Alfons K, Engstrom S
Department of Food Technology, Lund University, Sweden.
J Pharm Sci. 1998 Dec;87(12):1527-30. doi: 10.1021/js980209z.
The liquid sponge phase, a bicontinuous lipid-water system, formed in solvent-monoolein-water systems was investigated with respect to drug compatibility. The solvents propylene glycol and poly(ethylene glycol) swell the bicontinuous cubic phase of the monoolein-water system and form the sponge phase at constant water contents, 40 and 30% w/w, respectively. Amphiphilic drugs such as lidocaine participate in the bilayer and act on the interfacial curvature according to the amphiphilic packing concept. The interfacial curvatures increase/decrease depending on the salt/base forms of the molecules. The quantity of lidocaine that can be incorporated into the sponge phase depends not only on the form of lidocaine but also on the lipid content and the solvent used in the sponge phase. Addition of the water-insoluble gramicidin S to the sponge phase resulted in a stiff isotropic phase, possibly a cubic phase, indicating interaction of gramicidin S with the lipid bilayer. The in vitro release of lidocaine was significantly faster from the sponge phase in the propylene glycol system than from the corresponding cubic phase without solvent.
研究了在溶剂-单油酸甘油酯-水体系中形成的液体海绵相（一种双连续脂质-水体系）的药物相容性。溶剂丙二醇和聚乙二醇使单油酸甘油酯-水体系的双连续立方相膨胀，并分别在水含量恒定为40%（w/w）和30%（w/w）时形成海绵相。两亲性药物如利多卡因参与双层结构，并根据两亲性堆积概念作用于界面曲率。界面曲率根据分子的盐/碱形式增加/减少。可掺入海绵相的利多卡因量不仅取决于利多卡因的形式，还取决于脂质含量和海绵相中使用的溶剂。向海绵相中添加水不溶性短杆菌肽S会导致形成刚性各向同性相，可能是立方相，这表明短杆菌肽S与脂质双层发生了相互作用。在丙二醇体系中，利多卡因从海绵相的体外释放明显快于相应的无溶剂立方相。
