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采用维生素 E-TPGS 共载自组装磷脂纳米混合胶束系统改善芒果苷的生物药剂学性质。

Improving the biopharmaceutical attributes of mangiferin using vitamin E-TPGS co-loaded self-assembled phosholipidic nano-mixed micellar systems.

机构信息

University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160014, India.

Department of Histopathology, Post Graduate Institute of Medical Education and Research (PGIMER), Chandigarh, 160012, India.

出版信息

Drug Deliv Transl Res. 2018 Jun;8(3):617-632. doi: 10.1007/s13346-018-0498-4.

Abstract

The current research work encompasses the development, characterization, and evaluation of self-assembled phospholipidic nano-mixed miceller system (SPNMS) of a poorly soluble BCS Class IV xanthone bioactive, mangiferin (Mgf) functionalized with co-delivery of vitamin E TPGS. Systematic optimization using I-optimal design yielded self-assembled phospholipidic nano-micelles with a particle size of < 60 nm and > 80% of drug release in 15 min. The cytotoxicity and cellular uptake studies performed using MCF-7 and MDA-MB-231 cell lines demonstrated greater kill and faster cellular uptake. The ex vivo intestinal permeability revealed higher lymphatic uptake, while in situ perfusion and in vivo pharmacokinetic studies indicated nearly 6.6- and 3.0-folds augmentation in permeability and bioavailability of Mgf. In a nutshell, vitamin E functionalized SPNMS of Mgf improved the biopharmaceutical performance of Mgf in rats for enhanced anticancer potency.

摘要

本研究工作包括自组装磷脂纳米混合胶束系统(SPNMS)的开发、表征和评价,该系统是一种难溶性 BCS 分类 IV 型的姜黄素生物活性物质芒果苷(Mgf),与维生素 E TPGS 共递送。采用 I-最优设计进行系统优化,得到了粒径小于 60nm、15min 内药物释放超过 80%的自组装磷脂纳米胶束。使用 MCF-7 和 MDA-MB-231 细胞系进行的细胞毒性和细胞摄取研究表明,这种纳米胶束具有更高的杀伤效果和更快的细胞摄取速度。离体肠通透性研究表明,该纳米胶束具有更高的淋巴摄取能力,而在体灌注和体内药代动力学研究表明,Mgf 的通透性和生物利用度分别提高了近 6.6 倍和 3.0 倍。总之,维生素 E 功能化的 Mgf SPNMS 改善了 Mgf 在大鼠体内的生物药剂学性能,增强了其抗癌效力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f1af/5937873/0be16ca1b60f/13346_2018_498_Fig1_HTML.jpg

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