Purpose

Solid lipid nanoparticles (SLNs) have shown tremendous utility in the topical delivery of such anti-fungal moieties. Hence, it was aimed to develop luliconazole (LCZ)-loaded SLN-based topical nanogel for improvised efficacy against topical fungal infections.

Methods

Response surface methodology–based experimental design, i.e., BBD, was employed to prepare LCZ-SLNs by solvent diffusion method. The SLNs were characterized based on particle size, entrapment efficiency, polydispersity index, zeta potential, and morphological investigations by SEM and transformed into gel form using pH-triggered gelling mechanism. After characterization, pH, viscosity, and texture profile, the developed gel’s ex vivo drug release profiles were investigated, followed by ex vivo permeation studies and dermal retention studies. The developed gel was evaluated in vitro for its antifungal potential against Candida albicans and Sporotheix schenckii, safety, and long-term storage stability.

Results

The results showed the development of spherical shape colloidal nanosize particles (111.33 nm) with no aggregation. The drug entrapment efficiency was 63.65%, and the zeta potential was obtained to be 23.33 ± 2.5 mV, presenting good stability. LCZ showed prolonged in vitro release from SLNs dispersion and gel. In vitro anti-fungal investigation portrayed a significant reduction in the growth inhibition zone (p < .05) compared to the control group. The findings of the study suggest that the developed LCZ-loaded SLN topical gels are safe to use and have long storage stability.

Conclusion

In conclusion, SLNs with optimum particle size, high entrapment efficiency, and modified drug release patterns can offer a promising carrier for the topical delivery of luliconazole-like molecules.

中文翻译：

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QbD 驱动的基于固体脂质纳米颗粒 (SLN) 的卢立康唑纳米凝胶的开发和表征，用于有效管理皮肤真菌感染

目的

固体脂质纳米粒子（SLN）在局部递送此类抗真菌部分方面显示出巨大的效用。因此，我们的目标是开发负载卢立康唑 (LCZ) 的基于 SLN 的局部纳米凝胶，以提高对抗局部真菌感染的功效。

方法

采用基于响应面法的实验设计，即BBD，通过溶剂扩散法制备LCZ-SLN。根据粒径、包封效率、多分散指数、zeta 电位和 SEM 形态学研究对 SLN 进行表征，并使用 pH 触发的胶凝机制将其转化为凝胶形式。在表征、pH、粘度和质地特征之后，研究了开发的凝胶的离体药物释放特征，随后进行了离体渗透研究和皮肤保留研究。开发的凝胶在体外评估了其针对白色念珠菌和申克孢子丝的抗真菌潜力、安全性和长期储存稳定性。

结果

结果显示，形成了球形胶体纳米尺寸颗粒（111.33 nm），没有聚集。药物包封率为63.65%，zeta电位为23.33±2.5 mV，稳定性良好。 LCZ 在体外从 SLN 分散体和凝胶中释放出较长的时间。体外抗真菌研究表明， 与对照组相比，生长抑制区显着减少 ( p < .05)。研究结果表明，所开发的负载 LCZ 的 SLN 外用凝胶使用安全且具有长期储存稳定性。

结论

总之，具有最佳粒径、高包封效率和改进的药物释放模式的 SLN 可以为卢立康唑类分子的局部递送提供有前途的载体。