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琥珀酸舒马曲坦弹性囊用于经皮给药:特性和体外渗透研究。

Elastic vesicles of sumatriptan succinate for transdermal administration: characterization and in vitro permeation studies.

机构信息

Departamento de Fisiología, Farmacología y Toxicología, Facultad de Ciencias de la Salud, Universidad CEU Cardenal Herrera, Moncada, Spain.

出版信息

J Liposome Res. 2011 Mar;21(1):55-9. doi: 10.3109/08982101003736002. Epub 2010 Apr 30.

Abstract

Elastic liposomes, including sumatriptan succinate, were prepared for their transdermal administration. Lipid vesicles containing 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC) or l-α-phosphatidylcholine dilauroyl (DLPC) phospholipids were characterized for various parameters, including size, particle-size distribution (i.e., polydispersity index), and elasticity. In vitro transdermal experiments for the study of the skin penetration of sumatriptan succinate contained in liposomes were performed by using flow-through diffusion cells. The diameter of sumatriptan liposomes with different lipid compositions varied between 279 and 282 nm, and the polydispersity index value for the size distribution of liposomal formulations was <0.5. DLPC vesicles proved to be more elastic and provided a higher sumatriptan transdermal flux than vesicles formulated with DOPC phospolipid.

摘要

弹性脂质体,包括琥珀酸舒马普坦,被制备用于经皮给药。含有 1,2-二油酰基-sn-甘油-3-磷酸胆碱 (DOPC) 或 l-α-磷脂酰胆碱二月桂酰基 (DLPC) 磷脂的脂质体在各种参数方面进行了表征,包括大小、粒径分布(即多分散指数)和弹性。通过使用流通扩散细胞进行了体外透皮实验,以研究包含在脂质体中的琥珀酸舒马普坦的皮肤渗透。具有不同脂质组成的琥珀酸舒马普坦脂质体的直径在 279 和 282nm 之间变化,并且脂质体制剂的粒径分布的多分散指数值<0.5。DLPC 囊泡被证明具有更高的弹性,并提供比用 DOPC 磷脂形成的囊泡更高的舒马普坦经皮通量。

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