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基于微球的甲氧基肉桂酸乙基己酯改良防晒配方。

Microsphere based improved sunscreen formulation of ethylhexyl methoxycinnamate.

作者信息

Gogna Deepak, Jain Sunil K, Yadav Awesh K, Agrawal G P

机构信息

Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour University, Sagar-470 003, India.

出版信息

Curr Drug Deliv. 2007 Apr;4(2):153-9. doi: 10.2174/156720107780362285.

Abstract

Polymethylmethacrylate (PMMA) microspheres of ethylhexyl methoxycinnamate (EHM) were prepared by emulsion solvent evaporation method to improve its photostability and effectiveness as sunscreening agent. Process parameters like stirring speed and aqueous polyvinyl alcohol (PVA) concentration were analyzed in order to optimize the formulations. Shape and surface morphology of the microspheres were examined using scanning electron microscopy. Particle size of the microspheres was determined using laser diffraction particle size analyzer. The PMMA microspheres of EHM were incorporated in water-removable cream base. The in vitro drug release of EHM in pH 7.4 was performed using dialysis membrane. Thin layer chromatography was performed to determine photostability of EHM inside the microspheres. The formulations were evaluated for sun protection factor (SPF) and minimum erythema dose (MED) in albino rats. Cream base formulation containing microspheres prepared using EHM:PMMA in ratio of 1:3 (C(3)) showed slowest drug (EHM) release and those prepared with EHM: PMMA in ratio of 1:1 showed fastest release. The cream base formulations containing EHM loaded microspheres had shown better SPF (more than 16.0) as compared to formulation C(d) that contained 3% free EHM as sunscreen agent and showed SPF 4.66. These studies revealed that the incorporation of EHM loaded PMMA microspheres into cream base had greatly increased the efficacy of sunscreen formulation approximately four times. Further, photostability was also shown to be improved in PMMA microspheres.

摘要

通过乳液溶剂蒸发法制备了甲氧基肉桂酸乙基己酯(EHM)的聚甲基丙烯酸甲酯(PMMA)微球,以提高其作为防晒剂的光稳定性和有效性。分析了搅拌速度和聚乙烯醇(PVA)水溶液浓度等工艺参数,以优化配方。使用扫描电子显微镜检查微球的形状和表面形态。使用激光衍射粒度分析仪测定微球的粒径。将EHM的PMMA微球掺入可水洗乳膏基质中。使用透析膜在pH 7.4条件下进行EHM的体外药物释放实验。进行薄层色谱分析以确定微球内EHM的光稳定性。在白化大鼠中评估配方的防晒系数(SPF)和最小红斑剂量(MED)。含有按EHM:PMMA比例为1:3制备的微球的乳膏基质配方(C(3))显示药物(EHM)释放最慢,而按EHM:PMMA比例为1:1制备的配方显示释放最快。与含有3%游离EHM作为防晒剂且SPF为4.66的配方C(d)相比,含有负载EHM微球的乳膏基质配方显示出更好的SPF(超过16.0)。这些研究表明,将负载EHM的PMMA微球掺入乳膏基质中可使防晒配方的功效大幅提高约四倍。此外,PMMA微球的光稳定性也得到了改善。

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