Purpose

Many current drug delivery technologies are ineffective and require high concentrations of active drugs for effective therapy. Novel drug delivery systems (NDDS) are increasingly being investigated to achieve targeted and controlled drug release. This study uses a microsponge-loaded drug delivery system to overcome the problem associated with traditional therapy for diaper dermatitis. Therefore, we aimed to formulate and characterize luliconazole microsponge-loaded gel for anti-fungal activity.

Methods

Quasi-emulsion solvent diffusion method was used for developing luliconazole microsponge. The characterization of drug-loaded microsponge was investigated. Optimization of formulation carried out through in vitro release studies and entrapment efficacy. The formulation of microsponge-loaded gel was carried out and evaluated using physicochemical studies. The effectiveness of optimized formulations was examined for anti-fungal activity against Candida albicans.

Results

The prepared microsponge was found to have a particle size between 20 and 50 µm, an entrapment efficiency of 53 ± 0.3–92.7 ± 0.1% and a drug release of 71.8 ± 0.2–88.5 ± 0.02%. The pH was in the range of 6.8–7.4, and the viscosity of the prepared formulation was 265.5 cPs. In vitro, the release of luliconazole microsponge-loaded gel showed that formulation F6 has the highest percentage (%) of cumulative drug release (CDR) compared to other formulations. The anti-fungal activity of the microsponge-loaded gel against Candida albicans showed a clear zone of inhibition in the F6 formulation.

Conclusion

Our study results demonstrate that the F6 formulation has the highest % of CDR and shows better anti-fungal activity. Therefore, luliconazole microsponge-loaded gel formulation can improve drug delivery in diaper rash caused by fungal infection.

Graphical Abstract

中文翻译：

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治疗尿布皮炎的卢立康唑微海绵凝胶的配方和表征

目的

目前许多药物输送技术效果不佳，需要高浓度的活性药物才能有效治疗。人们越来越多地研究新型药物递送系统（NDDS），以实现靶向和受控的药物释放。这项研究使用微海绵负载的药物输送系统来克服与传统疗法治疗尿布皮炎相关的问题。因此，我们的目的是配制和表征卢立康唑微海绵凝胶的抗真菌活性。

方法

采用准乳液溶剂扩散法研制卢立康唑微海绵。研究了载药微海绵的表征。通过体外释放研究和包封功效进行配方优化。使用物理化学研究进行微海绵负载凝胶的配制和评估。检查了优化制剂针对白色念珠菌的抗真菌活性的有效性。

结果

制备的微海绵粒径在 20 至 50 µm 之间，包封率为 53 ± 0.3–92.7 ± 0.1%，药物释放率为 71.8 ± 0.2–88.5 ± 0.02%。pH 值范围为 6.8-7.4，所制备制剂的粘度为 265.5 cPs。在体外，卢立康唑微海绵负载凝胶的释放表明，与其他制剂相比，制剂F6具有最高的累积药物释放（CDR）百分比（%）。装载微海绵的凝胶对白色念珠菌的抗真菌活性在 F6 制剂中显示出明显的抑制区。

结论

我们的研究结果表明，F6 制剂具有最高的 CDR 百分比，并显示出更好的抗真菌活性。因此，卢立康唑微海绵凝胶制剂可以改善真菌感染引起的尿布疹的药物递送。

图形概要