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脂质双层包覆的纳米胶束能够实现药物的持续释放和增强内化。

Lipid-bilayer-coated nanogels allow for sustained release and enhanced internalization.

机构信息

Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, PR China.

Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, PR China.

出版信息

Int J Pharm. 2018 Nov 15;551(1-2):8-13. doi: 10.1016/j.ijpharm.2018.09.008. Epub 2018 Sep 6.

Abstract

Nanoparticle drug delivery system improves the therapeutic efficacy of a drug; however, achieving sustained release from nanoparticles is challenging, owing to the increase of surface area and pronounced burst release. In this study, by incorporating an organogel of 12-hydroxystearic acid (12-HSA) into lipid-bilayers, a gel-liposomal formulation was developed to sustain drug release over time. The lipid-bilayer-coated nanogels (LBCNs) with a particle size of approximately 200 nm and with a core-shell structure had an entrapment efficiency of up to 80% for paclitaxel. LBCNs could continually release both hydrophobic and water-soluble drugs over time. Interestingly, the incorporation of organogel enhanced the cellular uptake of liposomes significantly and, accordingly, enabled improved cytotoxicity of chemotherapy agent against the cancer cells. In conclusion, by formulating the organogel into the lipid bilayers, gel-liposomes were developed, allowing for sustained drug release, improved internalization and the resultant enhancement of cytotoxicity of chemotherapy agent to cancer cells.

摘要

纳米药物传递系统提高了药物的治疗效果;然而,由于表面积的增加和明显的爆发释放,实现纳米粒子的持续释放具有挑战性。在这项研究中,通过将 12-羟基硬脂酸(12-HSA)的有机凝胶纳入脂质双层,开发了一种凝胶脂质体制剂,以随着时间的推移持续释放药物。具有约 200nm 粒径和核壳结构的脂质双层包覆纳米凝胶(LBCN)对紫杉醇的包封效率高达 80%。LBCN 可以随着时间的推移持续释放疏水性和水溶性药物。有趣的是,有机凝胶的掺入显著增强了脂质体的细胞摄取,从而提高了化疗药物对癌细胞的细胞毒性。总之,通过将有机凝胶制剂成脂质双层,开发了凝胶脂质体,允许药物持续释放、改善内化,并因此增强化疗药物对癌细胞的细胞毒性。

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