离体
渗透
体内
Zeta电位
脂质体
纳米载体
药理学
药物输送
白色念珠菌
药品
人体皮肤
化学
体外
材料科学
色谱法
膜
医学
纳米技术
微生物学
纳米颗粒
生物
生物化学
生物技术
遗传学
作者
Manjot Kaur,Kanwardeep Singh,Subheet Kumar Jain
标识
DOI:10.1080/08982104.2019.1682602
摘要
Luliconazole is a new drug candidate for treatment of topical fungal infections. Its present therapy is associated with limitations of very poor and slow skin permeation, leading to required long term repeated administration for complete cure of disease. Lipid nanocarriers based elastic lipogel and ethogel formulations were developed in strength of 1% w/w and extensively characterized in vitro, ex-vivo, and in vivo and compared for their results to the marketed formulation. The prepared formulations were found to have ideal pH, nanometric vesicle size, encapsulation efficiency (92.7% and 91.2%), zeta potential (−17.0 and −32.8 mV), and viscosity (6.6 and 7.8 Pa.s) with no signs of instability on storage. In vitro activity against Candida albicans and dermatophytes demonstrated the prepared formulations to be 3 and 2.5 times more potent than marketed formulation, respectively. Ex vivo skin permeation and deposition studies, performed on various biological membranes and a synthetic membrane, manifest that Strat-M membrane resembles closest to the human skin followed by porcine ear skin, rat, and mice skin. Enhanced skin deposition of elastic lipogel and ethogel as compared to conventional marketed cream is also confirmed by SEM and CLSM analysis of the treated skin. In vivo antifungal activity on albino rats demonstrated vesicle based gel formulations to be safe, non irritant and more effective in topical treatment of fungal infections, with no drug reaching to systemic circulation. Thus, findings of the study demonstrate elastic liposomes and ethosomes, as a carrier are an attractive approach for enhanced topical delivery of Luliconazole.
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