关键词: antifungal drug electrospinning luliconazole nanofiber patch topical delivery

Mesh : Antifungal Agents / administration & dosage pharmacology chemistry Nanofibers / chemistry Candida albicans / drug effects Aspergillus niger / drug effects Drug Liberation Drug Delivery Systems / methods Imidazoles / chemistry administration & dosage pharmacology Delayed-Action Preparations Microbial Sensitivity Tests / methods Drug Carriers / chemistry Drug Stability

来  源:   DOI:10.1208/s12249-024-02815-9

Abstract:
This study introduces and assesses the potential of a Luliconazole-loaded nanofiber (LUL-NF) patch, fabricated through electrospinning, for enhancing topical drug delivery. The primary objectives involve evaluating the nanofiber structure, characterizing physical properties, determining drug loading and release kinetics, assessing antifungal efficacy, and establishing the long-term stability of the NF patch. LUL-NF patches were fabricated via electrospinning and observed by SEM at approximately 200 nm dimensions. The comprehensive analysis included physical properties (thickness, folding endurance, swelling ratio, weight, moisture content, and drug loading) and UV analysis for drug quantification. In vitro studies explored sustained drug release kinetics, while microbiological assays evaluated antifungal efficacy against Candida albicans and Aspergillus Niger. Stability studies confirmed long-term viability. Comparative analysis with the pure drug, placebo NF patch, LUL-NF patch, and Lulifod gel was conducted using agar diffusion, revealing enhanced performance of the LUL-NF patch. SEM analysis revealed well-defined LUL-NF patches (0.80 mm thickness) with exceptional folding endurance (> 200 folds) and a favorable swelling ratio (12.66 ± 0.73%). The patches exhibited low moisture uptake (3.4 ± 0.09%) and a moisture content of 11.78 ± 0.54%. Drug loading in 1 cm2 section was 1.904 ± 0.086 mg, showing uniform distribution and sustained release kinetics in vitro. The LUL-NF patch demonstrated potent antifungal activity. Stability studies affirmed long-term stability, and comparative analysis highlighted increased inhibition compared to a pure drug, LUL-NF patch, and a commercial gel. The electrospun LUL-NF patch enhances topical drug delivery, promising extended therapy through single-release, one-time application, and innovative drug delivery strategies, supported by thorough analysis.
摘要:
这项研究介绍并评估了装载卢立康唑的纳米纤维(LUL-NF)贴片的潜力,通过静电纺丝制造,用于增强局部药物递送。主要目标包括评估纳米纤维结构,表征物理性质,确定药物负载和释放动力学,评估抗真菌功效,并树立了NF贴剂的历久稳固性。通过静电纺丝制造LUL-NF贴片,并通过SEM在约200nm的尺寸下观察。综合分析包括物理性能(厚度,折叠耐力,溶胀率,体重,水分含量,和载药量)和用于药物定量的UV分析。体外研究探索了持续药物释放动力学,而微生物学试验评估了对白色念珠菌和黑曲霉的抗真菌功效。稳定性研究证实了长期生存能力。与纯药物的比较分析,安慰剂NF贴片,LUL-NF补丁,使用琼脂扩散进行Lulifod凝胶,揭示了LUL-NF补丁的增强性能。SEM分析显示良好定义的LUL-NF贴片(0.80mm厚度)具有优异的耐折性(>200倍)和有利的溶胀率(12.66±0.73%)。贴剂表现出低的水分吸收(3.4±0.09%)和11.78±0.54%的水分含量。1cm2切片的载药量为1.904±0.086mg,在体外表现出均匀分布和缓释动力学。LUL-NF贴片显示出有效的抗真菌活性。稳定性研究证实了长期稳定性,和比较分析强调了与纯药物相比抑制增加,LUL-NF补丁,和商业凝胶。电纺LUL-NF贴片增强局部药物递送,通过单次释放有希望的延长治疗,一次性申请,和创新的药物输送策略,在全面分析的支持下。
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