Preparation of Terbinafin-Encapsulated Solid Lipid Nanoparticles Containing Antifungal Carbopol<sup>®</sup> Hydrogel with Improved Efficacy: In Vitro, Ex Vivo and In Vivo Study
Nilesh R. Rarokar,
Sunil S. Menghani,
Deweshri R. Kerzare,
Pramod B. Khedekar,
Ashish P. Bharne,
Abdulhakeem S. Alamri,
Walaa F. Alsanie,
Majid Alhomrani,
Nagaraja Sreeharsha,
Syed Mohammed Basheeruddin Asdaq
Affiliations
Nilesh R. Rarokar
Computer Aided Drug Design Laboratory, Department of Pharmaceutical Sciences, Mahatma Jyotiba Fuley Shaikshanik Parisar, Rashtrasant Tukadoji Maharaj Nagpur University, Amravati Road, Nagpur 440033, India
Sunil S. Menghani
Department of Pharmaceutical Chemistry, Krupanidhi College of Pharmacy, Bangalore 560035, India
Deweshri R. Kerzare
Department of Pharmaceutical Chemistry, Dadasaheb Balpande College of Pharmacy, Nagpur 440037, India
Pramod B. Khedekar
Computer Aided Drug Design Laboratory, Department of Pharmaceutical Sciences, Mahatma Jyotiba Fuley Shaikshanik Parisar, Rashtrasant Tukadoji Maharaj Nagpur University, Amravati Road, Nagpur 440033, India
Ashish P. Bharne
Computer Aided Drug Design Laboratory, Department of Pharmaceutical Sciences, Mahatma Jyotiba Fuley Shaikshanik Parisar, Rashtrasant Tukadoji Maharaj Nagpur University, Amravati Road, Nagpur 440033, India
Abdulhakeem S. Alamri
Department of Clinical Laboratory Sciences, The Faculty of Applied Medical Sciences, Taif University, Taif 21944, Saudi Arabia
Walaa F. Alsanie
Department of Clinical Laboratory Sciences, The Faculty of Applied Medical Sciences, Taif University, Taif 21944, Saudi Arabia
Majid Alhomrani
Department of Clinical Laboratory Sciences, The Faculty of Applied Medical Sciences, Taif University, Taif 21944, Saudi Arabia
Nagaraja Sreeharsha
Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi Arabia
Syed Mohammed Basheeruddin Asdaq
Department of Pharmacy Practice, College of Pharmacy, AlMaarefa University, Dariyah, Riyadh 13713, Saudi Arabia
The present research was aimed to develop a terbinafin hydrochloride (TH)-encapsulated solid lipid nanoparticles (SLNs) hydrogel for improved antifungal efficacy. TH-loaded SLNs were obtained from glyceryl monostearate (lipid) and Pluronic® F68 (surfactant) employing high-pressure homogenization. The ratio of drug with respect to lipid was optimized, considering factors such as desired particle size and highest percent encapsulation efficiency. Lyophilized SLNs were then incorporated in the hydrogel prepared from 0.2–1.0% w/v carbopol 934P and further evaluated for rheological parameters. The z-average, zeta potential and polydispersity index were found to be 241.3 nm, −15.2 mV and 0.415, respectively. The SLNs show a higher entrapment efficiency of about 98.36%, with 2.12 to 6.3602% drug loading. SEM images, XRD and the results of the DSC, FTIR show successful preparation of SLNs after freeze drying. The TH-loaded SLNs hydrogel showed sustained drug release (95.47 ± 1.45%) over a period of 24 h. The results reported in this study show a significant effect on the zone of inhibition than the marketed formulation and pure drug in Candida albicans cultures, with better physical stability at cooler temperatures. It helped to enhance skin deposition inthe ex vivostudy and improved, in vitro and in vivo, the antifungal activity.
