Formulation and Evaluation of Lacidipine Loaded Nanoparticulate Oral Disintegrating Tablets

Abstract

Introduction: Hypertension is the main cause of Heart Diseases. As per world Statistics Heart Diseases are increasing year by Year. The Drug used in the present Research investigation is Lacidipine which is a Dihydropyridine calcium channel blocker that is used in the treatment of hypertension and angina pectoris.

Objectives: Lacidipine Loaded Nanoparticles were prepared by using Solvent-Antisolvent precipitation method to improve its solubility. The Nanosized Nanoparticles were prepared into Oral Disintegrating tablets by using suitable Super Disintegrants.

Method: The nanoparticles were created using Solvent-Antisolvent precipitation method, which used Anisole and N-Methyl 2 pyrrolidone as solvents and water as an antisolvent in various ratios of 1:1, 1:2, and 1:3, with Pluronic F 407 and Cremophore as stabilizers. The Nano suspension obtained through this method was Lyophilized. The Lyophilized powder was blended and Precompression parameters are applied, followed by the preparation of oral disintegrating tablets using Superdisintegrants such as sodium starch glycollate, cross caramellose sodium, and cross povidone via the Direct Compression method.

Results: All prepared oral disintegrating tablets had post compression parameters tested. According to the official limits, all of the formulations demonstrated the desired physicochemical properties. Within 30 minutes, drug release studies were performed on all formulations using a USP II paddle type apparatus and a pH 6.8 phosphate buffer. F9 had the highest drug release rate of any formulation (98.89%). F9 and marketed formulation drug release studies were carried out. F9 demonstrated 98.89% drug release versus 83.35% for the marketed formulation. Kinetic studies for the drug release mechanism were carried out on the optimized formulation F9. The release kinetics of the Optimized formulation F9 revealed that the formulation followed first order kinetics, with R2 = 0.869 indicating that drug release is concentration dependent.

Conclusion: Nanoparticles were prepared successfully by Solvent-Antisolvent precipitation method and Optimized Formulation was made into Oral Disintegrating Tablets to increase Solubility of the Formulation and expected Increase in the therapeutic efficacy of the poorly soluble Drug.