Fabrication of Transdermal Matrix Patch of Lercanidipine Hydrochloride Using Natural Polymer and Essential Oil

Abstract

The goal of the present research work was to develop and characterize a transdermal matrix patch of Lercanidipine hydrochloride (L.H.) for controlled drug delivery using the solvent evaporation method. To achieve controlled drug release, polymers such as Psyllium and HPMC K15M were optimized. Moreover, the skin permeation effect of essential oils such as linseed oil, jojoba oil, and pumpkin seed oil was investigated on Wistar rat skin. A 32 full factorial design was applied to optimize two formulation variables: concentration of essential oil as a permeation enhancer and polymer fixed-weight ratio. To study drug-excipients incompatibility, Fourier Transform Infrared Spectroscopy (FTIR) had employed, which showed the absence of chemical interaction. All formulations were evaluated for Physico-chemical parameters, ex-vivo drug release study, an in-vivo skin-irritation study on Wistar rats, and stability study. Developed matrix patch showed optimum Physico-chemical properties with the absence of skin irritation. An Ex-vivo drug release study revealed that both formulation variables show an effect on drug release from matrix patches. The effectiveness of the oils as the permeation enhancer was found to be in the following descending order: Pumpkin seed oil > Linseed oil > Jojoba oil. Therefore, pumpkin seed oil was selected as a permeation enhancer in the final Formulation that shows the highest flux (164.09±1.49 µg/cm2/h) and desired drug release for transdermal administration. Stability study shows that the patch was stable up to 6 months at 40±2 ˚C and 75±5 % R.H. and 30±2 ˚C and 65±5 % R.H. The present investigation demonstrates that the prepared matrix patch can deliver therapeutically effective controlled release dose of lercanidipine hydrochloride (L.H.) via transdermal route using pumpkin seed oil as the permeation enhancer.