Preparation of topical bimatoprost with enhanced skin infiltration and in vivo hair regrowth efficacy in androgenic alopecia
- Authors
- Subedi, Laxman; Pandey, Prashant; Shim, Jung-Hyun; Kim, Ki-Taek; Cho, Seung-Sik; Koo, Kyo-Tan; Kim, Beum Joon; Park, Jin Woo
- Issue Date
- Dec-2022
- Publisher
- TAYLOR & FRANCIS LTD
- Keywords
- Bimatoprost; prostaglandins; supersaturated topical delivery system; highly skin-permeable; alopecia; hair growth; hair follicles
- Citation
- DRUG DELIVERY, v.29, no.1, pp 328 - 341
- Pages
- 14
- Journal Title
- DRUG DELIVERY
- Volume
- 29
- Number
- 1
- Start Page
- 328
- End Page
- 341
- URI
- https://scholarworks.bwise.kr/cau/handle/2019.sw.cau/54955
- DOI
- 10.1080/10717544.2022.2027046
- ISSN
- 1071-7544
1521-0464
- Abstract
- To prepare a topical formulation of bimatoprost (BIM) with high skin permeability, we designed a solvent mixture system composed of ethanol, diethylene glycol monoethyl ether, cyclomethicone, and butylated hydroxyanisole, serving as a volatile solvent, nonvolatile co-solvent, spreading agent, and antioxidant, respectively. The ideal topical BIM formulation (BIM-TF#5) exhibited 4.60-fold higher human skin flux and a 529% increase in dermal drug deposition compared to BIM in ethanol. In addition, compared to the other formulations, BIM-TF#5 maximally activated human dermal papilla cell proliferation at a concentration of 5 mu M BIM, equivalent to 10 mu M minoxidil. Moreover, BIM-TF#5 (0.3% [w/w] BIM) significantly promoted hair regrowth in the androgenic alopecia mouse model and increased the area covered by hair at 10 days by 585% compared to the vehicle-treated mice, indicating that entire telogen area transitioned into the anagen phase. Furthermore, at day 14, the hair weight of mice treated with BIM-TF#5 (5% [w/w] BIM) was 8.45- and 1.30-fold greater than in the 5% (w/w) BIM in ethanol and 5% (w/v) minoxidil treated groups, respectively. In the histological examination, the number and diameter of hair follicles in the deep subcutis were significantly increased in the BIM-TF#5 (0.3 or 5% [w/w] BIM)-treated mice compared to the mice treated with vehicle or 5% (w/w) BIM in ethanol. Thus, our findings suggest that BIM-TF#5 is an effective formulation to treat scalp alopecia, as part of a novel therapeutic approach involving direct prostamide F2 alpha receptor-mediated stimulation of dermal papilla cells within hair follicles.
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