表面真菌感染用酮康唑微孔膜包衣剂的设计、制备与表征

IF 2.2 4区医学 Q3 MYCOLOGY

Journal de mycologie medicale Pub Date : 2025-04-19 DOI:10.1016/j.mycmed.2025.101551

Zhaowei Jin , Danqing Wu , Yangnan Chen , Yanqiu Long , Yan Liu , Zhiyun Zheng , Shuangying Gui , Yuzhe Huang , Ning He

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引用次数: 0

摘要

酮康唑（KCZ）是一种咪唑类抗真菌药物，其溶解度低、稳定性差，限制了其有效吸收和生物利用度。为了提高KCZ的透皮吸收和生物利用度，研制了一种KCZ微海绵基膜包衣剂（KCZ- msf）。采用乳液溶剂蒸发法制备KCZ-MS，并采用Box-Behnken设计（BBD）优化处方组成。利用扫描电镜（SEM）、傅里叶变换红外光谱（FTIR）和差示扫描量热法（DSC）对优化后的KCZ-MS进行了表征。通过正交实验进一步优化膜包衣剂的制备工艺，将优化后的KCZ-MS转化为适合皮肤外用的膜包衣剂。KCZ-MS为球形多孔结构，平均粒径为22.42±8.45 μm，载药效率为20.74%，包封效率为92.12%，药物与辅料相容性良好。优化后的KCZ-MSF具有良好的物理性能。体外透皮实验结果显示，KCZ- msf在6、12、24 h时的皮肤滞留量均超过市售KCZ乳膏。药代动力学实验结果表明，KCZ- msf的曲线下面积（AUC0-24）为420.71±21.77 μg/(g·h)，是KCZ薄膜包衣剂（KCZ- f）的2.05倍，是市售酮康唑乳膏的1.29倍。因此，KCZ-MSF为浅表皮肤真菌感染的治疗提供了一个更有前景的平台。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Ketoconazole-loaded microspone film coating agent for superficial fungal infection: design, preparation and characterization

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Ketoconazole-loaded microspone film coating agent for superficial fungal infection: design, preparation and characterization

Ketoconazole (KCZ), an imidazole antifungal drug, is constrained by its low solubility and poor stability, restricting its effective absorption and bioavailability. This study introduces a KCZ-loaded microsponge based film coating agent (KCZ-MSF), designed to enhance the transdermal absorption and bioavailability of KCZ. The KCZ-MS was prepared by emulsion solvent evaporation method and the composition of the prescription was optimized by Box-Behnken design (BBD). Moreover, characterization of the optimized KCZ-MS was conducted using scanning electron microscopy (SEM), Fourier-transform infrared spectroscopy (FTIR), and differential scanning calorimetry (DSC). The film coating agent's preparation was further optimized through orthogonal experiments, converting the optimized KCZ-MS into a film coating agent suitable for topical skin application. The KCZ-MS showed a spherical porous structure with a mean particle size of 22.42 ± 8.45 μm, a drug loading efficiency of 20.74 %, entrapment efficiency of 92.12 %, and good compatibility between the drug and excipients. The optimized KCZ-MSF displayed good physical properties. In vitro transdermal experiments revealed that the skin retention of KCZ-MSF surpassed that of commercially available KCZ cream at 6, 12, and 24 h. The pharmacokinetic experiment results indicate that the area under the curve (AUC_0–24) of KCZ-MSF 420.71 ± 21.77 μg/(g·h) is 2.05 times that of KCZ film coating agent (KCZ-F) and 1.29 times that of commercially available ketoconazole cream. Therefore, KCZ-MSF presents a more promising platform for the treatment of superficial skin fungal infections.

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来源期刊

Journal de mycologie medicale 医学-真菌学

CiteScore

5.10

自引率

2.80%

发文量

审稿时长

6-12 weeks

期刊介绍： The Journal de Mycologie Medicale / Journal of Medical Mycology (JMM) publishes in English works dealing with human and animal mycology. The subjects treated are focused in particular on clinical, diagnostic, epidemiological, immunological, medical, pathological, preventive or therapeutic aspects of mycoses. Also covered are basic aspects linked primarily with morphology (electronic and photonic microscopy), physiology, biochemistry, cellular and molecular biology, immunochemistry, genetics, taxonomy or phylogeny of pathogenic or opportunistic fungi and actinomycetes in humans or animals. Studies of natural products showing inhibitory activity against pathogenic fungi cannot be considered without chemical characterization and identification of the compounds responsible for the inhibitory activity. JMM publishes (guest) editorials, original articles, reviews (and minireviews), case reports, technical notes, letters to the editor and information. Only clinical cases with real originality (new species, new clinical present action, new geographical localization, etc.), and fully documented (identification methods, results, etc.), will be considered. Under no circumstances does the journal guarantee publication before the editorial board makes its final decision. The journal is indexed in the main international databases and is accessible worldwide through the ScienceDirect and ClinicalKey platforms.