This study aimed to establish a highly accurate method for quantifying methotrexate(MTX)concentrations in serum using an ultra-high performance liquid chromatography-tandem mass spectrometry system(UPLC-MS/MS)and to c...This study aimed to establish a highly accurate method for quantifying methotrexate(MTX)concentrations in serum using an ultra-high performance liquid chromatography-tandem mass spectrometry system(UPLC-MS/MS)and to compare its performance with the chemiluminescence microparticle immunoassay(CMIA).A total of 211 serum samples from pediatric patients with intracranial tumors undergoing high-dose MTX treatment were analyzed using both techniques.Correlation and agreement analyses were performed to assess the level of concordance between these methods.The results demonstrated a significant correlation(P<0.05)between the two methods,with correlation coefficients of 0.9913 and 0.9893,respectively.However,a statistical difference was noted in MTX serum concentrations at lower levels(0.04-1.5μmol/L),while no significant difference was observed at higher concentrations(1.5-400μmol/L).Specifically,in the 0.04-1.5μmol/L range(107 cases),Bland-Altman analysis indicated a bias of 0.018 between the two methods.Given the observed discrepancies,particularly at lower concentrations,it is advised that the UPLC-MS/MS method should not be used interchangeably with the CMIA assay for therapeutic drug monitoring in patients receiving high-dose MTX treatment.展开更多
Recently there has been a wide concern on inorganic nanoparticles as drug delivery carriers. CaCO3 particles have shown promising potential for the development of carriers for drugs, but little research had been perfo...Recently there has been a wide concern on inorganic nanoparticles as drug delivery carriers. CaCO3 particles have shown promising potential for the development of carriers for drugs, but little research had been performed regarding their safe dosage for maximizing the therapeutic activity without harming biosystems. In this study, we assessed the biological safety of porous spherical CaCO3 microparticles on Hela cells. The reactive oxygen species (ROS), glutathione (GSH), carbonyl content in proteins (CCP), DNA-protein crosslinks (DPC) and cell viability were measured. Results showed that with the exposure concentration increase, ROS and CCP in Hela cells presented a significant increase but GSH contents in Hela cells and cell viability showed a significant decrease respectively compared with the control. DPC coefficient ascended, but no statistically significant changes were observed. The results indicated that porous spherical CaCO3 microparticles may induce oxidative damage to Hela cells. But compared with other nanomaterials, porous spherical CaCO3 appeared to have good biocompatibility. The results implied that porous spherical calcium carbonate microparticles could be applied as relatively safe drug vehicles, but with the caveat that the effect of high dosages should not be ignored when attempting to maximize therapeutic activity by increasing the concentration.展开更多
AIM To evaluate platelet activation markers in psoriasis patients, compared to controls, and investigate their association with the inflammatory burden of psoriasis.METHODS Forty psoriatic patients without cardiovascu...AIM To evaluate platelet activation markers in psoriasis patients, compared to controls, and investigate their association with the inflammatory burden of psoriasis.METHODS Forty psoriatic patients without cardiovascular disease,and 12 healthy controls were subjected to measurement of baseline platelet CD62 P, CD63 and CD42 b expression, platelet-leukocyte complexes, i.e., platelet-monocyte complexes(PMC), platelet-neutrophil complexes(PNC) and platelet-lymphocyte complexes, and concentrations of platelet-derived microparticles(PMPs) using flow cytometry. Both larger-size(0.5-0.9 μm) and smallersize(< 0.5 μm) PMPs were determined. Serum interleukin(IL)-12 and IL-17 levels were also measured by enzyme-linked immunosorbent assay. The severity of psoriasis was evaluated by the Psoriasis Area Severity Index(PASI).RESULTS PMP concentrations were significantly higher in psoriasis patients than controls [mean±standard error of mean(SEM): 22±5/μL vs 11±6/μL; P=0.018), for both smaller-size(10±2/μL vs 4±2/μL; P=0.033) and larger-size(12±3/μL vs 6±4/μL; P=0.014) PMPs. Platelet CD62 P, CD63 and CD42 b expression and circulating PMC and PNC were similar between the two groups. Lower circulating PLC were observed in psoriasis patients compared to controls(mean±SEM: 16%±3% vs 23%±6%; P=0.047). Larger-size PMPs were related with IL-12 levels(P<0.001) and smaller-size PMPs with both IL-12 and IL-17 levels(P<0.001). Total PMPs also correlated with IL-12(P<0.001). CD63 expression was positively correlated with both IL-12 and IL-17(P<0.05). Increased PASI score was associated with increased levels of larger-size PMPs(r=0.45; P=0.011) and increased CD63 expression(r=0.47; P<0.01).CONCLUSION PMPs, known to be predictive of cardiovascular outcomes, are increased in psoriasis patients, and associated with high inflammatory disease burden. Enhanced platelet activation may be the missing link leading to cardiovascular events in psoriatic patients.展开更多
