Farkas E, Schubert R, Zelkó R
Pharmaceutical Institute, Semmelweis University, Hogyes E. Street 7, Budapest 1092, Hungary.
Int J Pharm. 2004 Jun 18;278(1):63-70. doi: 10.1016/j.ijpharm.2004.02.022.
Previous studies confirm that beta-sitosterol is very effective in altering the molecular packing of soybean lecithin bilayers even more than the cholesterol. The primary aim of the present study was to evaluate the influence of the beta-sitosterol portion in the lipid bilayer on the physical-chemical characteristics of the prepared gel systems, and its influence on the consequent drug release from the liposomes obtained from vesicular phospholipid gels (VPG-s) by redispersion. VPG-s were prepared of different molar ratios of lecithin:sterol components (10:90-35:65 mol%). The mixture was hydrated with the aqueous solution of chlorhexidin digluconate in order to achieve 30% (w/w) final concentration of the lipid mixtures and 4% (w/w) concentration of the drug in each homogenized VPG sample. To characterize the obtained VPG systems optical microscopic examinations using polarized light, differential scanning calorimetry (DSC), photon correlation spectroscopy (PCS), and dynamic surface tension measurements were carried out. Vertical type diffusion cell was applied to determine the amount of released chlorhexidine digluconate. As a result of the surface tension-decreasing effect of beta-sitosterol, the membrane deformability and the dispersity of the system increased. The increased dispersity and fluidity significantly increased the extent of released chlorhexidine from the vesicles.
先前的研究证实,β-谷甾醇在改变大豆卵磷脂双层的分子排列方面非常有效,甚至比胆固醇更有效。本研究的主要目的是评估脂质双层中β-谷甾醇部分对所制备凝胶系统物理化学特性的影响,以及其对通过再分散从囊泡磷脂凝胶(VPG-s)获得的脂质体中药物释放的影响。VPG-s由不同摩尔比的卵磷脂:甾醇成分(10:90 - 35:65摩尔%)制备而成。将混合物用葡萄糖酸氯己定水溶液水合,以使每个均质化的VPG样品中脂质混合物的最终浓度达到30%(w/w),药物浓度达到4%(w/w)。为了表征所获得的VPG系统,使用偏振光进行光学显微镜检查、差示扫描量热法(DSC)、光子相关光谱法(PCS)以及动态表面张力测量。应用垂直型扩散池来测定释放的葡萄糖酸氯己定的量。由于β-谷甾醇的表面张力降低作用,系统的膜变形性和分散性增加。分散性和流动性的增加显著提高了从囊泡中释放的氯己定的程度。