Abstract
Fenoldopam, a highly selective dopamine receptor agonist, is available in clinics as Corlopam™ i.v. for the management of severe hypertension. Recent reports demonstrate its anti-proliferative activity in vitro in a dose dependent manner. However, stability issues of the drug due to its susceptibility to oxidation, pH sensitivity, poor transdermal flux, and the barrier properties of skin present challenges to develop a topical formulation of fenoldopam. The aim of the present study is to suggest a stable topical formulation of fenoldopam for the treatment of psoriasis. Water washable ointment and glycerin-based carbopol anhydrous gel of fenoldopam intended for topical delivery were prepared and evaluated in vitro and in vivo. Results from pH dependent stability studies suggest the necessity to maintain acidic pH in final formulations. The presence of an acidic adjuster in ointment and unneutralised carbopol dispersion of anhydrous gel maintain the desired acidic environment in the formulations. Stability studies of prepared formulations performed for 90 days indicate that the drug remains stable in formulations. In vivo studies demonstrate the applicability of the formulations for better skin penetration, skin compliance, and photosafety. Efficacy studies using an imiquimod induced psoriasis model confirm the promising application of developed fenoldopam topical formulations for psoriasis.
Original language | English |
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Article number | 118726 |
Journal | International Journal of Pharmaceutics |
Volume | 573 |
DOIs | |
State | Published - 5 Jan 2020 |
Externally published | Yes |
Bibliographical note
Publisher Copyright:© 2019 Elsevier B.V.
Funding
The authors are thankful to Mr. Nagavendra Kommineni for preparation of manuscript. Authors also thankful to Director, NIPER-Hyderabad for providing required facilities, support, and encouragement throughout the project. This work was supported by a grant (FG 002) from YISSUM, The Hebrew University of Jerusalem. The authors are thankful to Mr. Nagavendra Kommineni for preparation of manuscript. Authors also thankful to Director, NIPER-Hyderabad for providing required facilities, support, and encouragement throughout the project. This work was supported by a grant ( FG 002 ) from YISSUM, The Hebrew University of Jerusalem .
Funders | Funder number |
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NIPER-Hyderabad | FG 002 |
YISSUM | |
Hebrew University of Jerusalem |
Keywords
- Fenoldopam
- Imiquimod induced psoriasis model
- Psoriasis
- Skin penetration
- Stability
- Topical delivery