In current work,Ni-Ti-CeO_(2) nanocomposite coatings were achieved by co-adding Ti microparticles and CeO_(2) nanoparticles.Designed experiments and COMSOL computer simulation were applied to reveal the synergistic ro...In current work,Ni-Ti-CeO_(2) nanocomposite coatings were achieved by co-adding Ti microparticles and CeO_(2) nanoparticles.Designed experiments and COMSOL computer simulation were applied to reveal the synergistic role of Ti microparticles and CeO_(2) nanoparticles in tailoring the spatial microstructures and properties of Ni-Ti-CeO_(2) nanocomposite coating.Unilaterally,the conductive Ti microparticles conducted the growth behavior of Ni grains by current density concentration,distorting electronic feld lines and heterogeneous nucleation.Individual domains consisting of inner nanograins and outer radial columnar grains surrounded Ti microparticles,where Ti microparticles acted as seeds.Ti microparticles tended to be aggregated,leading to spatial heterogeneity of microstructures.Ni deposits buried the Ti microparticles in forms of“covering model”,contributing to the formation of inside voids and rough surface and aggregation of Ti microparticles;on the other hand,the non-conductive CeO_(2)microparticles hardly changed the distribution of current density and electronic feld lines on the cathode surface.Ni deposits buried the CeO_(2)microparticle in forms of“stacking model”,avoiding the inside voids and aggregation of particles.The incorporation of CeO_(2)microparticle brought in microstructure evolutions only on its top side without disturbing the growth behavior of Ni grains on its lateral side or bottom,suggesting the limited effects.This was correlated with the presence of current concentration above the CeO_(2) microparticle at the last stage of burying CeO_(2) microparticle.The co-addition of Ti microparticles and CeO_(2) nanoparticles into Ni deposits exploited the complementary action of the two particles,which gave birth to satisfed spatial microstructures and improved hardness.Ti microparticles took major responsibility for microstructure evolutions,while the CeO_(2) nanoparticles were mainly in charge of the microstructure homogeneity.展开更多
Mesoporous TiO_2-B/anatase microparticles have been in-situ synthesized from K_2Ti_2O_5 without template.The TiO_2-B phase around the particle surface accelerates the diffusion of charges through the interface,while t...Mesoporous TiO_2-B/anatase microparticles have been in-situ synthesized from K_2Ti_2O_5 without template.The TiO_2-B phase around the particle surface accelerates the diffusion of charges through the interface,while the anatase phase in the core maintains the capacity stability.The heterojunction interface between the main polymorph of anatase and the trace of TiO_2-B exhibits promising lithium ion battery performance.This trace of 5%(by mass) TiO_2-B determined by Raman spectra brings the first discharge capacity of this material to 247 mA · h ·g^(-1),giving 20%improvement compared to the anatase counterpart Stability testing at 1 C reveals that the capacity maintains at 171 mA·h·^(-1),which is better than 162 mA·h·g^(-1) for single phase anatase or 159 mA·h·g^(-1) for TiO_2-B.The mesoporous TiO_2-B/anatase rnicroparticles also show superior rate performance with 100 mA·h·g^(-1) at 40 C,increased by nearly 25%as compared to pure anatase.This opens a possibility of a general design route,which can be applied to other metal oxide electrode materials for rechargeable batteries and supercapacitors.展开更多
