没食子酸/羟丙基-β-环糊精复合物：提高溶解度以应用于白色念珠菌体外/体内生物膜

Gallic acid/hydroxypropyl-β-cyclodextrin complex: Improving solubility for application on in vitro/ in vivo Candida albicans biofilms.

作者信息

Teodoro Guilherme Rodrigues, Gontijo Aline Vidal Lacerda, Borges Aline Chiodi, Tanaka Márcia Hiromi, Lima Gabriela de Morais Gouvêa, Salvador Marcos José, Koga-Ito Cristiane Yumi

机构信息

Oral Biopathology Graduate Program, São José dos Campos Institute of Science and Technology, Universidade Estadual Paulista/UNESP, São José dos Campos, SP, Brazil.

Departament of Environmental Engineering, São José dos Campos Institute of Science and Technology, Universidade Estadual Paulista/UNESP, São José dos Campos, SP, Brazil.

出版信息

PLoS One. 2017 Jul 11;12(7):e0181199. doi: 10.1371/journal.pone.0181199. eCollection 2017.

The aim of this study was to increase the solubility of gallic acid (GA) for the treatment of Candida albicans biofilm, which is very difficult to treat and requires high drug concentrations. Cyclodextrins (CDs) were used for this purpose. Complexes were evaluated by phase-solubility studies, prepared by spray drying and characterized by drug loading, scanning electron microscopy (SEM) and differential scanning calorimetry (DSC). The complexes were tested on C. albicans biofilm using in vitro and in vivo models. HPβCD formed soluble inclusion complexes with GA. The percentage of GA in GA/HPβCD was 10.8 ± 0.01%. The SEM and DSC analyses confirmed the formation of inclusion complexes. GA/HPβCD maintained the antimicrobial activity of the pure GA. GA/HPβCD was effective on C. albicans biofilms of 24 and 48h. The in vivo results showed an anti-inflammatory activity of GA/HPβCD with no difference in invading hypha counting among the groups. This study encourages the development of new antifungal agents.

本研究的目的是提高没食子酸（GA）的溶解度，用于治疗白色念珠菌生物膜，该生物膜很难治疗且需要高药物浓度。环糊精（CDs）用于此目的。通过相溶解度研究评估复合物，通过喷雾干燥制备复合物，并通过载药量、扫描电子显微镜（SEM）和差示扫描量热法（DSC）进行表征。使用体外和体内模型对复合物在白色念珠菌生物膜上进行测试。HPβCD与GA形成可溶性包合物。GA/HPβCD中GA的百分比为10.8±0.01%。SEM和DSC分析证实了包合物的形成。GA/HPβCD保持了纯GA的抗菌活性。GA/HPβCD对24小时和48小时的白色念珠菌生物膜有效。体内结果显示GA/HPβCD具有抗炎活性，各组间侵入菌丝计数无差异。本研究鼓励开发新的抗真菌药物。