Abstract

FORMULATION DESIGN, OPTIMIZATION AND EVALUATION OF MUCOADHESIVE BUCCAL TABLETS OF ATENOLOL

Vikash Dahiya, Dr. Saroj Jain and Dr. Seema Rohilla*

ABSTRACT

The aim of this study was to design and optimize mucoadhesive buccal tablets of atenolol for systemic delivery. Direct compression method was used for the preparation of buccal tablets, and screening studies were conducted with different polymers to determine their effects on tablet characteristics. Carbopol (CP) and hydroxyl propyl methyl cellulose (HPMC) were two polymer that were selected for further optimization studies by applying response surface methodology. Cumulative % drug release from buccal mucosa was selected as important response. Physicochemical compatibility of formulation excipients and atenolol was evaluated by using Fourier transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC) analysis. In vitro drug release profiles and release kinetics were investigated; swelling index and matrix erosion studies were conducted. Optimum formulation consisted of 25% CP and 40% HPMC, which provided 5.23±0.29 hour ex vivo RT, and 2.63±0.17 N DF. FT-IR spectroscopy and DSC analysis revealed that there was no chemical interaction present between tablet ingredients. Cumulative atenolol release of 94.11±5.19 % was achieved after 9 hours of in vitro dissolution studies, which was supported by swelling and matrix erosion analysis. Mechanism of atenolol release was fitted best to zero-order model, while release exponent (n) value of 0.799 demonstrated an anomalous (non-Fickian) release, indicating combined erosion and swelling mechanism. The results suggested that optimized buccal tablets of atenolol would be a promising and alternative delivery system for the treatment of hypertension and migraine.

Keywords: Atenolol, Carbopol, Hydroxy propyl methyl cellulose, Buccal tablets, Mucoadhesion, Quality by design, Drug Delivery.