The mechanical behavior of chonta palm wood(Bactris gasipaes) microparticles reinforced high density polyethylene(HDPE) under high strain-rate compressive and ballistic impact loading were investigated.The palm wood m...The mechanical behavior of chonta palm wood(Bactris gasipaes) microparticles reinforced high density polyethylene(HDPE) under high strain-rate compressive and ballistic impact loading were investigated.The palm wood microparticles were introduced into the HDPE via an extrusion process using parallel twin screw extruder to produce biocomposite containing 10, 20, 25, and 30 wt % chonta wood microparticles. In addition to mechanical tests, fractographic analysis was done to understand the failure mechanism in the biocomposites under dynamic and ballistic impact loads. The results indicate that both quasi-static and dynamic mechanical properties of HDPE are enhanced by reinforcement with chonta palm wood particles. The biocomposites containing 25 wt % wood microparticles exhibited the highest strength, stiffness, ballistic impact resistance and impact energy absorption capability. Introduction of microparticles of chonta palm wood as reinforcement into a polymeric matrix such as HDPE is therefore a promising method to develop biocomposites with enhanced capacity to withstand dynamic impact loading and absorb impact energy.展开更多
With hydrophilic surface and high surface area, porous silica has been applied to load insoluble drugs. Compared to solvent equilibrium method, resveratrol(RES)–mesoporous silica microparticles(MSM) solid dispersion ...With hydrophilic surface and high surface area, porous silica has been applied to load insoluble drugs. Compared to solvent equilibrium method, resveratrol(RES)–mesoporous silica microparticles(MSM) solid dispersion prepared by fluid bed demonstrated higher drug loading and more complete dissolution. Pore volume and diameter have more remarkable effects than surface area to the drug loading and in vitro dissolution profiles. RES–polyethylene glycol solid dispersion with high drug loading showed fast but incomplete dissolution due to the recrystallization. The combination of fluid bed and MSM was an effective strategy to improve drug loading as well as dissolution for poorly water-soluble drugs.展开更多
In the previous study, chitosan-succinyl-prednisolone conjugate microparticles (MP) were found to exhibit good efficacy and reduced toxicity nearly as well as their Eudragit L-coated microparticles (MP/EuL). This prop...In the previous study, chitosan-succinyl-prednisolone conjugate microparticles (MP) were found to exhibit good efficacy and reduced toxicity nearly as well as their Eudragit L-coated microparticles (MP/EuL). This proposes a question whether enteric-coating of MP is necessary or not. Although MP/EuL were already examined for their pharmacokinetic and gastrointestinal behaviors, MP have not been done yet. Therefore, in this study, MP were evaluated by investigating pharmacokinetic features in detail. MP with the in vitro features equivalent to those of the previous conjugate microparticles could be produced more readily in the modified preparative method. Pharmacokinetic and gastrointestinal behaviors of MP were investigated by intragastric dosing (5 mg PD eq./kg) to rats with 2,4,6-trinitrobenzenesulfonic acid-induced ulcerative colitis. The plasma concentration was suppressed extensively in MP as well as MP/EuL, supporting the reduction of PD systemic toxic side effects. However, the plasma level increased gradually up to 7 h in MP, but not in MP/EuL. At 8 h after dosing, MP were detected in the stomach to a fair extent, and free PD was found there, indicating that MP were subjected to trapping in the stomach probably due to positive charge of chitosan molecules. For MP, such prolonged localization and slow release of PD in the stomach were probably associated with the gradual increase in plasma concentration. Therefore, MP/EuL were evaluated to be superior to MP for effective targeting to ulcerative colitis. It is concluded that enteric-coating is very important for the targeting system using MP.展开更多
The objectives of the work were to develop a lipid based delivery system for aspirin and to evaluate its physicochemical and pharmacodynamic properties.Aspirin-loaded solid lipid microparticles(SLMs)were formulated by...The objectives of the work were to develop a lipid based delivery system for aspirin and to evaluate its physicochemical and pharmacodynamic properties.Aspirin-loaded solid lipid microparticles(SLMs)were formulated by hot homogenization and analysed for their encapsulation efficiency(EE%),in vitro release,particle size,anti-inflammatory and ulcer inhibition properties.Particle size ranged from 33.10±5.85 to 43.50±7.27μm for batches A1 to A3 SLMs loaded with 1,3 and 5%aspirin and containing Poloxamer 407,while batches B1,B2 and B3 formulated with Soluplus as surfactant had particle size range of 31.10±1.46 to 45.60±2.92μm.Batches A1 and B1 containing 1%of aspirin had the highest EE of 70 and 72%respectively.Maximum in vitro release of 95.1 and 93.2%were obtained at 8 h from batches A1 and B1 respectively.SLMs exhibited about 77.8%oedema inhibition,while the reference had 66.7%and ulcer inhibition range of 25-75%.Aspirin-loaded SLMs exhibited good properties and could be used orally twice daily for the treatment of inflammation.展开更多
