Arid
DOI10.1007/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
ISSN2190-393X
EISSN2190-3948
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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