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首页> 外文期刊>The Open Drug Delivery Journal >Sertaconazole-Loaded Cyclodextrin–Polysaccharide Hydrogels as Antifungal Devices§
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Sertaconazole-Loaded Cyclodextrin–Polysaccharide Hydrogels as Antifungal Devices§

机译：负载舒他康唑的环糊精-多糖水凝胶作为抗真菌药物§

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The aim of the present work was to develop novel hydrogels for delivering sertaconazole based on cyclodextrins and various biocompatible polysaccharides. Sertaconazole is an antifungal agent very effective for treatment of Candida albicans infections. However its poor aqueous solubility is still a challenging issue for developing suitable formulations. Complexation with cyclodextrins is a very attractive route to overcome this limitation, simultaneously enhancing its antifungal effectiveness. Hydroxypropyl-β-cyclodextrin (HPβCD) hydrogels prepared by direct cross-linking in presence of methylcellulose (MC), hydroxypropyl cellulose (HPC), hydroxypropyl methylcellulose (HPMC), carboxymethyl cellulose (CMCNa), or dextran were transparent and swelled in water without dissolving, which enables the formation of microenvironments very rich in cyclodextrin cavities responsible for hosting the drug and control its release rate. HPβCD hydrogels showed a high capability to load sertaconazole (with partition coefficients from 22 to 470) while still combining high water affinity (superabsorbency), versatile biomechanical properties (hardness and compressibility) and sustained release behavior (up to 4 days). Importantly, sertaconazol-loaded hydrogels showed effectiveness against Candida albicans in culture medium. HPβCD-polysaccharide hydrogels could be useful as sertaconazole delivery systems for the treatment of mucosal infections.
机译：本工作的目的是开发基于环糊精和各种生物相容性多糖的新型水凝胶，用于递送舍他康唑。舍他康唑是一种非常有效的抗真菌药，可治疗白色念珠菌感染。然而，其不良的水溶性仍然是开发合适制剂的挑战性问题。与环糊精的络合是克服这一局限性，同时增强其抗真菌效力的非常有吸引力的途径。通过在甲基纤维素（MC），羟丙基纤维素（HPC），羟丙基甲基纤维素（HPMC），羧甲基纤维素（CMCNa）或右旋糖酐存在下直接交联制备的羟丙基-β-环糊精（HPβCD）水凝胶是透明的且在水中溶胀而没有溶解，可以形成非常富集环糊精腔的微环境，这些腔负责容纳药物并控制其释放速率。 HPβCD水凝胶显示出很高的负载舍他康唑的能力（分配系数为22至470），同时仍具有高水亲和力（超吸收性），多种生物力学特性（硬度和可压缩性）和持续释放行为（长达4天）。重要的是，在培养基中，负载舍他康唑的水凝胶显示出对白色念珠菌的有效性。 HPβCD-多糖水凝胶可用作舍他康唑递送系统，用于治疗粘膜感染。

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