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由无定形聚酯制备的纳米胶囊:对物理化学特性、药物释放和光稳定性的影响。

Nanocapsules prepared from amorphous polyesters: effect on the physicochemical characteristics, drug release, and photostability.

作者信息

Fontana M C, Coradini K, Pohlmann A R, Guterres S S, Beck R C R

机构信息

Programa de Pós-Graduação em Ciências Farmacêuticas, Centro de Ciências da Saúde, Departamento de Farmácia Industrial, Av. Roraima, 1000, Universidade Federal de Santa Maria, Santa Maria, RS 97105-900, Brazil.

出版信息

J Nanosci Nanotechnol. 2010 May;10(5):3091-9. doi: 10.1166/jnn.2010.1920.

Abstract

The influence of the polymeric amorphous materials on the physicochemical and drug release properties of drug-loaded nanocapsules as well as their role on the protection of the entrapped drug against the degradation induced by UV radiation was evaluated. Nanocapsules were prepared by interfacial deposition of preformed polymer (PLA, PLGA 50:50, and PLGA 85:15) using clobetasol propionate as the drug model. In vitro drug release was evaluated by the dialysis bag method. Photochemical stability was studied under UVA radiation. After preparation, all formulations presented nanometric mean size (180-200 nm), polydispersity index below 0.20, acid pH, negative zeta potential, and encapsulation efficiency close to 100%. Clobetasol propionate-loaded PLGA nanocapsules presented a lower physicochemical stability, showing a high drug leakage during 3 months of storage. In vitro studies showed biphasic drug release from all nanocapsules (according to an anomalous transport) and no influence of the hydrophilic characteristics of the amorphous polymeric material on the release rate. The photostability of clobetasol propionate under UVA radiation was improved by its incorporation into PLA and PLGA nanocapsules showing that besides semicrystalline polymers, amorphous polymers could also efficiently protect nanoencapsulated drugs against UV radiation.

摘要

评估了聚合物无定形材料对载药纳米胶囊的物理化学和药物释放特性的影响,以及它们在保护包封药物免受紫外线辐射诱导降解方面的作用。以丙酸氯倍他索作为药物模型,通过预制聚合物(聚乳酸、丙交酯乙交酯共聚物50:50和丙交酯乙交酯共聚物85:15)的界面沉积制备纳米胶囊。采用透析袋法评估体外药物释放。在紫外线A辐射下研究光化学稳定性。制备后,所有制剂的平均粒径均为纳米级(180 - 200 nm),多分散指数低于0.20,呈酸性pH值,zeta电位为负,包封效率接近100%。载有丙酸氯倍他索的丙交酯乙交酯共聚物纳米胶囊的物理化学稳定性较低,在储存3个月期间显示出较高的药物泄漏率。体外研究表明,所有纳米胶囊均呈现双相药物释放(根据异常转运),无定形聚合物材料的亲水性特征对释放速率无影响。将丙酸氯倍他索包封于聚乳酸和丙交酯乙交酯共聚物纳米胶囊中可提高其在紫外线A辐射下的光稳定性,这表明除半结晶聚合物外,无定形聚合物也能有效保护纳米包封药物免受紫外线辐射。

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