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Formulation and evaluation of a novel cubosomal emulgel for topical delivery of luliconazole
Tenside Surfactants Detergents ( IF 1.2 ) Pub Date : 2022-07-14 , DOI: 10.1515/tsd-2022-2442
Anjali Ambalal Purohit 1 , Dikshita Ullas Chavan 1 , Shirleen Miriam Marques 1 , Cleona Elizabeth Mary DCruz 1 , Lalit Kumar 2 , Prashant Jivaji Bhide 1 , Rupesh Kalidas Shirodkar 1
Affiliation  

Despite numerous remarkable developments in clinical therapy, the world remains firmly in the grip of fungal infections. While conventional approaches to antifungal therapy are failing, dermatophytes continue to affect people’s daily lives, especially in humid and tropical areas, and pose a major medical problem. Cubosomes, the liquid crystalline nanostructures, are among the recently developed lipid nanoparticles that could potentially overcome the hurdles of conventional therapy. In the present study, cubosomes containing luliconazole, an antifungal drug, were formulated to overcome the limitation of poor water solubility and poor bioavailability of the drug for the main purpose of treating fungal infections. Various formulations of luliconazole loaded cubosomes were prepared with different ratios of lipid (glyceryl monooleate) and surfactant (poloxamer 407) using emulsification method. The prepared formulations were optimised and the optimised cubosomal dispersion was loaded into a carbomer-934 gel to form an emulsifying gel. All cubosomal dispersions had particle sizes ranging from 124 nm to 221.1 nm, optimal zeta potential and polydispersity index, and were found to be stable. The drug entrapment efficiency of the cubosomes was over 90%. The in vitro diffusion study showed that the developed formulation had a higher release rate than the marketed formulation. The in vitro antifungal activity study confirmed that the prepared emulsion formulation was also effective against Candida albicans. The novel drug delivery system developed in this study, the cubosomal emulgel, could thus be a favourable approach for the topical delivery of luliconazole for the treatment of fungal infections.

中文翻译:

卢立康唑局部给药的新型立方体乳剂的配方和评价

尽管临床治疗取得了许多显着进展,但世界仍牢牢地控制着真菌感染。虽然传统的抗真菌治疗方法失败了,但皮肤癣菌继续影响人们的日常生活,尤其是在潮湿和热带地区,并构成一个重大的医疗问题。立方体,液晶纳米结构,是最近开发的脂质纳米颗粒之一,可能克服常规治疗的障碍。在本研究中,为了克服药物水溶性差和生物利用度差的局限性,制备了含有抗真菌药物卢立康唑的长方体,主要用于治疗真菌感染。使用乳化方法,用不同比例的脂质(单油酸甘油酯)和表面活性剂(泊洛沙姆 407)制备了各种负载卢立康唑的立方体制剂。对制备的配方进行优化,并将优化后的立方分散体加载到 carbomer-934 凝胶中以形成乳化凝胶。所有立方体分散体的粒径范围从 124 nm 到 221.1 nm,具有最佳 zeta 电位和多分散指数,并且被发现是稳定的。立方体的药物包封率超过90%。这 并且被发现是稳定的。立方体的药物包封率超过90%。这 并且被发现是稳定的。立方体的药物包封率超过90%。这体外扩散研究表明,开发的制剂比市售制剂具有更高的释放率。这体外抗真菌活性研究证实,制备的乳剂配方对白色念珠菌. 因此,本研究中开发的新型给药系统,即立方体乳剂,可能是卢立康唑局部给药治疗真菌感染的有利方法。
更新日期:2022-07-14
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