Hamed Hamishehkar1, Saeed Ghanbarzadeh1,2, Sasan Sepehran3, Yousef Javadzadeh4, Zahra Mardhiah Adib5, Maryam Kouhsoltani6. 1. a Drug Applied Research Center, Tabriz University of Medical Sciences , Tabriz , Iran . 2. b Department of Pharmaceutics , Faculty of Pharmacy, Zanjan University of Medical Sciences , Zanjan , Iran . 3. c Biotechnology Research Center, Tabriz University of Medical Sciences , Tabriz , Iran . 4. d Dermatology & Dermopharmacy Research Team and Faculty of Pharmacy, Tabriz University of Medical Sciences , Tabriz , Iran . 5. e Students' Research Committee, Tabriz University of Medical Sciences , Tabriz , Iran , and. 6. f Research Center for Pharmaceutical Nanotechnology and Faculty of Dentistry, Tabriz University of Medical Sciences , Tabriz , Iran.
Abstract
CONTEXT: Flutamide is a potent anti-androgen with the several unwanted side effects in systemic administration, therefore, it has attracted special interest in the development of topically applied formulations for the treatment of androgenic alopecia. OBJECTIVE: The purpose of this study was to prepare and characterize the solid lipid nanoparticles (SLNs) of Flutamide for follicular targeting in the treatment of the androgenic alopecia. METHODS: Flutamide-loaded SLNs, promising drug carriers for topical application were prepared by hot melt homogenization method. Drug permeation and accumulation in the exercised rat skin and histological study on the male hamsters were performed to assess drug delivery efficiency in vitro and in vivo, respectively. RESULTS: The optimized Flutamide-loaded SLNs (size 198 nm, encapsulation efficiency percentage 65% and loading efficiency percentage 3.27%) exhibited a good stability during the period of at least 2 months. The results of X-ray diffraction showed Flutamide amorphous state confirming uniform drug dispersion in the SLNs structure. Higher skin drug deposition (1.75 times) of SLN formulation compared to Flutamide hydroalcoholic solution represented better localization of the drug in the skin. The in vivo studies showed more new hair follicle growth by utilizing Flutamide-loaded SLNs than Flutamide hydroalcoholic solution which could be due to the higher accumulation of SLNs in the hair follicles as well as slowly and continues release of the Flutamide through the SLNs maximizing hair follicle exposure by antiandrogenic drug. CONCLUSION: It was concluded Flutamide-loaded SLN formulation can be used as a promising colloidal drug carriers for topical administration of Flutamide in the treatment of androgenic alopecia.
CONTEXT: Flutamide is a potent anti-androgen with the several unwanted side effects in systemic administration, therefore, it has attracted special interest in the development of topically applied formulations for the treatment of androgenic alopecia. OBJECTIVE: The purpose of this study was to prepare and characterize the solid lipid nanoparticles (SLNs) of Flutamide for follicular targeting in the treatment of the androgenic alopecia. METHODS:Flutamide-loaded SLNs, promising drug carriers for topical application were prepared by hot melt homogenization method. Drug permeation and accumulation in the exercised rat skin and histological study on the male hamsters were performed to assess drug delivery efficiency in vitro and in vivo, respectively. RESULTS: The optimized Flutamide-loaded SLNs (size 198 nm, encapsulation efficiency percentage 65% and loading efficiency percentage 3.27%) exhibited a good stability during the period of at least 2 months. The results of X-ray diffraction showed Flutamide amorphous state confirming uniform drug dispersion in the SLNs structure. Higher skin drug deposition (1.75 times) of SLN formulation compared to Flutamide hydroalcoholic solution represented better localization of the drug in the skin. The in vivo studies showed more new hair follicle growth by utilizing Flutamide-loaded SLNs than Flutamide hydroalcoholic solution which could be due to the higher accumulation of SLNs in the hair follicles as well as slowly and continues release of the Flutamide through the SLNs maximizing hair follicle exposure by antiandrogenic drug. CONCLUSION: It was concluded Flutamide-loaded SLN formulation can be used as a promising colloidal drug carriers for topical administration of Flutamide in the treatment of androgenic alopecia.
Entities:
Keywords:
Androgenic alopecia; Flutamide; solid lipid nanoparticle; transdermal drug delivery
Authors: Won Young Jang; Dong Seon Kim; Sang Hee Park; Ji Hye Yoon; Chae Yun Shin; Lei Huang; Ket Nang; Masphal Kry; Hye-Woo Byun; Byoung-Hee Lee; Sarah Lee; Jongsung Lee; Jae Youl Cho Journal: Molecules Date: 2022-06-24 Impact factor: 4.927