Hollow calcium silicate microparticles were prepared by mixing a water-in-oil (W/O) emulsion containing silicate ions in aqueous phase with an oil phase containing a calcium/di-2-ethylhexyl phosphoric acid (D2EHPA) co...Hollow calcium silicate microparticles were prepared by mixing a water-in-oil (W/O) emulsion containing silicate ions in aqueous phase with an oil phase containing a calcium/di-2-ethylhexyl phosphoric acid (D2EHPA) complex. The inorganic precipitation reaction at the oil-water interface was accelerated by using a simple W/O emulsion. Hollow microparticles were obtained when the mole ratio of D2EHPA and calcium in the oil phase was nearly 2:1. The shell formation of the par-ticles depended on the acceleration of the precipitation reaction, which could be accomplished by controlling the concentrations of the calcium and silicate ions.展开更多
Objective: Hemp seed oil is perfect for most skin types;it moisturizes skin and protects it from inflammation, oxidation, and other causes of aging. The problem is that the Hemp oil-based products do not penetrate the...Objective: Hemp seed oil is perfect for most skin types;it moisturizes skin and protects it from inflammation, oxidation, and other causes of aging. The problem is that the Hemp oil-based products do not penetrate the skin;they remain on the skin’s surface. Recently researchers have been trying to prepare nano emulsions of hemp oil to facilitate its permeation to deep skin layers. In all techniques used today, surfactants are added to the emulsification process. These surfactants may cause unwanted skin side effects. In the present study, we prepare micronized Hemp (m-Hemp) without using any surfactants in the micronization process, thus avoiding the side effects associated with surfactant addition. Methods & Results: Particles size of m-Hemp was evaluated using electron microscopy. Various sizes of m-Hemp were found, the smallest being 100 nm in diameter. The antioxidation properties of m-Hemp were measured using the Electron Spin Resonance (ESR) technique and were found to be enhanced. Skin topography and morphology following a cream containing m-Hemp treatment were visualized by Optical Profilometry and ESEM respectively. The results show a marked improvement in skin topography in all measured parameters. In addition, human keratinocytes (HaCaT) were exposed to inflammatory conditions and were then treated using Hemp. As a result, one of the key inflammatory factors (IL-2) was significantly reduced after treatment with m-Hemp (p ≤ 0.0001). The skin penetration of the cream containing m-Hemp was tested on human skin using the IMOPE (Iterative Multi-plane Optical Property Extraction) system. The results indicate that m-Hemp penetrates both the stratum corneum and the deep epidermal layers towards the dermis. Conclusion: The new cream prepared with micronized Hemp shows significant anti-inflammatory and antioxidative effects and demonstrates the entrance of m-Hemp to the skin epidermal layer.展开更多
基金The Science and Technology Fund of Beijing Shijitan Hospital(Grant No.2022-C06)the National Key Research and Development Program of China(Grant No.2020YFF01014606).
文摘This study aimed to establish a highly accurate method for quantifying methotrexate(MTX)concentrations in serum using an ultra-high performance liquid chromatography-tandem mass spectrometry system(UPLC-MS/MS)and to compare its performance with the chemiluminescence microparticle immunoassay(CMIA).A total of 211 serum samples from pediatric patients with intracranial tumors undergoing high-dose MTX treatment were analyzed using both techniques.Correlation and agreement analyses were performed to assess the level of concordance between these methods.The results demonstrated a significant correlation(P<0.05)between the two methods,with correlation coefficients of 0.9913 and 0.9893,respectively.However,a statistical difference was noted in MTX serum concentrations at lower levels(0.04-1.5μmol/L),while no significant difference was observed at higher concentrations(1.5-400μmol/L).Specifically,in the 0.04-1.5μmol/L range(107 cases),Bland-Altman analysis indicated a bias of 0.018 between the two methods.Given the observed discrepancies,particularly at lower concentrations,it is advised that the UPLC-MS/MS method should not be used interchangeably with the CMIA assay for therapeutic drug monitoring in patients receiving high-dose MTX treatment.
