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含有甲氧基肉桂酸辛酯的聚-ε-己内酯纳米胶囊:制备与表征

Poly-epsilon-caprolactone nanocapsules containing octyl methoxycinnamate: preparation and characterization.

作者信息

Jiménez M M, Pelletier J, Bobin M F, Martini M C, Fessi H

机构信息

Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, Alcalá University, Madrid, Spain.

出版信息

Pharm Dev Technol. 2004 Aug;9(3):329-39. doi: 10.1081/pdt-200031456.

Abstract

This study investigates the different nanocapsules (NCs) made of poly-epsilon-caprolactone (PCL) containing the lipophilic sunscreen Escalol 557 [octyl methoxycinnamate (OMC)] and analyzes the influence of nanoparticle-based systems on light-induced decomposition of the sunscreen agent. The NCs were designed and prepared by the solvent displacement method. Formulation parameters, such as the nature and volume of the organic and aqueous phase and the nature and concentration of the surfactants and polymer, have relevant implications on NC elaboration. We investigated the influence of several technological (stirring speed: 300-800 rpm) and formulation factors [polymer amount, 195-244.5 mg; surfactant, Tween 85 (Polysorbate 85), Montanox 80 (Polysorbate 80), and Synperonic PE/F68 (Poloxamer 188) as stabilizing agents; and volume of the organic phase, 20-30 mL of acetone] on the particle size and the OMC loading capacity of the formulations--encapsulation efficiency and yield. The sizes of NC obtained were in the range of 309 to 1042 nm, the encapsulation efficiencies ranged from 93.82% to 99.97%, and yields of NC encapsulation ranged from 48.12% to 86.28%. Of all the preset experimental conditions, Montanox 80, 30 mL of acetone, 244.5 mg of polymer, and a stirring speed of 350 rpm have been selected as the best in this experimental design study. The experimental conditions selected to obtain OMC-loaded NC of 374 nm resulted in a high entrapment percentage (97.52%) and yield (82.95%). The PCL nanoparticles loaded with OMC were effective in reducing light-induced degradation of the sunscreen agent.

摘要

本研究考察了由聚己内酯(PCL)制成的含有亲脂性防晒剂埃斯卡洛尔557 [甲氧基肉桂酸辛酯(OMC)]的不同纳米胶囊(NCs),并分析了基于纳米颗粒的体系对防晒剂光致分解的影响。NCs通过溶剂置换法设计并制备。配方参数,如有机相和水相的性质和体积以及表面活性剂和聚合物的性质和浓度,对NCs的制备有重要影响。我们研究了几种工艺因素(搅拌速度:300 - 800转/分钟)和配方因素[聚合物用量,195 - 244.5毫克;表面活性剂,吐温85(聚山梨酯85)、蒙旦诺克斯80(聚山梨酯80)和泊洛沙姆PE/F68(泊洛沙姆188)作为稳定剂;以及有机相体积,20 - 30毫升丙酮]对制剂的粒径和OMC负载量——包封效率和产率的影响。所获得的NCs尺寸在309至1042纳米范围内,包封效率在93.82%至99.97%之间,NCs包封产率在48.12%至86.28%之间。在所有预设的实验条件中,蒙旦诺克斯80、30毫升丙酮、244.5毫克聚合物和350转/分钟的搅拌速度在本实验设计研究中被选为最佳条件。为获得374纳米的负载OMC的NCs而选择的实验条件导致了高包封率(97.52%)和产率(82.95%)。负载OMC的PCL纳米颗粒在减少防晒剂的光致降解方面是有效的。

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