Faculty of Pharmacy, Silpakorn University, Sanamchan Palace campus, Nakhon Pathom, 73000, Thailand.
AAPS PharmSciTech. 2013 Mar;14(1):133-40. doi: 10.1208/s12249-012-9904-2. Epub 2012 Dec 14.
The aim of this study is to develop meloxicam (MX)-loaded cationic transfersomes as skin delivery carriers and to investigate the influence of formulation factors such as cholesterol and cationic surfactants on the physicochemical properties of transfersomes (i.e., particle size, size distribution, droplet surface charge and morphology), entrapment efficiency, stability of formulations and in vitro skin permeation of MX. The transfersomes displayed a spherical structure. Their size, charge, and entrapment efficiency depended on the composition of cholesterol and cationic surfactants in the formulation. Transfersomes provided greater MX skin permeation than conventional liposomes and MX suspensions. The penetration-enhancing mechanism of skin permeation by the vesicles prepared in this study may be due to the vesicle adsorption to and/or fusion with the stratum corneum. Our results suggest that cationic transfersomes may be promising dermal delivery carriers of MX.
本研究旨在制备负载美洛昔康（MX）的阳离子传递体作为皮肤给药载体，并考察胆固醇和阳离子表面活性剂等制剂因素对传递体（粒径、粒径分布、载药胶束表面电荷和形态）、包封率、制剂稳定性以及 MX 体外经皮渗透的影响。传递体呈现球形结构。其粒径、表面电荷和包封率取决于制剂中胆固醇和阳离子表面活性剂的组成。与传统脂质体和 MX 混悬剂相比，传递体增加了 MX 的皮肤渗透。本研究制备的囊泡的经皮渗透增强机制可能归因于囊泡对角质层的吸附和/或融合。研究结果表明，阳离子传递体可能是 MX 的有前途的经皮给药载体。
