Abstract

DEVELOPMENT OF PROTRANSFERSOMAL SYSTEM FOR EFFECTIVE TRANSDERMAL DELIVERY OF NIFEDIPINE

Rajesh Kumar, *Murugesan Senthil Kumar

ABSTRACT

The purpose of the current study was to investigate the feasibility of new vesicular drug carrier system Protransfersome gel (PTG) as transdermal drug delivery system for Nifedipine. PTG formulations of Nifedipine were prepared by coacervation phase separation method and characterized for vesicle shape, size, entrapment efficiency, turbidity, and drug permeation across rat skin and were evaluated for their stability and bioavailability. For optimization of PTG, different formulations (PTG-1 to PTG-12) were prepared using the various quantity of drug, alcohol and varying the ratio of polymer and surfactant. The maximum entrapment efficiency (97.9 ± 0.35%) and optimum vesicles size (597 ± 4.0 nm) have been attained by optimizing the amount of surfactant (4 mg), alcohol (100 μl), and PC : S ratio (85 :15). The skin permeation studies were performed for 24 hrs on hairless abdominal skin of rat using the Franz diffusion cell. The flux value obtained from PTG (56.15 ± 2.14 μg/cm2/hr) is about 3-fold higher than that of the drug suspension (19.28 ± 2.14 μg/cm2/hr). PTG formulation showed good stability at 4 ± 1°C and after 3 months of storage, there was no change in liquid crystalline nature, drug content, and other characteristic parameters observed. The PTG formulation is non-irritant. Hence, the prepared formulation can be considered to be safe for topical application. In vivo pharmacokinetic study of PTG showed a significant increase in bioavailability of Nifedipine by 6.452 times with reference to an oral delivery of drug. From the CLSM study, it was confirmed that the penetration of the PTG entrapped dye was enhanced to the dermis from where it can go directly to the blood circulation.

Keywords: Transdermal delivery, Protransfersome gel, skin permeation, stability, bioavailability enhancement.