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

机译：支链共聚物稳定的纳米乳液作为新候选口服药物递送系统

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摘要

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.
机译：通过口服给药将药物递送到血液中可能患有许多并发症，包括差的溶解，首次通过代谢和流出转运蛋白如p-糖蛋白的活性干预;在许多临床条件下可能引起相当大的问题。在这里，我们使用了分支聚合物稳定的纳米乳液策略，以产生含有不同溶解的抗逆转录病毒药物的高稳健的油滴（例如花生油，蓖麻油和大豆油），用于每日对抗艾滋病毒/艾滋病。虽然通过CaCo-2肠道模型的渗透渗透差异非常有限，但蛋白酶抑制剂Lopinavir的渗透在乳液形式的上皮单层施加到乳液形式时比水溶液中的对照（约10倍）相当高（约10倍） DMSO车辆。所呈现的纳米乳液方法可允许针对各种药物的药物特异性渗透改善。

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  • 来源
    《RSC Advances》 |2018年第23期|共8页
  • 作者

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

  • 作者单位

    Univ Liverpool Dept Mol &

    Clin Pharmacol Block H 70 Pembroke Pl Liverpool L69 3GF Merseyside England;

    Univ Liverpool Dept Chem Crown St Liverpool L69 7ZD Merseyside England;

    Univ Liverpool Dept Chem Crown St Liverpool L69 7ZD Merseyside England;

    Univ Liverpool Dept Mol &

    Clin Pharmacol Block H 70 Pembroke Pl Liverpool L69 3GF Merseyside England;

    Univ Liverpool Dept Mol &

    Clin Pharmacol Block H 70 Pembroke Pl Liverpool L69 3GF Merseyside England;

    Univ Liverpool Dept Chem Crown St Liverpool L69 7ZD Merseyside England;

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  • 正文语种 eng
  • 中图分类 化学;
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