Branched copolymer-stabilised nanoemulsions as new candidate oral drug delivery systems

James J. Hobson, Stephanie Edwards, Rebecca. A. Slater, Philip Martin, Andrew Owen, Steve P. Rannard

Index: 10.1039/C8RA01944D

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Abstract

The delivery of drugs to the bloodstream via oral administration may suffer from a number of complications including poor dissolution, first pass metabolism and the active intervention of efflux transporters such as P-glycoproteins; drugs which are efflux substrates may cause considerable problems across many clinical conditions. Here we have employed a branch-polymer stabilised nanoemulsion strategy to create highly robust oil droplets (e.g. peanut oil, castor oil and soybean oil) containing different dissolved antiretroviral drugs used in the daily fight against HIV/AIDS. Although very limited difference in permeation through a Caco-2 gut epithelium model was seen for efavirenz, the permeation of the protease inhibitor lopinavir was considerably higher (approximately 10-fold) when applied to an epithelium monolayer in emulsion form than the control within an aqueous DMSO vehicle. The presented nanoemulsion approach may allow drug-specific permeation improvements for various drug substances.