulation efficiency of PMCM were 30.3%and 42.6%respectively.Potassium monopersulfate was fully released after 8 h,following a Fickian diffusion mechanism.Results showed that the microcapsules prepared with a high concentration of potassium monopersulfate solution showed a good antimicrobial effect.The microcapsule wall of the resulting PMCM increased with increasing ethyl cellulose content and had high thermal stability from the data of 69%residue rate.The excellent thermal stability and high sustained release performance of PMCM showed high application value.展开更多
Parenteral sustained release drug formulations, acting as preferable platforms for longterm exposure therapy, have been wildly used in clinical practice. However, most of these delivery systems must be given by hypode...Parenteral sustained release drug formulations, acting as preferable platforms for longterm exposure therapy, have been wildly used in clinical practice. However, most of these delivery systems must be given by hypodermic injection. Therefore, issues including needle-phobic, needle-stick injuries and inappropriate reuse of needles would hamper the further applications of these delivery platforms. Microneedles (MNs) as a potential alternative system for hypodermic needles can benefit from minimally invasive and self-administration. Recently, polymeric microneedle-mediated sustained release systems (MN@SRS) have opened up a new way for treatment of many diseases. Here, we reviewed the recent researches in MN@SRS for transdermal delivery, and summed up its typical design strategies and applications in various diseases therapy, particularly focusing on the applications in contraception, infection, cancer, diabetes, and subcutaneous disease. An overview of the present clinical translation difficulties and future outlook of MN@SRS was also provided.展开更多
Coated microneedles(MNs) are widely used for delivering biopharmaceuticals. In this study, a novel gel encapsulated coated MNs(GEC-MNs) was developed. The water-soluble drug coating was encapsulated with sodium algina...Coated microneedles(MNs) are widely used for delivering biopharmaceuticals. In this study, a novel gel encapsulated coated MNs(GEC-MNs) was developed. The water-soluble drug coating was encapsulated with sodium alginate(SA) in situ complexation gel. The manufacturing process of GEC-MNs was optimized for mass production. Compared to the water-soluble coated MNs(72.02% ± 11.49%), the drug delivery efficiency of the optimized GEC-MNs(88.42% ± 6.72%) was steadily increased, and this improvement was investigated through in vitro drug release. The sustained-release of BSA was observed in vitro permeation through the skin. The rhIFN α-1 b GEC-MNs was confirmed to achieve biosafety and 6-month storage stability. Pharmacokinetics of rhIFN α-1 b in GEC-MNs showed a linearly dosedependent relationship. The AUC of rhIFN α-1 b in GEC-MNs(4.51 ng/ml ·h) was bioequivalent to the intradermal(ID) injection(5.36 ng/ml ·h) and significantly higher than water-soluble coated MNs(3.12 ng/ml ·h). The rhIFN α-1 b elimination half-life of GEC-MNs, soluble coated MNs, and ID injection was 18.16, 1.44, and 2.53 h, respectively. The complexation-based GECMNs have proved to be more efficient, stable, and achieve the sustained-release of watersoluble drug in coating MNs, constituting a high value to biopharmaceutical.展开更多
A supramolecular nanoparticle that realized the loading and sustained release of ATP was successfully constructed from sulfato-b-cyclodextrin（SCD） and polyethylenimine（PEI）. The assembly and disassembly behaviors ...A supramolecular nanoparticle that realized the loading and sustained release of ATP was successfully constructed from sulfato-b-cyclodextrin（SCD） and polyethylenimine（PEI）. The assembly and disassembly behaviors of supramolecular nanoparticle were investigated by means of Tyndall effect,UV–vis spectroscopy, dynamic light scattering（DLS）, zeta potential and transmission electron microscopy（TEM）. Significantly, the resulting nanoparticle was disrupted with the increasing of p H and recovered to the spherical nanoparticle as the p H decreased to initial value. Owing to the positive zeta potential, the supramolecular nanoparticle showed the good loading and sustained release abilities towards ATP.展开更多
Development of functional bioinspired hydrogels that have good releases control character is necessary for the application of these materials in biomedical engineering.Herein,we report a composite hydrogel prepared fr...Development of functional bioinspired hydrogels that have good releases control character is necessary for the application of these materials in biomedical engineering.Herein,we report a composite hydrogel prepared from several biocompatible carboxymethyl konjac glucomannan(CKGM)/gelatin(G)/tannic acid(TA)functional nano-hydroxyapatite(TA@n-HA),which has good biodegradability and pH sensitivity.The mechanism of interaction between hydrogels was confirmed by Fourier transform infrared spectroscopy,X-ray diffraction,Scanning electron microscopy and Thermogravimetric analysis.The physico-chemical properties of CKGM/G hydrogels have been significantly improved through the incorporation of TA@n-HA within the matrix.Studies in the sustained release of epigallocatechin gallate(EGCG)demonstrated that the TA@n-HA/CKGM/G hydrogels exhibit not only better pH sensitive properties,but also enhanced biocompatibility and encapsulation in comparison to the matrix devoid of TA@n-HA.Consequently,TA@n-HA/CKGM/G hydrogels using EGCG as a drug release model show the potential for drug delivery.展开更多
