Chlorhexidine Mucoadhesive Buccal Tablets: The Impact of Formulation Design on Drug Delivery and Release Kinetics Using Conventional and Novel Dissolution Methods.
Chlorhexidine Mucoadhesive Buccal Tablets: The Impact of Formulation Design on Drug Delivery and Release Kinetics Using Conventional and Novel Dissolution Methods.
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DOI：
10.3390/ph14060493
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发表时间：
2021-05-23
期刊：
影响因子：
--
通讯作者：
Doudin K
中科院分区：
文献类型：
--
作者：
Al-Ani E;Hill D;Doudin K
口咽念珠菌病（OPC）是一种由念珠菌属引起的粘膜感染，在免疫力低下的人中很常见这种情况主要使用口服抗真菌药治疗。洗必泰（CHD）是一种杀真菌剂，可用作漱口水和口腔凝胶。由于目前制剂的停留时间较短，因此在OPC治疗中用作佐剂。本研究测定了其对C.白色念珠菌生物膜和与HEK 293人细胞系的生物相容性。然后，将其配制成粘膜粘附水凝胶口含片以延长其活性。不同比例的羟丙基甲基纤维素（HPMC），泊洛沙姆407（P407），和三种不同类型的多元醇用于制备片剂，然后研究其理化性质，离体粘膜粘附，药物释放曲线，和药物释放动力学。使用装置I和受控流速（CFR）方法进行释放。结果表明，CHD具有生物相容性，并且在20 µg/mL的浓度下对念珠菌生物膜有效。通过差示扫描量热法（DSC）和傅里叶变换红外光谱（FTIR）未观察到药物与辅料的相互作用。P407和多元醇比率的增加显示溶胀指数的降低和CHD体外释放的增加。CHD从所选制剂中的释放为86- 92%。结果表明，洗必泰片是一种可能的候选人，用于治疗口咽念珠菌病。
Oropharyngeal candidiasis (OPC) is a mucosal infection caused by Candida spp., and it is common among the immunocompromised. This condition is mainly treated using oral antifungals. Chlorhexidine (CHD) is a fungicidal and is available as a mouth wash and oral gel. It is used as an adjuvant in the treatment of OPC due to the low residence time of the current formulations. In this study, its activity was tested against C. albicans biofilm and biocompatibility with the HEK293 human cell line. Then, it was formulated as mucoadhesive hydrogel buccal tablets to extend its activity. Different ratios of hydroxypropyl methylcellulose (HPMC), poloxamer 407 (P407), and three different types of polyols were used to prepare the tablets, which were then investigated for their physicochemical properties, ex vivo mucoadhesion, drug release profiles, and the kinetics of drug release. The release was performed using Apparatus I and a controlled flow rate (CFR) method. The results show that CHD is biocompatible and effective against Candida biofilm at a concentration of 20 µg/mL. No drug excipient interaction was observed through differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FTIR). The increase in P407 and polyol ratios showed a decrease in the swelling index and an increase in CHD in vitro release. The release of CHD from the selected formulations was 86–92%. The results suggest that chlorhexidine tablets are a possible candidate for the treatment of oropharyngeal candidiasis.
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