Prasanthi D.*, Deepthi P.
G. Pulla Reddy College of Pharmacy, Mehdipatnam, Hyderabad, Telangana-500028, India
*Corresponding author:
Dr. D. Prasanthi, Associate Professor,
Department of Pharmaceutics,
G. Pulla Reddy College of Pharmacy, Mehdipatnam, Hyderabad, Telangana-500028, India.
Abstract
Objective: The objective is to study the effect of different terpenes on permeation and optimize the better terpene for transdermal itraconazole hydrogel in onychomycosis treatment. Materials and methods: Itraconazole hydrogels were prepared by dispersion method using synthetic polymer (Acrypol 974 and Acrypol 980) as gelling agents. Terpenes nerolidol, limonene, geraniol, carvone at 2.5% and 5% were used. The prepared gels were evaluated for pH, drug content, spreadability, viscosity, in-vitro studies, ex-vivo studies, skin irritation studies and stability studies. Results: The solubility of itraconazole (0.04±0.21mg/ml) was found to be highest with nerolidol (5%) in combination with DMSO (3%) and propylene glycol (1%) in water (5.99±1.5mg/ml). All the formulations have shown good physicochemical properties. In in-vitro diffusion studies through dialysis membrane the trend of release was following the order nerolidol>carvone>geraniol>limonene. Ex-vivo permeation studies of F5 and F13 have shown flux of 28.68±2.3µg/cm2/hr and 31.41±1.67µg/cm2/hr respectively, permeability coefficient of 585cm/hr×10ˉ³ and 641cm/hr×10ˉ³respectively, enhancement ratio of 12.97 and 14.21 respectively, in comparison to pure drug flux of 2.21±0.2 µg/cm2/hr. Skin irritation studies have shown to be non-irritant. FTIR compatibility studies indicate drug and excipients were compatible. The optimized formulation F13 was stable for one month at room temperature. Conclusion: Based on these results, it can be concluded that small alcoholic, liquid terpene with high degree of unsaturation and high lipophilicity (Nerolidol) can provide good permeation of itraconazole.
Keywords: Itraconazole, Acrypol 974, Acrypol 980, Onychomycosis, Terpenes