Melanoma treatment has been revolutionized with the development of targeted therapies and immunotherapies,which shows a positive influence on the patients.However,the long-term efficaciousness of such therapy is restr...Melanoma treatment has been revolutionized with the development of targeted therapies and immunotherapies,which shows a positive influence on the patients.However,the long-term efficaciousness of such therapy is restricted by side effects,limited clinical effects as well as quick resistance to treatment.In this work,we prepared magnetocaloric carrier-free bimetallic hydrogels,named manganese-iron oxide nanocubes@polyethylene glycol-hydrogels(MFO@PEG-Gels),to realize ion-interferential cell cycle arrest for melanoma treatment.In detail,the tumor site was exposed to alternating magnetic field(AMF)after intratumorally injected MFO@PEG-Gels,which generated hyperthermia and promoted the sol-gel phase transition for MFO sustained release.Under the tumor microenvironment,hydrogen peroxide triggered MFO degradation to induce Mn^(2+)and Fe^(3+)release.On one hand,Mn^(2+)blocked G1/S phase through the activation of p27 pathway.On the other hand,Fe^(3+)could arrest the G2/M phase by upregulating the polo-like kinase 4(PLK4)expression as well as inhibiting autolysosome formation to achieve the enhanced cell cycle arrest,thereby promoting the apoptosis of melanoma cells.In summary,this study proposed ion-interferential cell cycle arrest strategy by a multifunctional and injectable magnetic bimetallic hydrogel for melanoma treatment,which provided a secure and sustainable regimen for enhancing antitumor efficacy.展开更多
This study presents an exploration on extending the action of therapeutic proteins by crystallization strategy without new molecular entities generation.Recombinant human interferon a-2b(rhIFN),a model protein drug in...This study presents an exploration on extending the action of therapeutic proteins by crystallization strategy without new molecular entities generation.Recombinant human interferon a-2b(rhIFN),a model protein drug in this case,was crystallized using a hanging drop vapor diffusion method.A novel chelating technique with metal ions was employed to promote crystals formation.The physico-chemical characterization of the protein crystals,including morphology,particle size,X-ray diffraction,circular dichroism and biological potency evaluations were performed.In addition,the in vitro release behavior of rhIFN from crystal lattice suggested an exciting possibility of protein crystals as a longacting formulation.The work described here demonstrates the possibility of spherical crystals of biomacromolecules for controllable delivery application of therapeutic proteins.展开更多
Objective:To explore the effect of metoprolol succinate sustained-release tablets combined with Wenxin Granules in the treatment of coronary heart disease patients with arrhythmia.Methods:The research objects were 50 ...Objective:To explore the effect of metoprolol succinate sustained-release tablets combined with Wenxin Granules in the treatment of coronary heart disease patients with arrhythmia.Methods:The research objects were 50 patients with arrhythmia who were treated in our hospital from September 2019 to September 2020.According to different treatment methods,they were divided into observation group(Wenxin Granule+metoprolol succinate treatment)and control group(metoprolol succinate treatment),25 cases in each group.The curative effects of the two groups were compared.Results:After treatment,there was no significant difference in rnn50,RMSSD,sdnni and SDANN between the two groups(P>0.05).Compared with the control group,the SDNN in the observation group was higher than that in the control group(P<0.05);Before treatment,there was no significant difference in the above indexes between the two groups(P>0.05);The effective rates of the observation group and the control group were 92.00%and 68.00%respectively,and the curative effect of the observation group was higher than that of the control group(P<0.05);There was no significant difference in the incidence of adverse reactions between the two groups(P>0.05).Conclusion:In the treatment of patients with coronary heart disease and arrhythmia,Wenxin Granule Combined with metoprolol succinate sustained-release tablets has significant effect,which can effectively improve the dynamic electrocardiogram indexes of patients,improve the clinical efficacy,and has high safety.展开更多