文摘Recently there has been a wide concern on inorganic nanoparticles as drug delivery carriers. CaCO3 particles have shown promising potential for the development of carriers for drugs, but little research had been performed regarding their safe dosage for maximizing the therapeutic activity without harming biosystems. In this study, we assessed the biological safety of porous spherical CaCO3 microparticles on Hela cells. The reactive oxygen species (ROS), glutathione (GSH), carbonyl content in proteins (CCP), DNA-protein crosslinks (DPC) and cell viability were measured. Results showed that with the exposure concentration increase, ROS and CCP in Hela cells presented a significant increase but GSH contents in Hela cells and cell viability showed a significant decrease respectively compared with the control. DPC coefficient ascended, but no statistically significant changes were observed. The results indicated that porous spherical CaCO3 microparticles may induce oxidative damage to Hela cells. But compared with other nanomaterials, porous spherical CaCO3 appeared to have good biocompatibility. The results implied that porous spherical calcium carbonate microparticles could be applied as relatively safe drug vehicles, but with the caveat that the effect of high dosages should not be ignored when attempting to maximize therapeutic activity by increasing the concentration.
文摘AIM To evaluate platelet activation markers in psoriasis patients, compared to controls, and investigate their association with the inflammatory burden of psoriasis.METHODS Forty psoriatic patients without cardiovascular disease,and 12 healthy controls were subjected to measurement of baseline platelet CD62 P, CD63 and CD42 b expression, platelet-leukocyte complexes, i.e., platelet-monocyte complexes(PMC), platelet-neutrophil complexes(PNC) and platelet-lymphocyte complexes, and concentrations of platelet-derived microparticles(PMPs) using flow cytometry. Both larger-size(0.5-0.9 μm) and smallersize(< 0.5 μm) PMPs were determined. Serum interleukin(IL)-12 and IL-17 levels were also measured by enzyme-linked immunosorbent assay. The severity of psoriasis was evaluated by the Psoriasis Area Severity Index(PASI).RESULTS PMP concentrations were significantly higher in psoriasis patients than controls [mean±standard error of mean(SEM): 22±5/μL vs 11±6/μL; P=0.018), for both smaller-size(10±2/μL vs 4±2/μL; P=0.033) and larger-size(12±3/μL vs 6±4/μL; P=0.014) PMPs. Platelet CD62 P, CD63 and CD42 b expression and circulating PMC and PNC were similar between the two groups. Lower circulating PLC were observed in psoriasis patients compared to controls(mean±SEM: 16%±3% vs 23%±6%; P=0.047). Larger-size PMPs were related with IL-12 levels(P<0.001) and smaller-size PMPs with both IL-12 and IL-17 levels(P<0.001). Total PMPs also correlated with IL-12(P<0.001). CD63 expression was positively correlated with both IL-12 and IL-17(P<0.05). Increased PASI score was associated with increased levels of larger-size PMPs(r=0.45; P=0.011) and increased CD63 expression(r=0.47; P<0.01).CONCLUSION PMPs, known to be predictive of cardiovascular outcomes, are increased in psoriasis patients, and associated with high inflammatory disease burden. Enhanced platelet activation may be the missing link leading to cardiovascular events in psoriatic patients.
文摘In current work,Ni-Ti-CeO_(2) nanocomposite coatings were achieved by co-adding Ti microparticles and CeO_(2) nanoparticles.Designed experiments and COMSOL computer simulation were applied to reveal the synergistic role of Ti microparticles and CeO_(2) nanoparticles in tailoring the spatial microstructures and properties of Ni-Ti-CeO_(2) nanocomposite coating.Unilaterally,the conductive Ti microparticles conducted the growth behavior of Ni grains by current density concentration,distorting electronic feld lines and heterogeneous nucleation.Individual domains consisting of inner nanograins and outer radial columnar grains surrounded Ti microparticles,where Ti microparticles acted as seeds.Ti microparticles tended to be aggregated,leading to spatial heterogeneity of microstructures.Ni deposits buried the Ti microparticles in forms of“covering model”,contributing to the formation of inside voids and rough surface and aggregation of Ti microparticles;on the other hand,the non-conductive CeO_(2)microparticles hardly changed the distribution of current density and electronic feld lines on the cathode surface.Ni deposits buried the CeO_(2)microparticle in forms of“stacking model”,avoiding the inside voids and aggregation of particles.The incorporation of CeO_(2)microparticle brought in microstructure evolutions only on its top side without disturbing the growth behavior of Ni grains on its lateral side or bottom,suggesting the limited effects.This was correlated with the presence of current concentration above the CeO_(2) microparticle at the last stage of burying CeO_(2) microparticle.The co-addition of Ti microparticles and CeO_(2) nanoparticles into Ni deposits exploited the complementary action of the two particles,which gave birth to satisfed spatial microstructures and improved hardness.Ti microparticles took major responsibility for microstructure evolutions,while the CeO_(2) nanoparticles were mainly in charge of the microstructure homogeneity.
