Abstract

Objective: The present investigation focused on fabrication and evaluation of atenolol releasing buccal patches comprising mucoadhesive hydrophilic polymers like sodium alginate and tamarind seed polysaccharide with a drug-free backing layer (6 % ethylcellulose). Methods: Solvent evaporation technique being employed in the development of atenolol comprising buccal patches using mucoadhesive hydrophilic polymers. The prepared buccal patch formulations were tested for thickness, weight variation, folding endurance, drug content, moisture content, moisture absorption, % swelling, surface pH, in vitro residence time and mucoadhesion studies. The drug permeation through goat buccal mucosal membrane was conducted with the use of Franz diffusion cell in phosphate buffer saline, pH 6.8 and was subjected to FT-IR and SEM characterization. Stability study was performed as per ICH guidelines. Results: For all the buccal patch formulations, the average weight, thickness, drug content, moisture content, moisture absorption, % swelling, surface pH study exhibited satisfactory results. Out of 7 different buccal patches, the formulation FA-1 revealed the highest mucoadhesive strength (31.36±0.95 g), the force of adhesion (0.31±0.04 N), maximum swelling index (341±0.83 %) and more than 24 h in vitro residence time. The buccal patch formulation FA-1 indicated highest drug permeation (97.51 %) in 24 h and was found to be stable. FT-IR examination confirms lack of drug polymer interaction. SEM investigation reveals a smooth surface of the buccal patch. Conclusion: The developed buccal patches comprising atenolol can be very promising in increasing patient compliance and reducing dosing frequency.

Highlights

  • The peroral mode of drug administration is a convenient and popular path of medication delivery accepted universally

  • The buccal route is preferred over other noninvasive routes on the basis of the following reasons: The drug administration via buccal route provides, bypassing of presystemic metabolism, improve bioavailability, sustained manner drug delivery, rapid onset of action, easy termination of therapy as per requirement, increased ease of drug administration and improved patient acceptance [5-7]

  • The present study was an attempt to develop, evaluate and characterize atenolol comprising buccal patches consisting drug in a mucoadhesive polymeric layer of sodium alginate and tamarind seed polysaccharide and a drug free backing membrane composed of 6% ethyl cellulose employing solvent evaporation technique

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Summary

Introduction

The peroral mode of drug administration is a convenient and popular path of medication delivery accepted universally. The difficulties associated with the oral route such as presystemic metabolism, drug degradation in the gastrointestinal environment, poor bioavailability of certain group of drugs necessitate the development of some other non-invasive route like buccal, transdermal, rectal, inhalation route of drug administration [1, 2]. The buccal route is preferred over other noninvasive routes on the basis of the following reasons: The drug administration via buccal route provides, bypassing of presystemic metabolism, improve bioavailability, sustained manner drug delivery, rapid onset of action, easy termination of therapy as per requirement, increased ease of drug administration and improved patient acceptance [5-7]. Atenolol due to small dose, substantial first-pass metabolism, less half-life and low oral bioavailability, makes it a suitable candidate for delivery by buccal path [8, 9]

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