Stability of liposomes plays a crucial role in drug delivery,especially in oral aspect.The structural modification of liposomes has been the orientation of efforts to improve their stability and enable the controllabi...Stability of liposomes plays a crucial role in drug delivery,especially in oral aspect.The structural modification of liposomes has been the orientation of efforts to improve their stability and enable the controllability of payload release.This study reported a selenylation strategy to optimize the liposomal structure in an attempt to enhance the nanocarrier’s stability,hence the bioavailability of emodin(EM),an active compound with poor water-solubility.EM-loaded selenized liposomes(EM-Se@LPs)were prepared by thin film dispersion followed by in situ reduction technique.The results showed that EM-Se@LPs were provided with enhancive gastrointestinal stability and exhibited sustained release of drug compared with EM-loaded liposomes(EM-LPs).However,the modified liposomes with Se depositing onto the interior and exterior bilayers did not substantially facilitate absorption of EM.The reinforced structure of liposomes irrelevant to absorption was affirmed to be due to good stability and absorbability of EM itself.Nevertheless,the present work provides an alternative option for stabilization of liposomes instead of conventional methods,which may be promising for oral delivery of physiologically unstable and/or poorly absorbed drugs and systemic drug delivery.展开更多
Based on diffusion of nerve growth factor（NGF） from degradable material,a novel nerve guidance conduit（NGC） with sustained NGF release was prepared by embedding NGF into a degradable RGD-modified composite which h...Based on diffusion of nerve growth factor（NGF） from degradable material,a novel nerve guidance conduit（NGC） with sustained NGF release was prepared by embedding NGF into a degradable RGD-modified composite which has good cell affinity and biocompatibility.In vitro,the NGF release was quantified using enzyme-linked immunosorbent assay method,and the bioactivity of released NGF was examined by PC-12 cell bioassay.In vivo,the performance of the NGF-containing conduit was examined using rat sciatic nerve defect model.The experimental results show that the NGF release process is prolonged over 30 days,and at least some degree of NGF bioactivity is preserved after the fabrication process.Due to the promoting effect of bioactive released NGF on nerve regeneration,the performance of NGC for nerve repair is improved significantly.The results of this study indicate that the sustained NGF release system is suitable for peripheral nerve repair.展开更多
The development and validation of an isocratic high performance liquid chromatographic method is described for the determination of tamsulosin hydrochloride in sustained release tablets. The determination was performe...The development and validation of an isocratic high performance liquid chromatographic method is described for the determination of tamsulosin hydrochloride in sustained release tablets. The determination was performed on a Diamonsil BDS C18 column with a mobile phase consisting of a mixture of acetonitrile, methanol and 0 5% phosphoric acid solution (20∶30∶50, V/V/V ) at a flow rate of 1 0 mL/min. UV detection was made at 274 nm. The linear range for tamsulosin hydrochloride was 0 81-8 10 μg/mL. The mean recovery was 99 8% ( S R=0 7%, n =9), and the precision was found to be 0 45% ( n =9). The proposed method can be used for routine analysis of tamsulosin hydrochloride in sustained release tablets.展开更多
Summary： To study the bioequivalence of a kind of progesterone sustained release suppository, a randomized cross over study was conducted in 12 rabbits. A single rectal dose of 2.75 mg/kg progesterone sustained relea...Summary： To study the bioequivalence of a kind of progesterone sustained release suppository, a randomized cross over study was conducted in 12 rabbits. A single rectal dose of 2.75 mg/kg progesterone sustained released suppository （tested formulation, T） and progesterone suppository （reference formulation, R） was administered; a muhiple dose of 2.75 mg/kg was given up to seven times with an interval of 8 h. Concentrations in serum were determined by a competitive enzyme immunoassay. The main parameters of T were： for single and multiple doses, C was 48.8±11.8 ng/mL and 43.5±9.4 ng/mL. Tmax was 0.5±0.3 h and 0. 4±0.3 h, AUC〈（0-21h） was 362. 4±143 ng·h·mL^-1 and 310.6±70. 3 ng·h·mL^-1 , respectively. The relative bioavailability of T to R were （104.2±13.4） % and （111.4±19. 1） %, respectively. Statistical analysis showed that the two formulations were bioequivalent and T had sustained released feature.展开更多
[Objectives] To study the coating process of paeonol sustained release pills by extrusion-spheronization method taking ethyl cellulose as the coating material. [Methods] Paeonol pills were made by Auari AW-95 Full Aut...[Objectives] To study the coating process of paeonol sustained release pills by extrusion-spheronization method taking ethyl cellulose as the coating material. [Methods] Paeonol pills were made by Auari AW-95 Full Automatic Pill Making Machine. Coating of paeonol sustained release pills was prepared by Auari Mini Pill Polishing Machine. The prescription and process factors of paeonol sustained release pills coating were investigated by single factor experiment and orthogonal experiment. The release of paeonol sustained release pills was determined according to the cumulative release curve of paeonol. [Results] The prepared paeonol sustained release pills released slowly within 24 h, and the release rate reached 80% in 12 h. [Conclusions] The prepared paeonol sustained release pills basically meet the 24 h sustained release standard, and can be further developed and applied.展开更多
文摘Naturally degradable capsule provides a platform for sustained fragrance release.However,practical challenges such as low encapsulation efficiency and difficulty in sustained release are still limited in using fragranceloaded capsules.In this work,the natural materials sodium alginate and gelatine are dissolved and act as the aqueous phase,lavender is dissolved in caprylic/capric triglyceride(GTCC)as the oil phase,and SiO_(2) nanoparticles with neutralwettability as a solid emulsifier to form O/W Pickering emulsions simultaneously.Finally,multi-core capsules are prepared using the drop injection method with emulsions as templates.The results show that the capsules have been successfully prepared with a spherical morphology and multi-core structure,and the encapsulation rate of multi-core capsules can reach up to 99.6%.In addition,the multi-core capsules possess desirable sustained release performance,the cumulative sustained release rate of fragrance at 25℃over 49 days is only 32.5%.It is attributed to the significant protection of multi-core structure,Pickering emulsion nanoparticle membranes,and hydrogel network shell for encapsulated fragrance.This study is designed to deliver a new strategy for using sustained-release technology with fragrance in food,cosmetics,textiles,and other fields.
基金supported by National Natural Science Foundation of China(Nos.22325602,22176060)Program of Shanghai Academic/Technology Research Leader(No.23XD1421000)+2 种基金Project supported by Shanghai Municipal Science and Technology Major Project(No.2018SHZDZX03)the Program of Introducing Talents of Discipline to Universities(No.B16017)Science and Technology Commission of Shanghai Municipality(No.20DZ2250400)。
文摘H_(2)O_(2)is an environmentally friendly oxidizing agent with minimal secondary pollution;however,its application has always been constrained by factors such as storage and transportation.In this study,we propose an innovative method for storing and releasing H_(2)O_(2)using hydrogels.Commercial hydrogels(sodium polyacrylate)can undergo swelling and absorb H_(2)O_(2)in aqueous solutions,and the swollen hydrogel can continuously release H_(2)O_(2)under osmotic pressure.And the characteristics of osmotic pressure drive ensure the recyclability of hydrogel for H_(2)O_(2)storage.Experimental results demonstrate that H_(2)O_(2)can stably exist within the hydrogel for an extended period,and this strategy helps to avoid explosion the risk and potential environmental hazards during the transportation of H_(2)O_(2).Finally,experiments confirm that the hydrogel controlled sustained release of H_(2)O_(2)is effective in both Fenton reactions and the process of bacterial inactivation.This work introduces new ideas for the storage of H_(2)O_(2),and the sustained release of H_(2)O_(2)may have significant implications in the fields of healthcare,environmental science,catalysis,and beyond.
文摘Aim To prepare the sustained release melatonin tablet with HPMC matrix and study its pharmacokinetics and bioavailatility. Methods HPMC was used as matrix to formulate the sustained release tablet. The influences of the size of melatonin, type and amount of HPMC, drug loading, type and amount of additives, and compressing pressure were investigated. Plasma concentration of melatonin in dogs after intravenous injection of two doses and oral administration of sustained release tablets and unmodified release capsules was detected by HPLC using fluorescence detector. Results The drug release from sustained release tablets was influenced by the size of melatonin, type and amount of HPMC, drug loading, and type and amount of additives. Melatonin was found to fit two compartment model after intravenous injection, AUC was proportional to doses, and t(1/2β) of two doses has no significant difference. Relative bioavailability of melatonin sustained release tablet to normal capsule was 83.8%, and absolute bioavailability was 3.75% for sustained release tablet and 4.49% for capsule. Conclusion The melatonin sustained release tablet was well formulated. The absolute bioavilability for oral administration of either sustained release tablet or unmodified release capsule of melatonin was less than 5%. The bioavailability of melatonin sustained release tablet was lower than that of unmodified release capsule, but MRT of sustained release tablet was significantly longer than that of capsule.
文摘To investigate the pharmacokinetic characteristics of moclobemide sustainedrelease tablets after multiple oral dose administration in healthy Chinese volunteers. MethodsMoclobemide sustained release tablets were given as a multiple oral dose regimen of 300 mg oncedaily for five consecutive days to 12 healthy volunteers. The concentrations of moclobemide inplasma were determined by reversed-phase high performance liquid chromatography. The partialpharmacokinetic parameters were calculated using 3p97 pharmacokinetic program. Results Theconcentration-time profile fitted an one-compartment model best. The steady-state pharmacokineticparameters of moclobemide sustained release tablets after multiple oral doses were as follows:C_(max) was (1 950 +- 156) μg· L^(-1), T_(max) was (6.00 +-1.55) h, T_(1/2(kel)) was (3.14 +-0.12)h, AUC_(ss 0-24) was (22 836 +- 1 842) μg·h· L^(-1), MRT was (7.68+-0.36) h, CL/F_((s)) was(20.2+-2.1) L·h^(-1), and V/F_((c)) was (91.4+-9.4) L, respectively. No marked adverse events werenoted during this study. Conclusion The formulation has a sustained-release effect and goodtolerance in the healthy volunteers, which provides useful information for clinical practice.
基金supported by the National Natural Science Foundation of China,Nos.31771322,31571235the National Science Foundation of Beijing,No.7212121+3 种基金Beijing Science Technology New Star Cross Subject,No.2018019Science and Technology Plan Project of Shenzhen,No.JCYJ 20190806162205278the Key Laboratory of Trauma and Neural Regeneration(Peking University),Ministry of Educationa grant from National Center for Trauma Medicine,No.BMU2020XY005-01(all to PXZ).
文摘Exosomes derived from mesenchymal stem cells are of therapeutic interest because of their important role in intracellular communication and biological regulation.On the basis of previously studied nerve conduits,we designed a polydopamine-modified chitin conduit loaded with mesenchymal stem cell-derived exosomes that release the exosomes in a sustained and stable manner.In vitro experiments revealed that rat mesenchymal stem cell-derived exosomes enhanced Schwann cell proliferation and secretion of neurotrophic and growth factors,increased the expression of Jun and Sox2 genes,decreased the expression of Mbp and Krox20 genes in Schwann cells,and reprogrammed Schwann cells to a repair phenotype.Furthermore,mesenchymal stem cell-derived exosomes promoted neurite growth of dorsal root ganglia.The polydopamine-modified chitin conduits loaded with mesenchymal stem cell-derived exosomes were used to bridge 2 mm rat sciatic nerve defects.Sustained release of exosomes greatly accelerated nerve healing and improved nerve function.These findings confirm that sustained release of mesenchymal stem cell-derived exosomes loaded into polydopamine-modified chitin conduits promotes the functional recovery of injured peripheral nerves.
文摘The purpose of this study was to develop a PLGA microspheres-based donepezil(DP)formulation which was expected to sustain release of DP for one week with high encapsulation efficiency(EE).DP derived from donepezil hydrochloride was encapsulated in PLGA microspheres by the O/W emulsion-solvent evaporation method.The optimized formulation which avoided the crushing of microspheres during the preparation process was characterized in terms of particle size,morphology,drug loading and EE,physical state of DP in the matrix and in vitro and in vivo release behavior.DP microspheres were prepared successfully with average diameter of 30m,drug loading of 15.92±0.31%and EE up to 78.79±2.56%.Scanning electron microscope image showed it has integrated spherical shape with no drug crystal and porous on its surface.Differential scanning calorimetry and X-ray diffraction results suggested DP was in amorphous state or molecularly dispersed in microspheres.The Tg of PLGA was increased with the addition of DP.The release profile in vitro was characterized with slow but continuous release that lasted for about one week and fitted well with first-order model,which suggested the diffusion governing release mechanism.After single-dose administration of DP microspheres via subcutaneous injection in rats,the plasma concentration of DP reached peak concentration at 0.50 d,and then declined gradually,but was still detectable at 15 d.A good correlation between in vitro and in vivo data was obtained.The results suggest the potential use of DP microspheres for treatment of Alzheimer’s disease over long periods.
基金support From the Open Fund Project of Key Lab.of Biomass Energy and Material,Jiangsu Province(JSBEM201907)the Ordinary University Young Innovative Talents Project of Guangdong Province(2018KQNCX119).
