Fabrication and Evaluation of Luliconazole Loaded Leciplex against Candidiasis

Gaurirani Anil Telang, A. A. Monde, K. S. Ashtekar, U. Bagul
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Abstract

Background: Fungal infections pose a significant public health concern due to the extended duration of treatment needed and the frequent reoccurrence of the disease. Objectives: This study was aimed to enhance the permeability of luliconazole with sustain release for prolonged period for the effective treatment of fungal infection by incorporating it into lipid based nanocarrier system. Methods: Luliconazole loaded leciplex were prepared by one step fabrication method using phospholipid, Dimethyldidodecyl ammonium bromide and transcutol P. The prepared leciplex were optimized by using Box Behnken statistical design. Furthermore, luliconazole loaded leciplex were incorporated into carbopol gel system and evaluated for various parameters. Results: The luliconazole loaded leciplex showed high entrapment efficiency (98.8% ± 1.2) and size were recorded around 428.11 nm with a polydispersity index value of 0.35 ± 0.12, along with zeta potential of +26.30 mV.  The Transmission Electron Microscopy studies revealed the spherical morphology of the leciplex. The developed leciplex gel was evaluated for its pH, viscosity, spreadability, hardness and adhesiveness. Furthermore, in vitro and ex vivo release kinetics demonstrated the sustained drug release pattern. Moreover, histopathology studies conducted on the rat skin revealed that the prepared formulation was non - irritant and non – toxic. The antifungal assay of developed formulations (containing only 0.3 % w/v luliconazole) showed significantly greater antifungal activity against Candida albicans as compared to marketed formulation (containing 1 % w/v luliconazole). Conclusion: By taking all the results in to account it can be concluded that luliconazole loaded leciplex formulation is simple to prepare and showed excellent activity in against Candida albicans.
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制备和评估抗念珠菌病的卢利康唑载体 Leciplex
背景:真菌感染是一个重大的公共卫生问题,因为它需要长时间的治疗,而且经常复发。研究目的本研究旨在通过在脂质纳米载体系统中加入氟硅唑,增强其渗透性并延长其持续释放时间,从而有效治疗真菌感染。研究方法使用磷脂、二甲基十二烷基溴化铵和 Transcutol P,通过一步制备法制备出含卢利康唑的复合物。此外,还将含氟硅唑的leciplex加入到carbopol凝胶系统中,并对各种参数进行了评估。结果:装载了氟环唑的leciplex显示出较高的包埋效率(98.8% ± 1.2),尺寸约为428.11 nm,多分散指数值为0.35 ± 0.12,zeta电位为+26.30 mV。 透射电子显微镜研究显示,leciplex 呈球形。对所开发的乐可复凝胶的 pH 值、粘度、铺展性、硬度和粘附性进行了评估。此外,体外和体内释放动力学研究也证明了这种药物的持续释放模式。此外,对大鼠皮肤进行的组织病理学研究表明,制备的配方无刺激性和毒性。与市场上销售的制剂(含 1 % w/v 卢立康唑)相比,所开发制剂(仅含 0.3 % w/v 卢立康唑)的抗真菌测定显示出更强的抗白色念珠菌活性。结论综合考虑所有结果,可以得出结论:含有氟硅唑的复方制剂制备简单,对白色念珠菌具有出色的抗真菌活性。
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