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Preparation of Terbinafin-Encapsulated Solid Lipid Nanoparticles Containing Antifungal Carbopol® Hydrogel with Improved Efficacy: In Vitro, Ex Vivo and In Vivo Study.
Rarokar, Nilesh R; Menghani, Sunil S; Kerzare, Deweshri R; Khedekar, Pramod B; Bharne, Ashish P; Alamri, Abdulhakeem S; Alsanie, Walaa F; Alhomrani, Majid; Sreeharsha, Nagaraja; Asdaq, Syed Mohammed Basheeruddin.
Affiliation
  • Rarokar NR; Computer Aided Drug Design Laboratory, Department of Pharmaceutical Sciences, Mahatma Jyotiba Fuley Shaikshanik Parisar, Rashtrasant Tukadoji Maharaj Nagpur University, Amravati Road, Nagpur 440033, India.
  • Menghani SS; Department of Pharmaceutical Chemistry, Krupanidhi College of Pharmacy, Bangalore 560035, India.
  • Kerzare DR; Department of Pharmaceutical Chemistry, Dadasaheb Balpande College of Pharmacy, Nagpur 440037, India.
  • Khedekar PB; Computer Aided Drug Design Laboratory, Department of Pharmaceutical Sciences, Mahatma Jyotiba Fuley Shaikshanik Parisar, Rashtrasant Tukadoji Maharaj Nagpur University, Amravati Road, Nagpur 440033, India.
  • Bharne AP; Computer Aided Drug Design Laboratory, Department of Pharmaceutical Sciences, Mahatma Jyotiba Fuley Shaikshanik Parisar, Rashtrasant Tukadoji Maharaj Nagpur University, Amravati Road, Nagpur 440033, India.
  • Alamri AS; Department of Clinical Laboratory Sciences, The Faculty of Applied Medical Sciences, Taif University, Taif 21944, Saudi Arabia.
  • Alsanie WF; Centre of Biomedical Sciences Research (CBSR), Deanship of Scientific Research, Taif University, Taif 21944, Saudi Arabia.
  • Alhomrani M; Department of Clinical Laboratory Sciences, The Faculty of Applied Medical Sciences, Taif University, Taif 21944, Saudi Arabia.
  • Sreeharsha N; Centre of Biomedical Sciences Research (CBSR), Deanship of Scientific Research, Taif University, Taif 21944, Saudi Arabia.
  • Asdaq SMB; Department of Clinical Laboratory Sciences, The Faculty of Applied Medical Sciences, Taif University, Taif 21944, Saudi Arabia.
Pharmaceutics ; 14(7)2022 Jun 30.
Article in En | MEDLINE | ID: mdl-35890289
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.
Key words

Full text: 1 Collection: 01-internacional Database: MEDLINE Language: En Journal: Pharmaceutics Year: 2022 Document type: Article Affiliation country: India Country of publication: Switzerland

Full text: 1 Collection: 01-internacional Database: MEDLINE Language: En Journal: Pharmaceutics Year: 2022 Document type: Article Affiliation country: India Country of publication: Switzerland