基金Supported by the Program for Changjiang Scholars and Innovative Research Team in University(PCSIRT 0732)the National Natural Science Foundation of China(21136004,20736002,21176113,20876073)+2 种基金NSFC-RGC(20731160614)China Postdoctoral Science Foundation(20110491407)the National Basic Research Program of China(2009CB623407,2009CB219902 and 2009CB226103)
文摘Mesoporous TiO_2-B/anatase microparticles have been in-situ synthesized from K_2Ti_2O_5 without template.The TiO_2-B phase around the particle surface accelerates the diffusion of charges through the interface,while the anatase phase in the core maintains the capacity stability.The heterojunction interface between the main polymorph of anatase and the trace of TiO_2-B exhibits promising lithium ion battery performance.This trace of 5%(by mass) TiO_2-B determined by Raman spectra brings the first discharge capacity of this material to 247 mA · h ·g^(-1),giving 20%improvement compared to the anatase counterpart Stability testing at 1 C reveals that the capacity maintains at 171 mA·h·^(-1),which is better than 162 mA·h·g^(-1) for single phase anatase or 159 mA·h·g^(-1) for TiO_2-B.The mesoporous TiO_2-B/anatase rnicroparticles also show superior rate performance with 100 mA·h·g^(-1) at 40 C,increased by nearly 25%as compared to pure anatase.This opens a possibility of a general design route,which can be applied to other metal oxide electrode materials for rechargeable batteries and supercapacitors.
基金the financial supports of the Natural Sciences and Engineering Research Council of Canada (NSERC)The financial support of the National Secretary of Science and Technology of the Ecuador (SENESCYT) and Ecuadorian Army
文摘The mechanical behavior of chonta palm wood(Bactris gasipaes) microparticles reinforced high density polyethylene(HDPE) under high strain-rate compressive and ballistic impact loading were investigated.The palm wood microparticles were introduced into the HDPE via an extrusion process using parallel twin screw extruder to produce biocomposite containing 10, 20, 25, and 30 wt % chonta wood microparticles. In addition to mechanical tests, fractographic analysis was done to understand the failure mechanism in the biocomposites under dynamic and ballistic impact loads. The results indicate that both quasi-static and dynamic mechanical properties of HDPE are enhanced by reinforcement with chonta palm wood particles. The biocomposites containing 25 wt % wood microparticles exhibited the highest strength, stiffness, ballistic impact resistance and impact energy absorption capability. Introduction of microparticles of chonta palm wood as reinforcement into a polymeric matrix such as HDPE is therefore a promising method to develop biocomposites with enhanced capacity to withstand dynamic impact loading and absorb impact energy.
文摘With hydrophilic surface and high surface area, porous silica has been applied to load insoluble drugs. Compared to solvent equilibrium method, resveratrol(RES)–mesoporous silica microparticles(MSM) solid dispersion prepared by fluid bed demonstrated higher drug loading and more complete dissolution. Pore volume and diameter have more remarkable effects than surface area to the drug loading and in vitro dissolution profiles. RES–polyethylene glycol solid dispersion with high drug loading showed fast but incomplete dissolution due to the recrystallization. The combination of fluid bed and MSM was an effective strategy to improve drug loading as well as dissolution for poorly water-soluble drugs.
