Formulation and evaluation of polymeric nanoparticles of an antihypetensive drug labetalol

Abstract

Labetalol is an adrenergic receptor blocking agent used in the treatment of hypertension and characterized by high solubility and high permeability which corresponds to BCS class I drug. Plasma half life ranges from 6 & bioavailability is 25%. Ethyl cellulose was used as a rate controlling polymer. Effects of addition of ethyl cellulose on in vitro dissolution were studied. Nanoparticles were formulated using different polymer ratios. In vitro drug release was carried out by using USP Type II at 50 rpm in 900 ml of acidic dissolution medium (pH 1.2) for 2 hours, followed by 900 ml alkaline dissolution medium (pH7.4) for 12 hours. Mean dissolution time is used to characterize drug release rate from a dosage form. Several kinetic models were applied to the dissolution profiles to determine the drug release kinetics. Excipients are selected by FTIR studies. Finally the nanoparticles were evaluated for various characteristics like encapsulation efficiency, percentage yield, partial size and the In vitro release for 12 hrs. The nanoparticles were found to be discrete, spherical, and free-flowing. The nanoparticles were uniform in size, and the microencapsulation efficiency was in the range of 52.5-81.7%. The surface morphology of prepared Labetalol nanoparticles was observed under scanning electron Microscopy. Nanoparticles had good spherical geometry. The stability study was performed at 40ºC ± 2ºC and 75 ± 5% RH for 6 months.
 Keywords: Nanoparticles; Labetalol, Hypertension, Ethyl Cellulose, Dissolution, entrapment efficiency.

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