文摘Environmental cleaning is an important aspect of bacteria control.Ethyl cellulose microcapsules containing potassium monopersulfate(PMCM)were prepared by emulsified solvent diffusion method.The chemical structure and microstructure of the obtained PMCM was characterized by methods of Fourier transform infrared spectroscopy(FT-IR),optical microscopy,scanning electron microscopy and X-ACT energy dispersive X-ray spectroscopy.The SEM micrographs of the PMCM containing 21.6%of C,46.8%of O,10.7%of S and 19.4%of K was relatively smooth.Thermal stability,sustained release performance,and antimicrobial activity of PMCM were investigated.The results showed that the drug loading and encapsulation efficiency of PMCM were 30.3%and 42.6%respectively.Potassium monopersulfate was fully released after 8 h,following a Fickian diffusion mechanism.Results showed that the microcapsules prepared with a high concentration of potassium monopersulfate solution showed a good antimicrobial effect.The microcapsule wall of the resulting PMCM increased with increasing ethyl cellulose content and had high thermal stability from the data of 69%residue rate.The excellent thermal stability and high sustained release performance of PMCM showed high application value.
基金financial support from the National Natural Science Foundation of China (32071342 and 31922042)Guangdong Special Support Program (2019TQ05Y209)the Fundamental Research Funds for the Central Universities (19ykzd31)。
文摘Parenteral sustained release drug formulations, acting as preferable platforms for longterm exposure therapy, have been wildly used in clinical practice. However, most of these delivery systems must be given by hypodermic injection. Therefore, issues including needle-phobic, needle-stick injuries and inappropriate reuse of needles would hamper the further applications of these delivery platforms. Microneedles (MNs) as a potential alternative system for hypodermic needles can benefit from minimally invasive and self-administration. Recently, polymeric microneedle-mediated sustained release systems (MN@SRS) have opened up a new way for treatment of many diseases. Here, we reviewed the recent researches in MN@SRS for transdermal delivery, and summed up its typical design strategies and applications in various diseases therapy, particularly focusing on the applications in contraception, infection, cancer, diabetes, and subcutaneous disease. An overview of the present clinical translation difficulties and future outlook of MN@SRS was also provided.
文摘Coated microneedles(MNs) are widely used for delivering biopharmaceuticals. In this study, a novel gel encapsulated coated MNs(GEC-MNs) was developed. The water-soluble drug coating was encapsulated with sodium alginate(SA) in situ complexation gel. The manufacturing process of GEC-MNs was optimized for mass production. Compared to the water-soluble coated MNs(72.02% ± 11.49%), the drug delivery efficiency of the optimized GEC-MNs(88.42% ± 6.72%) was steadily increased, and this improvement was investigated through in vitro drug release. The sustained-release of BSA was observed in vitro permeation through the skin. The rhIFN α-1 b GEC-MNs was confirmed to achieve biosafety and 6-month storage stability. Pharmacokinetics of rhIFN α-1 b in GEC-MNs showed a linearly dosedependent relationship. The AUC of rhIFN α-1 b in GEC-MNs(4.51 ng/ml ·h) was bioequivalent to the intradermal(ID) injection(5.36 ng/ml ·h) and significantly higher than water-soluble coated MNs(3.12 ng/ml ·h). The rhIFN α-1 b elimination half-life of GEC-MNs, soluble coated MNs, and ID injection was 18.16, 1.44, and 2.53 h, respectively. The complexation-based GECMNs have proved to be more efficient, stable, and achieve the sustained-release of watersoluble drug in coating MNs, constituting a high value to biopharmaceutical.
基金the National Natural Science Foundation of China (Nos. 21432004, 21672113, 21772099 and 91527301) for financial support
文摘A supramolecular nanoparticle that realized the loading and sustained release of ATP was successfully constructed from sulfato-b-cyclodextrin（SCD） and polyethylenimine（PEI）. The assembly and disassembly behaviors of supramolecular nanoparticle were investigated by means of Tyndall effect,UV–vis spectroscopy, dynamic light scattering（DLS）, zeta potential and transmission electron microscopy（TEM）. Significantly, the resulting nanoparticle was disrupted with the increasing of p H and recovered to the spherical nanoparticle as the p H decreased to initial value. Owing to the positive zeta potential, the supramolecular nanoparticle showed the good loading and sustained release abilities towards ATP.
基金financially supported by the National Natural Science Foundation of China(Grant No.31772045)the program on Fujian Agriculture and Forestry University of doctoral students going abroad(Grant No.324-112110089)scientific research foundation graduate school of Fujian Agriculture and Forestry University(Grant No.324-1122yb064)。
文摘Development of functional bioinspired hydrogels that have good releases control character is necessary for the application of these materials in biomedical engineering.Herein,we report a composite hydrogel prepared from several biocompatible carboxymethyl konjac glucomannan(CKGM)/gelatin(G)/tannic acid(TA)functional nano-hydroxyapatite(TA@n-HA),which has good biodegradability and pH sensitivity.The mechanism of interaction between hydrogels was confirmed by Fourier transform infrared spectroscopy,X-ray diffraction,Scanning electron microscopy and Thermogravimetric analysis.The physico-chemical properties of CKGM/G hydrogels have been significantly improved through the incorporation of TA@n-HA within the matrix.Studies in the sustained release of epigallocatechin gallate(EGCG)demonstrated that the TA@n-HA/CKGM/G hydrogels exhibit not only better pH sensitive properties,but also enhanced biocompatibility and encapsulation in comparison to the matrix devoid of TA@n-HA.Consequently,TA@n-HA/CKGM/G hydrogels using EGCG as a drug release model show the potential for drug delivery.
