Objective:To investigate the percutaneous penetration enhancement effect of essential oil from Zanthoxylum bungeanum Maxim.(Z.bungeanum oil)on active components in externally-applied traditional Chinese medicines.Meth...Objective:To investigate the percutaneous penetration enhancement effect of essential oil from Zanthoxylum bungeanum Maxim.(Z.bungeanum oil)on active components in externally-applied traditional Chinese medicines.Methods:Five model drugs,geniposide,puerarin,ferulic acid,tetramethylpyrazine,and osthole,were chosen based on their lipophilicity and tested using in vitro transdermal permeation studies consisting of Franz diffusion cells and full thickness rat abdominal skin.Scanning electron microscopy was employed to observe the morphological changes of rat skin tissue after treatment with Z.bungeanum oil.The molecular interactions between the oil and the polar head groups in stratum corneum(SC)lipids were monitored using molecular dynamic simulation,and the SC/vehicle partition coefficients and saturation solubilities of the selected model drugs treated with and without the oil were also determined to ascertain its mechanisms of action.Results:As oil concentration increased,the log ERflow trended toward a negative linear relationship with the lipophilicity of drugs.After treatment with Z.bungeanum oil,a mild lifting up and wrinkle on the SC surface were observed,and appeared to become more pronounced as oil concentration increased.There was no significant difference between the control and the Z.bungeanum oil at different concentrations in terms of saturation solubility of GP,while saturation solubilities of the 4 other drugs gradually increased as oil concentration increased.The oxygen-containing constituents in Z.bungeanum oil,such as terpinen-4-ol and 1,8-cineole,which accounted for 57.95%of total oil,could form stable hydrogen bonds with the polar head group of ceramide 3.Conclusion:Z.bungeanum oil facilitated transdermal permeation of drugs with different lipophilicity,including the extremely hydrophilic and lipophilic drugs,whereas it exhibited greater enhancement activity for strongly hydrophilic drugs.The mechanisms of transdermal permeation enhancement by the oil could be explained with SC/vehicle partitio展开更多
Objective:To investigate the percutaneous penetration effect of essential oil of mint from Mentha haplocalyx Briq.on the complex active components in Chinese herbal external preparations,and assess its toxicity on the...Objective:To investigate the percutaneous penetration effect of essential oil of mint from Mentha haplocalyx Briq.on the complex active components in Chinese herbal external preparations,and assess its toxicity on the skin cells.Methods:The cytotoxicity of mint oil on HaCaT keratinocytes and CCC-ESF-1 fibroblasts was measured using an MTT assay.Five model drugs with a wide range of lipophilicity,namely osthole,tetramethylpyrazine,ferulic acid,puerarin,and geniposide,were tested using in vitro permeation studies to investigate the percutaneous penetration enhancement effect of mint oil.Secondary structure alterations of skin stratum corneum(SC)were measured using Fourier transform infrared spectroscopy(FTIR).Saturation solubilities and SC/vehicle partition coefficients of the five model drugs with and without mint oil were also determined to understand the potential mechanisms of the essential oil.Results:Half maximal inhibitory concentration(IC50)values of mint oil were significantly higher in HaCaT and CCC-ESF-1 cell lines than values in the well-established and standard penetration enhancer Azone.Conclusions:Mint oil at proper concentration could effectively facilitate percutaneous penetration of both lipophilic and hydrophilic drugs,and exhibit higher efficiency for moderate hydrophilic drugs.Mechanisms of penetration enhancement by mint oil could be explained with saturation solubility,SC/vehicle partition coefficient and the secondary structure change of SC.展开更多
Rheumatoid arthritis is a chronic,systemic autoimmune disease predominantly based on joint lesions with an extremely high disability and deformity rate.Several drugs have been used for the treatment of rheumatoid arth...Rheumatoid arthritis is a chronic,systemic autoimmune disease predominantly based on joint lesions with an extremely high disability and deformity rate.Several drugs have been used for the treatment of rheumatoid arthritis,but their use is limited by suboptimal bioavailability,serious adverse effects,and nonnegligible first-pass effects.In contrast,transdermal drug delivery systems(TDDSs)can avoid these drawbacks and improve patient compliance,making them a promising option for the treatment of rheumatoid arthritis(RA).Of course,TDDSs also face unique challenges,as the physiological barrier of the skin makes drug delivery somewhat limited.To overcome this barrier and maximize drug delivery efficiency,TDDSs have evolved in terms of the principle of transdermal facilitation and transdermal facilitation technology,and different generations of TDDSs have been derived,which have significantly improved transdermal efficiency and even achieved individualized controlled drug delivery.In this review,we summarize the different generations of transdermal drug delivery systems,the corresponding transdermal strategies,and their applications in the treatment of RA.展开更多
