Branched copolymer-stabilised nanoemulsions as new candidate oral drug delivery systems
Branched copolymer-stabilised nanoemulsions as new candidate oral drug delivery systems
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DOI：
10.1039/c8ra01944d
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发表时间：
2018-01-01
期刊：
影响因子：
3.9
通讯作者：
Rannard, Steve P.
中科院分区：
文献类型：
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作者：
Hobson, James J.;Edwards, Stephanie;Rannard, Steve P.
通过口服给药将药物递送至血流可能遭受许多并发症，包括溶解不良、首过代谢和外排转运蛋白如P-糖蛋白的主动干预;作为外排底物的药物可能在许多临床病症中引起相当大的问题。在这里，我们采用了一种支链聚合物稳定的纳米乳液策略，以产生高度稳定的油滴（例如花生油，蓖麻油和大豆油），其中含有不同的溶解抗逆转录病毒药物，用于日常对抗艾滋病毒/艾滋病。虽然观察到依法韦仑通过Caco-2肠上皮模型的渗透差异非常有限，但蛋白酶抑制剂洛匹那韦以乳剂形式应用于上皮单层时的渗透显著高于（约10倍）含水DMSO溶剂中的对照品。所提出的纳米乳液方法可以允许各种药物物质的药物特异性渗透改善。
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.