Knowledge Resource Center for Ecological Environment in Arid Area
DOI | 10.1007/s13346-013-0186-3 |
Investigation of the transdermal transport of charged local anesthetics in the presence of triterpene saponin glycosides | |
Pino, Christopher J.1; Scherer, Michael A.1; Shastri, V. Prasad1,2,3 | |
通讯作者 | Shastri, V. Prasad |
来源期刊 | DRUG DELIVERY AND TRANSLATIONAL RESEARCH
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ISSN | 2190-393X |
EISSN | 2190-3948 |
出版年 | 2014 |
卷号 | 4期号:2页码:131-138 |
英文摘要 | Percutaneous absorption and transdermal delivery of water-soluble drugs have proven to be challenging due to their low permeability through skin. Avicins which are triterpene saponin glycosides (TSGs) derived from the desert plant Acacia victoriae have not been investigated to date as chemical penetration enhancers due to their higher molecular weight (MW 2,000 Da). It was recently shown that avicins exhibit remarkable mobility across skin lipids in spite of their large size due to their unique chemical structure. In this study, the permeation of local anesthetics, lidocaine-HCl, prilocaine-HCl, and bupivacaine-HCL from aqueous vehicle, across full-thickness porcine skin was investigated in the presence of F094-a mixture of avicins. F094 was capable of enhancing the permeability of all three anesthetics from aqueous formulations at extremely low concentrations ranging from 0.1 to 1 % w/v. The enhancement, which ranged from 2- to 5-fold, was surprisingly independent of molecular weight of the anesthetics and showed clear correlation with aqueous phase solubility of the anesthetics. Since F094 was found to have no impact on the octanol/water partition coefficients of the anesthetics, this suggests that TSGs like avicins most likely impact the aqueous pathways (pericellular/ pores within lipids) and as such represent an alternative means of enhancing the transdermal transport of charged drugs from water-based formulations. |
英文关键词 | Chemical penetration enhancers Avicins Polysaccharide Pericellular Aqueous transport Macromolecules |
类型 | Article |
语种 | 英语 |
国家 | USA ; Germany |
收录类别 | SCI-E |
WOS记录号 | WOS:000357370300004 |
WOS关键词 | ACACIA-VICTORIAE BENTHAM ; INDUCE APOPTOSIS ; AVICINS ; ENHANCEMENT ; PENETRATION ; METABOLISM ; MEMBRANE ; STRESS ; FAMILY ; DRUGS |
WOS类目 | Instruments & Instrumentation ; Medicine, Research & Experimental ; Pharmacology & Pharmacy |
WOS研究方向 | Instruments & Instrumentation ; Research & Experimental Medicine ; Pharmacology & Pharmacy |
资源类型 | 期刊论文 |
条目标识符 | http://119.78.100.177/qdio/handle/2XILL650/181570 |
作者单位 | 1.Vanderbilt Univ, Dept Biomed Engn, Nashville, TN 37235 USA; 2.Univ Freiburg, Inst Macromol Chem, D-79104 Freiburg, Germany; 3.Univ Freiburg, BIOSS Ctr Biol Signalling Studies, D-79104 Freiburg, Germany |
推荐引用方式 GB/T 7714 | Pino, Christopher J.,Scherer, Michael A.,Shastri, V. Prasad. Investigation of the transdermal transport of charged local anesthetics in the presence of triterpene saponin glycosides[J],2014,4(2):131-138. |
APA | Pino, Christopher J.,Scherer, Michael A.,&Shastri, V. Prasad.(2014).Investigation of the transdermal transport of charged local anesthetics in the presence of triterpene saponin glycosides.DRUG DELIVERY AND TRANSLATIONAL RESEARCH,4(2),131-138. |
MLA | Pino, Christopher J.,et al."Investigation of the transdermal transport of charged local anesthetics in the presence of triterpene saponin glycosides".DRUG DELIVERY AND TRANSLATIONAL RESEARCH 4.2(2014):131-138. |
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