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Alginate-poloxamer beads for clotrimazole delivery: Molecular interactions, mechanical properties, and anticandidal activity.
International Journal of Biological Macromolecules ( IF 8.2 ) Pub Date : 2020-01-23 , DOI: 10.1016/j.ijbiomac.2020.01.217
Rapee Khlibsuwan 1 , Watcharee Khunkitti 2 , Thaned Pongjanyakul 3
Affiliation  

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.

中文翻译:

海藻酸钠-泊洛沙姆珠用于克霉唑的递送:分子相互作用,机械性能和抗候选活性。

在这项研究中,通过添加泊洛沙姆(PLX)修饰了负载克霉唑(CZ)的藻酸钙(CA)珠。将PLX188或PLX407掺入藻酸钠(SA)分散液中会导致SA Zeta电位降低,并导致粘度协同作用。带有羧基和羟基的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珠比CA珠具有更高的CZ截留效率。由于PLX胶束可溶解CZ,因此所用的最高PLX含量可在微珠中形成无定形形式的CZ。添加0.5或1%w / v PLX可以增强CZ负载的CA微珠。此外,PLX-CA珠的吸水率比CA珠低。PLX胶束化作用可以增强CZ释放并增强CZ对抗白色念珠菌的功效。这项研究表明,SA与PLX的分子相互作用以及CZ的PLX胶束化可以改善CZ负载的CA微珠的特性,这为用作口服念珠菌病的片剂的药物递送系统或药物储库提供了良好的潜力。
更新日期:2020-01-23
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