Pharmacodynamic Studies of Lercanidipine hydrochloride Transdermal Therapeutic Systems
Journal Title: Indo American Journal of Pharmaceutical Research - Year 2012, Vol 2, Issue 4
Abstract
This article reports the assessment of lercanidipine hydrochloride (LH) for transdermal delivery. In-vitro permeation studies were carried out across the porcine ear skin in presence of various penetration enhancers. Pharmaceutical excipients and chemicals namely dimethyl sulfoxide (DMSO), isopropyl myristate (IPM), sodium lauryl sulphate (SLS), eugenol, citral, hyaluronidase were facilitated to evaluate as effective penetration enhancer. Among all, hyaluronidase emerged as effective penetration enhancer with highest flux 111.8±0.030 μg/cm2/hr, Kp 0.0172±0.040 cm/hr and enhancement ratio 5.37±0.01 than others. Later, LH (10 mg/3.14 cm2) transdermal patches (designated as EL formulations) were prepared by using EC and PVP K-30 as polymers in 1:2 ratio incorporating optimized hyaluronidase (5% w/w) as penetration enhancer, n - dibutyl phthalate (30% w/w) as a plasticizer. The ex-vivo permeation studies of EL formulations exhibited satisfactory cumulative percent of drug permeation, transdermal flux, permeability coefficient and diffusion coefficient. The curve fitment data indicated that the in-vitro permeation data of model formulations fitted well into zero order equation (average R2=0.9713 to 0.9866) better than first order and Higuchi model. The pharmacodynamic studies were carried out employing rat tail cuff method in albino rats. Hypertension was successfully induced by methyl prednisolone acetate (MPA) (40 mg/kg) subcutaneously for 2 weeks. The fabricated EL transdermal patches were significantly decreased the blood pressure (BP) in close to normal values for 24 hours. Furthermore, the satisfactory results were supported by one way ANOVA.
Authors and Affiliations
Subhash P. G. , Dinesh B. M. , Ravikumar M.
Keywords
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