基金supported by National Natural Science Foundation of China(No.82273873)Young Elite Scientists Sponsorship Program by Tianjin(No.0701320001)+2 种基金Major Special Projects(No.0402080005)Natural Science Foundation of Tianjin(No.21JCYBJC00660)Young Program Natural Science Foundation of Tianjin(No.20JCQNJC01610)。
文摘Melanoma treatment has been revolutionized with the development of targeted therapies and immunotherapies,which shows a positive influence on the patients.However,the long-term efficaciousness of such therapy is restricted by side effects,limited clinical effects as well as quick resistance to treatment.In this work,we prepared magnetocaloric carrier-free bimetallic hydrogels,named manganese-iron oxide nanocubes@polyethylene glycol-hydrogels(MFO@PEG-Gels),to realize ion-interferential cell cycle arrest for melanoma treatment.In detail,the tumor site was exposed to alternating magnetic field(AMF)after intratumorally injected MFO@PEG-Gels,which generated hyperthermia and promoted the sol-gel phase transition for MFO sustained release.Under the tumor microenvironment,hydrogen peroxide triggered MFO degradation to induce Mn^(2+)and Fe^(3+)release.On one hand,Mn^(2+)blocked G1/S phase through the activation of p27 pathway.On the other hand,Fe^(3+)could arrest the G2/M phase by upregulating the polo-like kinase 4(PLK4)expression as well as inhibiting autolysosome formation to achieve the enhanced cell cycle arrest,thereby promoting the apoptosis of melanoma cells.In summary,this study proposed ion-interferential cell cycle arrest strategy by a multifunctional and injectable magnetic bimetallic hydrogel for melanoma treatment,which provided a secure and sustainable regimen for enhancing antitumor efficacy.
基金The authors wish to thank the National Natural Science Foundation of China (No. 81072604/31170967) for financial support.
文摘This study presents an exploration on extending the action of therapeutic proteins by crystallization strategy without new molecular entities generation.Recombinant human interferon a-2b(rhIFN),a model protein drug in this case,was crystallized using a hanging drop vapor diffusion method.A novel chelating technique with metal ions was employed to promote crystals formation.The physico-chemical characterization of the protein crystals,including morphology,particle size,X-ray diffraction,circular dichroism and biological potency evaluations were performed.In addition,the in vitro release behavior of rhIFN from crystal lattice suggested an exciting possibility of protein crystals as a longacting formulation.The work described here demonstrates the possibility of spherical crystals of biomacromolecules for controllable delivery application of therapeutic proteins.
文摘Objective:To explore the effect of metoprolol succinate sustained-release tablets combined with Wenxin Granules in the treatment of coronary heart disease patients with arrhythmia.Methods:The research objects were 50 patients with arrhythmia who were treated in our hospital from September 2019 to September 2020.According to different treatment methods,they were divided into observation group(Wenxin Granule+metoprolol succinate treatment)and control group(metoprolol succinate treatment),25 cases in each group.The curative effects of the two groups were compared.Results:After treatment,there was no significant difference in rnn50,RMSSD,sdnni and SDANN between the two groups(P>0.05).Compared with the control group,the SDNN in the observation group was higher than that in the control group(P<0.05);Before treatment,there was no significant difference in the above indexes between the two groups(P>0.05);The effective rates of the observation group and the control group were 92.00%and 68.00%respectively,and the curative effect of the observation group was higher than that of the control group(P<0.05);There was no significant difference in the incidence of adverse reactions between the two groups(P>0.05).Conclusion:In the treatment of patients with coronary heart disease and arrhythmia,Wenxin Granule Combined with metoprolol succinate sustained-release tablets has significant effect,which can effectively improve the dynamic electrocardiogram indexes of patients,improve the clinical efficacy,and has high safety.
