Division of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand.
Division of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand; Biomaterials for Pharmaceutical Formulation and Drug Delivery, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand; Biofilm Research Group, Faculty of Dentistry, Khon Kaen University, Khon Kaen 40002, Thailand.
Int J Biol Macromol. 2020 Apr 1;148:1061-1071. doi: 10.1016/j.ijbiomac.2020.01.217. Epub 2020 Jan 23.
Calcium alginate (CA) beads loaded with clotrimazole (CZ) were modified by adding poloxamer (PLX) in this study. Blends of PLX188 or PLX407 into sodium alginate (SA) dispersions caused a decrease in the SA zeta potential and led to viscosity synergism. SA with carboxyl and hydroxyl groups can interact with the hydroxyl groups of PLX via hydrogen bonding. A stronger interaction of SA with PLX407 was found when compared to the interaction between SA and PLX188. The PLX-CA beads gave a higher CZ entrapment efficiency than the CA beads. The highest PLX content used created an amorphous form of CZ in the beads because of the CZ solubilization by the PLX micelles. The addition of 0.5 or 1% w/v PLX can strengthen the CZ-loaded CA beads. Furthermore, the PLX-CA beads display a lower water uptake than the CA beads. PLX micellization can enhance CZ release and enhance the efficacy of CZ against Candida albicans. This study indicates that the molecular interaction of SA with PLX and the PLX micellization of CZ can improve the characteristics of CZ-loaded CA beads, which offer good potential for use as drug delivery systems or drug reservoirs in tablets for oral candidiasis.
本研究通过添加泊洛沙姆（PLX）对载克霉唑（CZ）海藻酸钠（CA）微球进行改性。PLX188 或 PLX407 与海藻酸钠（SA）分散体的混合物导致 SA 动电位降低，并导致粘度协同作用。具有羧基和羟基的 SA 可以通过氢键与 PLX 的羟基相互作用。与 SA 和 PLX188 之间的相互作用相比，发现 SA 与 PLX407 的相互作用更强。PLX-CA 微球的 CZ 包封效率高于 CA 微球。由于 PLX 胶束使 CZ 增溶，使用的最高 PLX 含量在微球中形成了 CZ 的无定形形式。添加 0.5 或 1%w/v PLX 可以增强载 CZ 的 CA 微球。此外，PLX-CA 微球的吸水率低于 CA 微球。PLX 胶束化可以增强 CZ 的释放，并提高 CZ 对白念珠菌的功效。本研究表明，SA 与 PLX 的分子相互作用以及 CZ 的 PLX 胶束化可以改善载 CZ 的 CA 微球的特性，为将其用作口腔念珠菌病片剂中的药物传递系统或药物储库提供了良好的潜力。