The care of obstetrics patients has improved dramatically over the past few decades.Unfortunately,rates of cesarean section remain high,and decreasing this rate requires close care and follow-up in the prenatal outpat...The care of obstetrics patients has improved dramatically over the past few decades.Unfortunately,rates of cesarean section remain high,and decreasing this rate requires close care and follow-up in the prenatal outpatient setting.Counseling regarding cesarean delivery and vaginal delivery is imperative.Opportunities still exist in helping patients objectively weigh the decision for cesarean delivery versus vaginal delivery.Additional developments have occurred in the intrapartum and the postpartum setting,with an aim to improve patient and neonatal outcomes.Changes have been implemented for patients undergoing cesarean delivery including preoperative and intraoperative treatment of pain,nausea,and vomiting,as well as postoperative care bundles that improve patient outcomes.Innovations have also occurred in the care of postpartum patients after vaginal delivery,again with improvements in patient outcomes.This article summarizes the current evidence,provides care recommendations,and identifies the next steps in improving obstetrics care.展开更多
An insulin-loaded emulsion system （IES） was developed as a hypoglycaemic drug for transmucosal delivery. The selected formulation was a stable oil/water emulsion system. The particles in the emulsion system were dis...An insulin-loaded emulsion system （IES） was developed as a hypoglycaemic drug for transmucosal delivery. The selected formulation was a stable oil/water emulsion system. The particles in the emulsion system were distributed evenly, and the particle size ranged from 20 to 260 nm（ average size ： 67.5 nm ）. Soybean lecithin played an important role in the emulsion system due to its abilities of acting as both absorption enhancer for insulin uptake through sublingual mucosa and oily phase for the emulsion system. The laser confocal scanning microscopic（LCSM） study showed that FITC-labelled insulin could penetrate the sublingual mucosa of rabbits, and the phase diagrams of the emulsion system suggested that soybean lecithin could take the place of oily phase to construct a stable emulsion system even if the traditional oil was absent. The applications of soybean lecithin as pharmaceutical biomaterial were extended for the further usage by present studies.展开更多
基金National Natural Science Foundation of China(No.81473365)Postgraduate Project of Beijing University of Chinese Medicine(No.2016-JYB-XS095)The authors also thank the Innovative Research Team of Beijing University of Chinese Medicine(No.2011-CXTD-13)for its financial support.
文摘Objective:To investigate the percutaneous penetration enhancement effect of essential oil from Zanthoxylum bungeanum Maxim.(Z.bungeanum oil)on active components in externally-applied traditional Chinese medicines.Methods:Five model drugs,geniposide,puerarin,ferulic acid,tetramethylpyrazine,and osthole,were chosen based on their lipophilicity and tested using in vitro transdermal permeation studies consisting of Franz diffusion cells and full thickness rat abdominal skin.Scanning electron microscopy was employed to observe the morphological changes of rat skin tissue after treatment with Z.bungeanum oil.The molecular interactions between the oil and the polar head groups in stratum corneum(SC)lipids were monitored using molecular dynamic simulation,and the SC/vehicle partition coefficients and saturation solubilities of the selected model drugs treated with and without the oil were also determined to ascertain its mechanisms of action.Results:As oil concentration increased,the log ERflow trended toward a negative linear relationship with the lipophilicity of drugs.After treatment with Z.bungeanum oil,a mild lifting up and wrinkle on the SC surface were observed,and appeared to become more pronounced as oil concentration increased.There was no significant difference between the control and the Z.bungeanum oil at different concentrations in terms of saturation solubility of GP,while saturation solubilities of the 4 other drugs gradually increased as oil concentration increased.The oxygen-containing constituents in Z.bungeanum oil,such as terpinen-4-ol and 1,8-cineole,which accounted for 57.95%of total oil,could form stable hydrogen bonds with the polar head group of ceramide 3.Conclusion:Z.bungeanum oil facilitated transdermal permeation of drugs with different lipophilicity,including the extremely hydrophilic and lipophilic drugs,whereas it exhibited greater enhancement activity for strongly hydrophilic drugs.The mechanisms of transdermal permeation enhancement by the oil could be explained with SC/vehicle partitio
基金the National Natural Science Foundation of China(No.81473365)the Innovative Research Team in Beijing University of Chinese Medicine(No.2011-CXTD-13).
