Investigation of the transdermal transport of charged local anesthetics in the presence of triterpene saponin glycosides

Drug Delivery and Translational Research
Christopher J PinoV Prasad Shastri

Abstract

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 like...Continue Reading

References

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Dec 14, 2012·Proceedings of the National Academy of Sciences of the United States of America·Christopher J PinoV Prasad Shastri

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