Gravity-induced coating flows of vaginal gel formulations:: In vitro experimental analysis
Gravity-induced coating flows of vaginal gel formulations:: In vitro experimental analysis
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DOI：
10.1002/jps.20194
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发表时间：
2004-12-01
影响因子：
3.8
通讯作者：
Katz, DF
中科院分区：
文献类型：
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作者：
Kieweg, SL;Geonnotti, AR;Katz, DF
局部杀菌药物制剂对HIV的疗效部分取决于它们的涂层分布和在阴道上皮上的滞留。本研究主要研究重力作用下阴道凝胶的包衣流动，以及配方组成和表面润湿性对包衣的影响。我们假设屈服应力和表面润湿性的存在会影响涂层。实验成像并分析了凝胶在倾斜的亲水或疏水表面上的涂层流动。体外润湿条件支持那些被认为存在于体内阴道上皮上的条件。研究了六种商品化阴道凝胶：三种聚丙烯酸(PAA)和三种纤维素基。我们的研究小组将这些凝胶用于补充人体活体研究和其他体外实验分析；这项研究是将体内和体外测量联系起来的第一步。PAA凝胶包衣不同于纤维素基凝胶：前者具有屈服应力，可防止初始凝胶形状在滑动过程中变形。纤维素凝胶的涂布流动取决于表面的润湿性。PAA凝胶的滑移率与拟合的屈服应力值成反比。纤维素凝胶(亲水性表面)的涂膜流动速率与稠度指数无关，而与剪切稀化指数成反比。这项研究介绍了一种简单的方法来比较试验配方，并将它们的流动与凝胶成分和物理性质联系起来。它还表明了目前商业凝胶在涂层方面的差异。(C)2004年Wiley-Liss，Inc.和美国药剂师协会。
Efficacy of topical microbicidal drug delivery formulations against HIV depends in part on their coating distributions and retention on vaginal epithelium. This study focused on gravity-induced coating flows of vaginal gels, and effects of formulation composition and surface wettability on coating. We hypothesized that presence of a yield stress, and surface wettability, affect coating. Experiments imaged and analyzed coating flows of gels on inclined model hydrophilic or hydrophobic surfaces. The in vitro wettability conditions bracket those believed to exist on vaginal epithelium in vivo. Six commercial vaginal gels were studied: three polyacrylic acid-based (PAA) and three cellulose-based. Our research group uses these gels in complementary human in vivo studies and other in vitro experimental analyses; this study is a first step in linking the in vivo and in vitro measurements. Coating by PAA gels was different from cellulose-based gels: the former exhibited yield stresses, which prevented initial gel shape from deforming during sliding. Coating flows of cellulose gels depended upon surface wettability. The slipping rates of the PAA gels ranked inversely with fitted yield stress values. The coating flow rates of the cellulose gels (hydrophilic surface) did not correlate with consistency index, but ranked inversely with the shear-thinning index. This study introduces a simple methodology for comparing trial formulations and relating their flows to gel constituents and physical properties. It also suggests differences in coating by current commercial gels. (C) 2004 Wiley-Liss, Inc. and the American Pharmacists Association.