文摘In the previous study, chitosan-succinyl-prednisolone conjugate microparticles (MP) were found to exhibit good efficacy and reduced toxicity nearly as well as their Eudragit L-coated microparticles (MP/EuL). This proposes a question whether enteric-coating of MP is necessary or not. Although MP/EuL were already examined for their pharmacokinetic and gastrointestinal behaviors, MP have not been done yet. Therefore, in this study, MP were evaluated by investigating pharmacokinetic features in detail. MP with the in vitro features equivalent to those of the previous conjugate microparticles could be produced more readily in the modified preparative method. Pharmacokinetic and gastrointestinal behaviors of MP were investigated by intragastric dosing (5 mg PD eq./kg) to rats with 2,4,6-trinitrobenzenesulfonic acid-induced ulcerative colitis. The plasma concentration was suppressed extensively in MP as well as MP/EuL, supporting the reduction of PD systemic toxic side effects. However, the plasma level increased gradually up to 7 h in MP, but not in MP/EuL. At 8 h after dosing, MP were detected in the stomach to a fair extent, and free PD was found there, indicating that MP were subjected to trapping in the stomach probably due to positive charge of chitosan molecules. For MP, such prolonged localization and slow release of PD in the stomach were probably associated with the gradual increase in plasma concentration. Therefore, MP/EuL were evaluated to be superior to MP for effective targeting to ulcerative colitis. It is concluded that enteric-coating is very important for the targeting system using MP.
文摘The objectives of the work were to develop a lipid based delivery system for aspirin and to evaluate its physicochemical and pharmacodynamic properties.Aspirin-loaded solid lipid microparticles(SLMs)were formulated by hot homogenization and analysed for their encapsulation efficiency(EE%),in vitro release,particle size,anti-inflammatory and ulcer inhibition properties.Particle size ranged from 33.10±5.85 to 43.50±7.27μm for batches A1 to A3 SLMs loaded with 1,3 and 5%aspirin and containing Poloxamer 407,while batches B1,B2 and B3 formulated with Soluplus as surfactant had particle size range of 31.10±1.46 to 45.60±2.92μm.Batches A1 and B1 containing 1%of aspirin had the highest EE of 70 and 72%respectively.Maximum in vitro release of 95.1 and 93.2%were obtained at 8 h from batches A1 and B1 respectively.SLMs exhibited about 77.8%oedema inhibition,while the reference had 66.7%and ulcer inhibition range of 25-75%.Aspirin-loaded SLMs exhibited good properties and could be used orally twice daily for the treatment of inflammation.
文摘Hollow calcium silicate microparticles were prepared by mixing a water-in-oil (W/O) emulsion containing silicate ions in aqueous phase with an oil phase containing a calcium/di-2-ethylhexyl phosphoric acid (D2EHPA) complex. The inorganic precipitation reaction at the oil-water interface was accelerated by using a simple W/O emulsion. Hollow microparticles were obtained when the mole ratio of D2EHPA and calcium in the oil phase was nearly 2:1. The shell formation of the par-ticles depended on the acceleration of the precipitation reaction, which could be accomplished by controlling the concentrations of the calcium and silicate ions.
文摘Objective: Hemp seed oil is perfect for most skin types;it moisturizes skin and protects it from inflammation, oxidation, and other causes of aging. The problem is that the Hemp oil-based products do not penetrate the skin;they remain on the skin’s surface. Recently researchers have been trying to prepare nano emulsions of hemp oil to facilitate its permeation to deep skin layers. In all techniques used today, surfactants are added to the emulsification process. These surfactants may cause unwanted skin side effects. In the present study, we prepare micronized Hemp (m-Hemp) without using any surfactants in the micronization process, thus avoiding the side effects associated with surfactant addition. Methods & Results: Particles size of m-Hemp was evaluated using electron microscopy. Various sizes of m-Hemp were found, the smallest being 100 nm in diameter. The antioxidation properties of m-Hemp were measured using the Electron Spin Resonance (ESR) technique and were found to be enhanced. Skin topography and morphology following a cream containing m-Hemp treatment were visualized by Optical Profilometry and ESEM respectively. The results show a marked improvement in skin topography in all measured parameters. In addition, human keratinocytes (HaCaT) were exposed to inflammatory conditions and were then treated using Hemp. As a result, one of the key inflammatory factors (IL-2) was significantly reduced after treatment with m-Hemp (p ≤ 0.0001). The skin penetration of the cream containing m-Hemp was tested on human skin using the IMOPE (Iterative Multi-plane Optical Property Extraction) system. The results indicate that m-Hemp penetrates both the stratum corneum and the deep epidermal layers towards the dermis. Conclusion: The new cream prepared with micronized Hemp shows significant anti-inflammatory and antioxidative effects and demonstrates the entrance of m-Hemp to the skin epidermal layer.
