Swarnakar Nitin K, Jain Vikas, Dubey Vaibhav, Mishra Dinesh, Jain N K
Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour University, Sagar (M.P.), 470003, India.
Pharm Res. 2007 Dec;24(12):2223-30. doi: 10.1007/s11095-007-9409-y. Epub 2007 Sep 8.
Formulation and characterization of progesterone loaded hexosomes employing a novel method for oromucosal delivery.
Hexosomes were prepared employing a method in which ethanolic solution of lipid phase (monolein and oleic acid) was vortexed with aqueous phase (surfactant solution) and characterized for particle size, morphology and internal structure. FT-IR and confocal laser scanning microscopy (CLSM) were performed to investigate the possible mechanism and penetration pathway of hexosomes within the mucosa.
Hexosomes exhibited anisotropy, hexagonal shape and nanometric size (251.2+/-1.8 nm). Internal structure confirmed by X-ray diffraction peaks with spacing ratio of radical1:radical3:radical4 proved two-dimensional hexagonal arrangements. Entrapment efficiency of system was greater than 95%. In vitro release studies revealed an enhanced transmucosal flux (4.67+/-0.14 microg cm(-2) h(-1)) and decreased lag time (1.54 h) across albino rabbit mucosa. FT-IR and CLSM of treated mucosa shows lipid extraction phenomena as well as structural irregularities within intercellular lipids respectively. These irregularities can function as 'virtual channels' facilitating hexosome's penetration.
Developed hexosomes formulation exhibited high entrapment efficiency, high permeability and better stability on storage, thus proposing itself a novel carrier for enhanced oromucosal delivery of progesterone.
采用一种新型方法制备用于口腔黏膜给药的载孕酮六方相脂质体并对其进行表征。
采用脂质相（单油酸甘油酯和油酸）的乙醇溶液与水相（表面活性剂溶液）涡旋混合的方法制备六方相脂质体，并对其粒径、形态和内部结构进行表征。进行傅里叶变换红外光谱（FT-IR）和共聚焦激光扫描显微镜（CLSM）研究，以探讨六方相脂质体在黏膜内的可能作用机制和渗透途径。
六方相脂质体呈现各向异性、六边形形状且粒径为纳米级（251.2±1.8 nm）。通过X射线衍射峰证实的内部结构，其间距比为根号1:根号3:根号4，证明为二维六方排列。该体系的包封率大于95%。体外释放研究表明，经白化兔黏膜的透黏膜通量增强（4.67±0.14 μg cm⁻² h⁻¹）且滞后时间缩短（1.54 h）。经处理黏膜的FT-IR和CLSM分别显示脂质提取现象以及细胞间脂质内的结构不规则性。这些不规则性可作为“虚拟通道”促进六方相脂质体的渗透。
所开发的六方相脂质体制剂表现出高包封率、高渗透性以及储存时更好的稳定性，因此自身可作为一种新型载体用于增强孕酮的口腔黏膜给药。