文摘Objective:To investigate the percutaneous penetration effect of essential oil of mint from Mentha haplocalyx Briq.on the complex active components in Chinese herbal external preparations,and assess its toxicity on the skin cells.Methods:The cytotoxicity of mint oil on HaCaT keratinocytes and CCC-ESF-1 fibroblasts was measured using an MTT assay.Five model drugs with a wide range of lipophilicity,namely osthole,tetramethylpyrazine,ferulic acid,puerarin,and geniposide,were tested using in vitro permeation studies to investigate the percutaneous penetration enhancement effect of mint oil.Secondary structure alterations of skin stratum corneum(SC)were measured using Fourier transform infrared spectroscopy(FTIR).Saturation solubilities and SC/vehicle partition coefficients of the five model drugs with and without mint oil were also determined to understand the potential mechanisms of the essential oil.Results:Half maximal inhibitory concentration(IC50)values of mint oil were significantly higher in HaCaT and CCC-ESF-1 cell lines than values in the well-established and standard penetration enhancer Azone.Conclusions:Mint oil at proper concentration could effectively facilitate percutaneous penetration of both lipophilic and hydrophilic drugs,and exhibit higher efficiency for moderate hydrophilic drugs.Mechanisms of penetration enhancement by mint oil could be explained with saturation solubility,SC/vehicle partition coefficient and the secondary structure change of SC.
基金supported by the Scientific Research Project of Liaoning Province Education Department (2020LJC16),China。
文摘Rheumatoid arthritis is a chronic,systemic autoimmune disease predominantly based on joint lesions with an extremely high disability and deformity rate.Several drugs have been used for the treatment of rheumatoid arthritis,but their use is limited by suboptimal bioavailability,serious adverse effects,and nonnegligible first-pass effects.In contrast,transdermal drug delivery systems(TDDSs)can avoid these drawbacks and improve patient compliance,making them a promising option for the treatment of rheumatoid arthritis(RA).Of course,TDDSs also face unique challenges,as the physiological barrier of the skin makes drug delivery somewhat limited.To overcome this barrier and maximize drug delivery efficiency,TDDSs have evolved in terms of the principle of transdermal facilitation and transdermal facilitation technology,and different generations of TDDSs have been derived,which have significantly improved transdermal efficiency and even achieved individualized controlled drug delivery.In this review,we summarize the different generations of transdermal drug delivery systems,the corresponding transdermal strategies,and their applications in the treatment of RA.
文摘The care of obstetrics patients has improved dramatically over the past few decades.Unfortunately,rates of cesarean section remain high,and decreasing this rate requires close care and follow-up in the prenatal outpatient setting.Counseling regarding cesarean delivery and vaginal delivery is imperative.Opportunities still exist in helping patients objectively weigh the decision for cesarean delivery versus vaginal delivery.Additional developments have occurred in the intrapartum and the postpartum setting,with an aim to improve patient and neonatal outcomes.Changes have been implemented for patients undergoing cesarean delivery including preoperative and intraoperative treatment of pain,nausea,and vomiting,as well as postoperative care bundles that improve patient outcomes.Innovations have also occurred in the care of postpartum patients after vaginal delivery,again with improvements in patient outcomes.This article summarizes the current evidence,provides care recommendations,and identifies the next steps in improving obstetrics care.
文摘An insulin-loaded emulsion system （IES） was developed as a hypoglycaemic drug for transmucosal delivery. The selected formulation was a stable oil/water emulsion system. The particles in the emulsion system were distributed evenly, and the particle size ranged from 20 to 260 nm（ average size ： 67.5 nm ）. Soybean lecithin played an important role in the emulsion system due to its abilities of acting as both absorption enhancer for insulin uptake through sublingual mucosa and oily phase for the emulsion system. The laser confocal scanning microscopic（LCSM） study showed that FITC-labelled insulin could penetrate the sublingual mucosa of rabbits, and the phase diagrams of the emulsion system suggested that soybean lecithin could take the place of oily phase to construct a stable emulsion system even if the traditional oil was absent. The applications of soybean lecithin as pharmaceutical biomaterial were extended for the further usage by present studies.
基金This work is supported by National Science Foundation under the contract ECCS-1303134,National Institutes of Health under the contract R21 NS084148-01A1,the National Science Foundation of Beijing (No.7161014),Key Science and Technology Project of Zhejiang Provincial Health Department (No.WKJ2013-2-022) and National Natural Science Foundation of China (No.81371396).