基金supported by the Guangzhou Basic and Applied Basic Research Project(2022)。
文摘Stability of liposomes plays a crucial role in drug delivery,especially in oral aspect.The structural modification of liposomes has been the orientation of efforts to improve their stability and enable the controllability of payload release.This study reported a selenylation strategy to optimize the liposomal structure in an attempt to enhance the nanocarrier’s stability,hence the bioavailability of emodin(EM),an active compound with poor water-solubility.EM-loaded selenized liposomes(EM-Se@LPs)were prepared by thin film dispersion followed by in situ reduction technique.The results showed that EM-Se@LPs were provided with enhancive gastrointestinal stability and exhibited sustained release of drug compared with EM-loaded liposomes(EM-LPs).However,the modified liposomes with Se depositing onto the interior and exterior bilayers did not substantially facilitate absorption of EM.The reinforced structure of liposomes irrelevant to absorption was affirmed to be due to good stability and absorbability of EM itself.Nevertheless,the present work provides an alternative option for stabilization of liposomes instead of conventional methods,which may be promising for oral delivery of physiologically unstable and/or poorly absorbed drugs and systemic drug delivery.
基金Funded by the National Program on Key Basic Research Project (No. 2005CB623905)
文摘Based on diffusion of nerve growth factor（NGF） from degradable material,a novel nerve guidance conduit（NGC） with sustained NGF release was prepared by embedding NGF into a degradable RGD-modified composite which has good cell affinity and biocompatibility.In vitro,the NGF release was quantified using enzyme-linked immunosorbent assay method,and the bioactivity of released NGF was examined by PC-12 cell bioassay.In vivo,the performance of the NGF-containing conduit was examined using rat sciatic nerve defect model.The experimental results show that the NGF release process is prolonged over 30 days,and at least some degree of NGF bioactivity is preserved after the fabrication process.Due to the promoting effect of bioactive released NGF on nerve regeneration,the performance of NGC for nerve repair is improved significantly.The results of this study indicate that the sustained NGF release system is suitable for peripheral nerve repair.
文摘The development and validation of an isocratic high performance liquid chromatographic method is described for the determination of tamsulosin hydrochloride in sustained release tablets. The determination was performed on a Diamonsil BDS C18 column with a mobile phase consisting of a mixture of acetonitrile, methanol and 0 5% phosphoric acid solution (20∶30∶50, V/V/V ) at a flow rate of 1 0 mL/min. UV detection was made at 274 nm. The linear range for tamsulosin hydrochloride was 0 81-8 10 μg/mL. The mean recovery was 99 8% ( S R=0 7%, n =9), and the precision was found to be 0 45% ( n =9). The proposed method can be used for routine analysis of tamsulosin hydrochloride in sustained release tablets.
文摘Summary： To study the bioequivalence of a kind of progesterone sustained release suppository, a randomized cross over study was conducted in 12 rabbits. A single rectal dose of 2.75 mg/kg progesterone sustained released suppository （tested formulation, T） and progesterone suppository （reference formulation, R） was administered; a muhiple dose of 2.75 mg/kg was given up to seven times with an interval of 8 h. Concentrations in serum were determined by a competitive enzyme immunoassay. The main parameters of T were： for single and multiple doses, C was 48.8±11.8 ng/mL and 43.5±9.4 ng/mL. Tmax was 0.5±0.3 h and 0. 4±0.3 h, AUC〈（0-21h） was 362. 4±143 ng·h·mL^-1 and 310.6±70. 3 ng·h·mL^-1 , respectively. The relative bioavailability of T to R were （104.2±13.4） % and （111.4±19. 1） %, respectively. Statistical analysis showed that the two formulations were bioequivalent and T had sustained released feature.
基金Supported by National Natural Science Foundation of China(81560659)Science and Technology Research Project of Jiangxi Provincial Department of Education(GJJ201219,GJJ2200903)+1 种基金National College Students Innovation and Entrepreneurship Training Program(202210412022)Science and Technology Plan of Jiangxi Provincial Health Commission(202211411).
文摘[Objectives] To study the coating process of paeonol sustained release pills by extrusion-spheronization method taking ethyl cellulose as the coating material. [Methods] Paeonol pills were made by Auari AW-95 Full Automatic Pill Making Machine. Coating of paeonol sustained release pills was prepared by Auari Mini Pill Polishing Machine. The prescription and process factors of paeonol sustained release pills coating were investigated by single factor experiment and orthogonal experiment. The release of paeonol sustained release pills was determined according to the cumulative release curve of paeonol. [Results] The prepared paeonol sustained release pills released slowly within 24 h, and the release rate reached 80% in 12 h. [Conclusions] The prepared paeonol sustained release pills basically meet the 24 h sustained release standard, and can be further developed and applied.
