IN-VIVO CHARACTERIZATION OF TRANSDERMAL PATCHES OF ALISKIREN HEMIFUMARATE FOR TREATMENT OF HYPERTENSIONAbstract
The low bioavailability of drugs in the oral drug delivery system is the main concern and the development of a delivery system with a controlled release profile. This research aims in the dose reduction of aliskiren hemifumarate, evaluate the release efficacy of the drug from the patches by using various permeation enhancers. FTIR studies established the drug and polymer compatibility. The transdermal patches were prepared by using a solvent casting method using different polymers and permeation enhancers. The keshary chein diffusion cell was used for performing in-vitro permeation studies. By physicochemical parameters and in-vitro release pattern, the formulation made from MethocelK 15M (1:1.5) was selected for in-vivo studies. The steady plasma concentration was observed on application of developed transdermal patches, as confirmed by bioavailability studies in rats. The bioavailability was also improved as compared to oral administration. The SEM studies of transdermal patches show that the patches prepared with MethocelK 15M with cineol as penetration enhancer exhibited the uniform distribution of the drug. The hypertension was induced in rats using dexamethasone and treated with oral administration & application of the transdermal patch. The patches significantly controlled hypertension from the first hour. The stability studies indicated satisfactory performance as evaluated for assay & description on storage for six months. Conclusion: The developed transdermal patch exhibited therapeutic superiority over oral drug delivery.
B. Sethi * and R. Mazumder
Department of Pharmaceutics, SGT College of Pharmacy, SGT University, Budhera, Gurugram, Haryana, India.
05 August 2018
14 October 2018
20 October 2018
01 April 2019