SUSTAINED RELEASE MUCOADHESIVE MICROCAPSULES OF RAMIPRIL BY IONIC GELATION TECHNIQUE: FORMULATION DESIGN, OPTIMIZATION AND CHARACTERIZATION

Korlapati Venkateswara Rao,V V Venkatchalam

doi:10.22159/ijpps.2017v9i2.12660

Abstract

Objective: The major objective of the research work was to design, optimise and characterise sodium alginate based sustained release mucoadhesive microcapsules of ramipril by ionic gelation method.Methods: An experimental set-up was designed to investigate the optimal combination of mucoadhesive polymers such as carbopol 974P, HPMC (K4M and K100M), Na CMC and chitosan and their drug compatibility with respect to reliabilities. Preliminary screening of the formulation variables was accomplished by Taguchi design followed by Box-Behnken design for systematic optimisation. The suitable mathematical model was selected, response surface analysis was performed and optimised formulation was chosen by numerical optimization and desirability function method. Characterization of the prepared microcapsules for several inherent properties like particle size, drug content, sphericity, entrapment efficiency, loose surface crystal study, swelling index, micromeritic properties, moisture content, in vitro drug release, mucoadhesive strength and in vivo antihypertensive activity was performed.Results: Differential Scanning Calorimetry (DSC) thermograms and Fourier Transform Infra-Red (FT-IR) spectral studies revealed no incompatibility between the pure drug and selected polymers. The spherical nature of the prepared microcapsules was established by surface morphology studies.Conclusion: The resultant sustained release mucoadhesive microcapsules of ramipril remained stable when subjected to stress conditions unveiling it as a better alternative delivery system with superior therapeutic efficacy.

Highlights

The oral route is most sought-after for the administration of drug molecules to the systemic circulation due to ease of administration, better treatment and patient compliance and costeffective [1]
This calls for the development of ramipril loaded novel mucoadhesive multiparticulate drug delivery systems to enhance its oral bioavailability with improved pharmacodynamic potential [11, 12]
The results obtained from preliminary formulation studies indicated the levels of Na-alginate and HPMC K100M, crosslinking time (h) and conc

Summary

Introduction

The oral route is most sought-after for the administration of drug molecules to the systemic circulation due to ease of administration, better treatment and (or) patient compliance and costeffective [1]. Mucoadhesive microcapsules are the multiple unit particulate systems contain mucoadhesive polymers, which provide sustained release action upon intimate contact with the epithelial mucous membrane lining [4, 5]. Such formulation protects the drug from the gastric acidic environment, increases the oral bioavailability of drugs and reduces the variability. The conventional dosage forms available in the market fail to satiate the needs of enhancing the oral bioavailability and to improve the patient compliance This calls for the development of ramipril loaded novel mucoadhesive multiparticulate drug delivery systems to enhance its oral bioavailability with improved pharmacodynamic potential [11, 12]. The mucoadhesive drug delivery systems contain polymers of diverse chemical nature, requires optimization of them to obtain the robust formulations with desired therapeutic performance [16]

Methods

Results

Conclusion