Hamed Hamishehkar1, Javad Shokri2, Shahoo Fallahi3, Azin Jahangiri4, Saeed Ghanbarzadeh4, Maryam Kouhsoltani5. 1. a Drug Applied Research Center . 2. b Dermatology & Dermopharmacy Research Team and Faculty of Pharmacy . 3. c Biotechnology Research Center . 4. d Students' Research Committee and Faculty of Pharmacy , and. 5. e Research Center for Pharmaceutical Nanotechnology and Faculty of Dentistry, Tabriz University of Medical Sciences , Tabriz , Iran.
Abstract
CONTEXT: Cellulite refers to dimpled appearance of the skin, usually located in the thighs and buttocks regions of most adult women. OBJECTIVE: The aim of this study was to formulate topically used caffeine-loaded solid lipid nanoparticle (SLN) for the treatment of cellulite. METHODS: SLNs were prepared by hot homogenization technique using Precirol® as lipid phase. The physical characterization and stability studies of SLNs as well as in vitro skin permeation and histological studies in rat skin were conducted. RESULTS: The mean particle size, encapsulation efficiency and loading efficiency percentages for optimized SLN formulation were 94 nm, 86 and 28%, respectively. In vitro drug release demonstrated that caffeine-loaded SLN incorporated into carbopol made hydrogel (caffeine-SLN-hydrogel) exhibited a sustained drug release compared to the caffeine hydrogel over 24 h. Caffeine-loaded SLNs showed a good stability during 12 months of storage at room temperature. The DSC and XRD results showed that caffeine was dispersed in SLN in an amorphous state. In vitro permeation studies illustrated higher drug accumulation in the skin with caffeine-SLN-hydrogel compared to caffeine hydrogel. The flux value of caffeine through rat skin in caffeine-SLN-hydrogel was 3.3 times less than caffeine hydrogel, representing lower systemic absorption. In contrast with caffeine hydrogel, the histological studies showed the complete lysis of adipocytes by administration of caffeine-SLN-hydrogel in the deeper skin layers. CONCLUSION: Results of this study indicated that SLNs are promising carrier for improvement of caffeine efficiency in the treatment of cellulite following topical application on the skin.
CONTEXT: Cellulite refers to dimpled appearance of the skin, usually located in the thighs and buttocks regions of most adult women. OBJECTIVE: The aim of this study was to formulate topically used caffeine-loaded solid lipid nanoparticle (SLN) for the treatment of cellulite. METHODS: SLNs were prepared by hot homogenization technique using Precirol® as lipid phase. The physical characterization and stability studies of SLNs as well as in vitro skin permeation and histological studies in rat skin were conducted. RESULTS: The mean particle size, encapsulation efficiency and loading efficiency percentages for optimized SLN formulation were 94 nm, 86 and 28%, respectively. In vitro drug release demonstrated that caffeine-loaded SLN incorporated into carbopol made hydrogel (caffeine-SLN-hydrogel) exhibited a sustained drug release compared to the caffeine hydrogel over 24 h. Caffeine-loaded SLNs showed a good stability during 12 months of storage at room temperature. The DSC and XRD results showed that caffeine was dispersed in SLN in an amorphous state. In vitro permeation studies illustrated higher drug accumulation in the skin with caffeine-SLN-hydrogel compared to caffeine hydrogel. The flux value of caffeine through rat skin in caffeine-SLN-hydrogel was 3.3 times less than caffeine hydrogel, representing lower systemic absorption. In contrast with caffeine hydrogel, the histological studies showed the complete lysis of adipocytes by administration of caffeine-SLN-hydrogel in the deeper skin layers. CONCLUSION: Results of this study indicated that SLNs are promising carrier for improvement of caffeine efficiency in the treatment of cellulite following topical application on the skin.