Oral drug delivery with nanoparticles has demonstrated great potential for drugs with poor bioavailability. Efficient delivery is possible by overcoming both the mucus and epithelial barrier of the gastrointestinal tract (GIT). Cationic lipid-assisted nanoparticles (CLANs), which are composed of amphiphilic block copolymers and cationic lipids, have been well studied and have been proved beneficial for drug delivery. In this study, CLANs prepared by poly(ethylene glycol)-block-poly(lactic acid) (PEG-b-PLA) and 1,2-dioleoyl-3-trimethylammonium-propanechloride (DOTAP) or N,N-bis(2-hydroxyethyl)-N-methyl-N-(2-cholesteryloxycarbonyl aminoethyl)ammoniumbromide (BHEM-Chol) were used for oral delivery of tacrolimus (FK506) for ulcerative colitis treatment. The average size of these nanoparticles is around 110 nm and the zeta-potential is 35 mV. These nanoparticles maintained their size in buffer solutions of pH 1.2 and 6.8, and slowly release the encapsulated drug. CLANs can be accumulated in the colon and transported through the epithelium in the colitis model by dextran sulfate sodium salt (DSS), leading to attenuation of DSS-induced colitis.

中文翻译：

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他克莫司与阳离子脂质辅助纳米颗粒的结合用于溃疡性结肠炎的治疗†

具有纳米颗粒的口服药物递送已证明具有生物利用度较差的药物的巨大潜力。通过克服粘液和胃肠道上皮屏障（GIT），可以实现高效递送。由两亲性嵌段共聚物和阳离子脂质组成的阳离子脂质辅助纳米颗粒（CLANs）已得到充分研究，并已证明对药物递送有利。在这项研究中，所有CLAN制备由聚（乙二醇） -嵌段-聚（乳酸）（PEG- b -PLA）和1,2-二油酰基-3-三甲基铵- propanechloride（DOTAP）或ñ，ñ双（2- -羟乙基）-N-甲基-N-（2-胆固醇基氧羰基氨基乙基）溴化铵（BHEM-Chol）用于他克莫司（FK506）的口服给药，用于溃疡性结肠炎的治疗。这些纳米粒子的平均大小约为110 nm，ζ电位为35 mV。这些纳米颗粒在pH 1.2和6.8的缓冲溶液中保持其大小，并缓慢释放封装的药物。CLAN可以在结肠炎模型中的结肠中积聚，并通过硫酸葡聚糖硫酸钠盐（DSS）穿过上皮运输，从而减轻DSS诱导的结肠炎。