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辅酶Q10和D-泛酰三乙酸负载脂质体的设计、优化与表征

Design, optimization and characterization of coenzyme Q10- and D-panthenyl triacetate-loaded liposomes.

作者信息

Çelik Burak, Sağıroğlu Ali Asram, Özdemir Samet

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Bezmialem Vakıf University.

Department of Pharmaceutical Technology, Faculty of Pharmacy, Yeditepe University, Istanbul, Turkey.

出版信息

Int J Nanomedicine. 2017 Jul 7;12:4869-4878. doi: 10.2147/IJN.S140835. eCollection 2017.

Abstract

Coenzyme Q10 (CoQ10) is a lipid-soluble molecule found naturally in many eukaryotic cells and is essential for electron transport chain and energy generation in mitochondria. D-Panthenyl triacetate (PTA) is an oil-soluble derivative of D-panthenol, which is essential for coenzyme A synthesis in the epithelium. Liposomal formulations that encapsulate both ingredients were prepared and optimized by applying response surface methodology for increased stability and skin penetration. The optimum formulation comprised 4.17 mg CoQ10, 4.22 mg PTA and 13.95 mg cholesterol per 100 mg of soy phosphatidylcholine. The encapsulation efficiency of the optimized formulation for CoQ10 and PTA was found to be 90.89%±3.61% and 87.84%±4.61%, respectively. Narrow size distribution was achieved with an average size of 161.6±3.6 nm, while a spherical and uniform shape was confirmed via scanning electron microscopy and transmission electron microscopy images. Cumulative release of 90.93% for PTA and 24.41% for CoQ10 was achieved after 24 hours of in vitro release study in sink conditions. Physical stability tests indicated that the optimized liposomes were suitable for storage at 4°C for at least 60 days. The results suggest that the optimized liposomal formulation would be a promising delivery system for both ingredients in various topical applications.

摘要

辅酶Q10(CoQ10)是一种脂溶性分子,天然存在于许多真核细胞中,对线粒体中的电子传递链和能量产生至关重要。D-泛酰三乙酸酯(PTA)是D-泛醇的油溶性衍生物,对上皮细胞中辅酶A的合成至关重要。通过应用响应面法制备并优化了包裹这两种成分的脂质体制剂,以提高稳定性和皮肤渗透性。最佳配方为每100mg大豆磷脂酰胆碱含有4.17mg CoQ10、4.22mg PTA和13.95mg胆固醇。优化后的制剂对CoQ10和PTA的包封率分别为90.89%±3.61%和87.84%±4.61%。平均粒径为161.6±3.6nm,实现了窄粒径分布,同时通过扫描电子显微镜和透射电子显微镜图像证实了其球形且均匀的形状。在水槽条件下进行24小时体外释放研究后,PTA的累积释放率为90.93%,CoQ10的累积释放率为24.41%。物理稳定性测试表明,优化后的脂质体适合在4°C下储存至少60天。结果表明,优化后的脂质体制剂将是这两种成分在各种局部应用中的一种有前景的递送系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2356/5511013/1d9f82992ad7/ijn-12-4869Fig1.jpg

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