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用于制备具有可控释放特性和细胞相容性的聚(L-乳酸)纳米粒子的新型表面活性剂用于药物输送。

Novel surfactant for preparation of poly(L-lactic acid) nanoparticles with controllable release profile and cytocompatibility for drug delivery.

机构信息

College of Chemistry and Chemical Engineering, Yangzhou University, Yangzhou 225002, PR China.

College of Chemistry and Chemical Engineering, Yangzhou University, Yangzhou 225002, PR China.

出版信息

Colloids Surf B Biointerfaces. 2014 Mar 1;115:377-83. doi: 10.1016/j.colsurfb.2013.12.015. Epub 2013 Dec 16.

Abstract

Poly(L-lactic acid) nanoparticles loaded with a hydrophobic drug were prepared by an emulsion-evaporation process (oil in water) with a novel, effective and biocompatible surfactant butanedioic acid, 2-sulfo-1,4-butanedioic acid ditridecyl ester (sodium salt, 1:1) (BASDE). The particles are spherical in morphology and their diameters are controllable from 50 to 550nm with poly-dispersity indexes within the range of 0.122-0.340. The drug entrapment efficiency and drug content were measured by spectrophotometry. The drug release rate is affected by both the size of the particles and the drug content in the particles. In vitro cytotoxicity data indicate that these drug-loaded PLA nanoparticles are safe for hypodermic injection regard to the toxicological acceptance. This study demonstrates that using BASDE surfactant, the size of PLA nanoparticles can be controlled at the nanoscale with a narrow size distribution, and the drug release is controllable with excellent in vitro cytocompatibility. This may be due to efficient emulsification capability and biocompatibility of BASDE.

摘要

载疏水药物的聚(L-乳酸)纳米粒采用乳液蒸发法(油包水)制备,使用新型有效且生物相容的表面活性剂丁二酸-2-磺基-1,4-丁二醇二酯(钠盐,1:1)(BASDE)。所得纳米粒呈球形,粒径可从 50nm 至 550nm 范围内调控,多分散指数在 0.122-0.340 之间。采用分光光度法测定载药纳米粒的载药量和包封率。药物释放率既受纳米粒粒径又受纳米粒中药物含量的影响。体外细胞毒性数据表明,这些载药 PLA 纳米粒对于皮下注射是安全的,符合毒理学接受标准。该研究表明,使用 BASDE 表面活性剂,可以在纳米尺度上控制 PLA 纳米粒的粒径且粒径分布较窄,并具有可控制的药物释放,同时表现出优异的体外细胞相容性。这可能归因于 BASDE 的高效乳化能力和生物相容性。

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