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通过复乳溶剂蒸发技术制备的PHEA-PLA生物相容性纳米颗粒。

PHEA-PLA biocompatible nanoparticles by technique of solvent evaporation from multiple emulsions.

作者信息

Cavallaro Gennara, Craparo Emanuela Fabiola, Sardo Carla, Lamberti Gaetano, Barba Anna Angela, Dalmoro Annalisa

机构信息

Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, via Archirafi 32, 90123 Palermo, Italy.

Dipartimento di Ingegneria Industriale (DIIn), Università degli Studi di Salerno, via Giovanni Paolo II, 132, 84084 Fisciano (SA), Italy.

出版信息

Int J Pharm. 2015 Nov 30;495(2):719-27. doi: 10.1016/j.ijpharm.2015.09.050. Epub 2015 Sep 26.

Abstract

Nanocarriers of amphiphilic polymeric materials represent versatile delivery systems for poorly water soluble drugs. In this work the technique of solvent evaporation from multiple emulsions was applied to produce nanovectors based on new amphiphilic copolymer, the α,β-poly(N-2-hydroxyethyl)-DL-aspartamide-polylactic acid (PHEA-PLA), purposely synthesized to be used in the controlled release of active molecules poorly soluble in water. To this aim an amphiphilic derivative of PHEA, a hydrophilic polymer, was synthesized by derivatization of the polymeric backbone with hydrophobic grafts of polylactic acid (PLA). The achieved copolymer was thus used to produce nanoparticles loaded with α tocopherol (vitamin E) adopted as lipophilic model molecule. Applying a protocol based on solvent evaporation from multiple emulsions assisted by ultrasonic energy and optimizing the emulsification process (solvent selection/separation stages), PHEA-PLA nanostructured particles with total α tocopherol entrapment efficiency (100%), were obtained. The drug release is expected to take place in lower times with respect to PLA due to the presence of the hydrophilic PHEA, therefore the produced nanoparticles can be used for semi-long term release drug delivery systems.

摘要

两亲性聚合物材料的纳米载体是用于水溶性差的药物的通用递送系统。在这项工作中,采用了从多重乳液中蒸发溶剂的技术,以基于新型两亲性共聚物α,β-聚(N-2-羟乙基)-DL-天冬酰胺-聚乳酸(PHEA-PLA)制备纳米载体,该共聚物是特意合成用于控制释放水溶性差的活性分子的。为此,通过用聚乳酸(PLA)的疏水接枝对聚合物主链进行衍生化,合成了亲水性聚合物PHEA的两亲性衍生物。由此得到的共聚物用于制备负载α生育酚(维生素E)的纳米颗粒,α生育酚用作亲脂性模型分子。通过应用基于在超声能量辅助下从多重乳液中蒸发溶剂的方案并优化乳化过程(溶剂选择/分离阶段),获得了α生育酚总包封效率为100%的PHEA-PLA纳米结构颗粒。由于亲水性PHEA的存在,预计药物释放相对于PLA会在更短的时间内发生,因此所制备的纳米颗粒可用于半长期释放药物递送系统。

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