Abstract
Objective: The objective of this research was to formulation, optimization, and evaluation of gastric-mucoadhesive microparticles which contains selective β1 receptor antagonist atenolol.
 Methods: The following chemicals were used, atenolol (Gangwal Chemicals Pvt. Ltd., Mumbai), ethyl cellulose (EC) (Loba Chemie Pvt. Ltd., Mumbai), Carbopol 940 (Loba Chemie Pvt. Ltd., Mumbai), liquid paraffin (Arora Pharmaceuticals Pvt. Ltd., New Delhi), and Span 80 (Central Drug House (P) Ltd., New Delhi). Microparticles were prepared by the emulsification solvent evaporation technique using polymers of Carbomer 934p (CP) and EC. Disc formulations were prepared by direct compression technique from microparticles. Microparticles of combined polymers were designed according to 22 factorial central composite design (CCD), taking EC concentration and surfactant concentration as the independent variables. A total of 13 batches were prepared. The dependent variables were percentage of % drug released and % entrapment efficiency.
 Results and Discussion: All evaluation tests were done for the prepared 13 formulations, such as percentage entrapment efficiency, percentage drug release, swelling index, percentage yield, and particle size analysis. The entrapment efficiency of optimized formulation was found to be 72.02%. The entrapment efficiency increases with increase in EC concentration and stirring speed. Optimized formulation was further subjected to study of drug release kinetics based on the R2 value; it was observed that Korsmeyer Peppas release kinetic model was found to be best suited for formulation of atenolol with EC: carbopol 934 by solvent evaporation method.
 Conclusion: The optimized formulation of microparticles containing atenolol was found to be homogeneous, good appearance and had well flow properties and better release kinetics.
Highlights
It is evident from the recent scientific and patient literature that an increased interest in novel dosage forms that are retained in stomach for a prolonged and predictable period of time exists today in academic and industrial research groups
Mucoadhesive drug delivery systems contain a mucoadhesive polymer that adheres to the gastric mucosal surface and prolong its gastric retention in the gastrointestinal tract (GIT)
The adhesion of polymers with mucous membrane may be mediated by hydration, bonding, or receptor
Summary
Solubility study The solubility study of drugs was performed in water, methanol, ethanol, acetone, 0.1 N hydrochloric acid (HCl), phosphate buffer pH 6.8, and phosphate buffer pH 7.4, individually by keeping the drug containing test tube on vortex mixture [10,11]. The solution containing 10 μg/ml of atenolol in 0.1 N HCl was scanned over the range of 200–400 nm against 0.1 N HCl as blank using double-beam spectrophotometer. The absorbance of each prepared solution was measured at λmax 274 nm using double-beam spectrophotometer against 0.1 N HCl as blank [16,17]. Bulk Density For the determination of bulk density, weight quantities of microparticles were introduced into graduated measuring cylinder and were tapped mechanically or either manually till a constant volume was obtained. Tapped Density The cylinder containing known amount of microparticles was given 100 tabs on tap density apparatus [32] It calculated by formula: Tapped density =. Studies using SEM provided a better understanding of the morphological characteristics of the microparticles [40]
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