治疗真菌感染的Luliconazole bilosomal gel：开发、优化及抗真菌活性。

IF 3 Q2 PHARMACOLOGY & PHARMACY

Therapeutic delivery Pub Date : 2025-07-03 DOI:10.1080/20415990.2025.2527578

Kartik Aralelimath, Jagannath Sahoo, Sarika Wairkar

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引用次数: 0

摘要

目的：露立康唑是一类具有较高抗真菌活性的咪唑类药物。露立康唑有缺点，如水溶性低，皮肤渗透性差。方法：利用乙醇注射、大豆卵磷脂、胆固醇、Span 60和胆汁盐制备了负载luliconazole的胆小体（LZBSs）。采用23因子设计优化配方。结果：优化后的小泡大小为177.3±0.00 nm，包封效率为90.0±2.5%，zeta电位为-54.8±3.15 mV。透射电镜分析证实了脂质体囊泡的球形，ATR-FTIR结果支持了脂质体的形成，没有任何相互作用。将LZBS装入Carbopol凝胶（LZBS凝胶）中，进行体外和体外释药研究；结果表明，缓释时间为24 h，缓释率分别为90.53±7.89%和84.97±5.58%。抗真菌研究表明，LZBS凝胶对白色念珠菌的抗真菌活性优于市售药物和纯药物。结论：鲁里康唑生物体凝胶具有抗真菌感染的作用。

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Luliconazole bilosomal gel for treating fungal infection: development, optimization and antifungal activity.

Aims: Luliconazole is a class of imidazole that exhibits high antifungal activity. Luliconazole has drawbacks, such as low aqueous solubility and poor skin penetration.

Methods: To overcome these limitations, luliconazole-loaded bilosomes (LZBSs) were developed via ethanol injection, using soy lecithin, cholesterol, Span 60, and bile salt. A 2³ factorial design was employed to optimize the formulation.

Results: The optimized batch of LZBS resulted in a vesicle size of 177.3 ± 0.00 nm with an entrapment efficacy of 90.0 ± 2.5 % and zeta potential of -54.8 ± 3.15 mV. TEM analysis confirmed the spherical shape of bilosome vesicles and ATR-FTIR results supported the formation of bilosomes without any interaction. LZBS was loaded into Carbopol gel (LZBS gel) and evaluated for in vitro and ex vivo drug release study; results showed extended release of 90.53 ± 7.89 % and 84.97 ± 5.58 %, respectively, up to 24 h. Antifungal study for LZBS gel demonstrated superior activity against Candida albicans as compared to marketed and pure drug.

Conclusion: Thus, luliconazole-loaded bilosome gel proved to be effective against fungal infections.

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来源期刊

Therapeutic delivery PHARMACOLOGY & PHARMACY-

CiteScore

5.50

自引率

0.00%

发文量

期刊介绍： Delivering therapeutics in a way that is right for the patient - safe, painless, reliable, targeted, efficient and cost effective - is the fundamental aim of scientists working in this area. Correspondingly, this evolving field has already yielded a diversity of delivery methods, including injectors, controlled release formulations, drug eluting implants and transdermal patches. Rapid technological advances and the desire to improve the efficacy and safety profile of existing medications by specific targeting to the site of action, combined with the drive to improve patient compliance, continue to fuel rapid research progress. Furthermore, the emergence of cell-based therapeutics and biopharmaceuticals such as proteins, peptides and nucleotides presents scientists with new and exciting challenges for the application of therapeutic delivery science and technology. Successful delivery strategies increasingly rely upon collaboration across a diversity of fields, including biology, chemistry, pharmacology, nanotechnology, physiology, materials science and engineering. Therapeutic Delivery recognizes the importance of this diverse research platform and encourages the publication of articles that reflect the highly interdisciplinary nature of the field. In a highly competitive industry, Therapeutic Delivery provides the busy researcher with a forum for the rapid publication of original research and critical reviews of all the latest relevant and significant developments, and focuses on how the technological, pharmacological, clinical and physiological aspects come together to successfully deliver modern therapeutics to patients. The journal delivers this essential information in concise, at-a-glance article formats that are readily accessible to the full spectrum of therapeutic delivery researchers.