Evaluation of topical econazole nitrate formulations with potential for treating Raynaud's phenomenon.
Pharm Dev Technol
; 24(6): 689-699, 2019 Jul.
Article
in En
| MEDLINE
| ID: mdl-30712434
ABSTRACT
The purpose of this work was to design and characterize a topical formulation of econazole nitrate (EN) with potential for treating Raynaud's phenomenon (RP). Four topical dosage forms (F1_topical solution, F2_HPMC or hydroxypropyl methylcellulose dispersion, F3_VersaBase® cream, and F4_Lipoderm® Activemax™ Cream) containing 3% w/w EN were prepared and characterized for drug content, pH, viscosity, spreadability, drug crystallinity, stability, and in vitro permeation using Franz cells across pig ear skin, and results were compared to the 1% marketed EN cream. All four formulations had acceptable physical and visual characteristics required for topical application, with 3% w/w EN. The order of amount of drug permeated from highest to lowest was F2 (10.27%) > F4 (2.47%) > F1 (2.28%) > F3 (1.47%) > marketed formulation (0.22%). Formulation F2 showed better penetration of the drug into the stratum corneum, epidermis, and dermis layers. The drug concentration in the stratum corneum and epidermis was approximately 10-20 times higher with F2 compared to the marketed formulation. All formulations were found to be stable for up to 6 months. All four EN formulations were found to be better than the 1% marketed cream. Formulation F2_HPMC dispersion could be further explored as a treatment option for RP.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Raynaud Disease
/
Pharmaceutical Vehicles
/
Econazole
/
14-alpha Demethylase Inhibitors
/
Antifungal Agents
Limits:
Animals
/
Humans
Language:
En
Journal:
Pharm Dev Technol
Journal subject:
FARMACIA
Year:
2019
Document type:
Article
Affiliation country: