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

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 a...

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Bibliographic Details
Published in:RSC advances 2018-01, Vol.8 (23), p.12984-12991
Main Authors: Hobson, James J, Edwards, Stephanie, Slater, Rebecca. A, Martin, Philip, Owen, Andrew, Rannard, Steve P
Format: Article
Language:English
Subjects:
Acquired immune deficiency syndrome
AIDS
Antiretroviral drugs
Castor oil
Chemistry
Drug delivery systems
Drugs
Efflux
Epithelium
HIV
Human immunodeficiency virus
Metabolism
Nanoemulsions
Peanuts
Penetration
Protease inhibitors
Soybean oil
Soybeans
Substrates
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Summary: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. Branched copolymers offer very efficient nanoemulsion stabilisers with benefits for oral drug delivery.
ISSN:2046-2069
2046-2069
DOI:10.1039/c8ra01944d