Pharmacokinetic and Pharmacodynamic Studies of Nifedipine Loaded Microspheres for the Treatment of Hypertension

Abstract

Purpose: The purpose of this research work was to evaluate the Pharmacokinetic (PK), Pharmacodynamic (PD), and the distribution pattern of mucoadhesive microspheres of nifedipine. Methods: Firstly, the emulsion solvent evaporation technique was used to prepare the mucoadhesive microspheres. The microspheres were characterized by Fourier Transform Infrared Spectroscopy (FTIR) and in vivo studies were carried on Wistar rats. Results: Blood samples of rats were withdrawal at 2, 4, and 8 h time interval, after the administration of Mucoadhesive microspheres of nifedipine (Mm-N) and the Saline solution of nifedipine (Ss-N) separately. The Area Under the Curve (AUC) of Mm-N was seven foaled and Cmax around four foaled high when compared with Ss-N with a significant difference P<0.005. Hypertension induced with DOCA (deoxycorticosterone acetate) and the Blood Pressure (BP) of hypertensive rats were recorded at 0, 0.5, 1, 2, 3, 4, 5, 6 h time interval after given Mm-N and Ss-N to different groups. The BP of rats was better control with Mm-N and regular after 2 h with high significant difference P<0.0001 however, the Ss-N have an insignificant difference with P>0.05. The Mm-N was distributed in the upper part of the Gastrointestinal Tract (GIT) after 8 h confirmed with the help of the fluorescence microscopic examination. Conclusion: This study indicates that the nifedipine was present in the blood for a more extended period, and the blood pressure was easily controlled with mucoadhesive microspheres of nifedipine. Therefore, mucoadhesive microspheres of nifedipine would be an excellent alternative over conventional drug delivery for the treatment of hypertension.