“IMPLEMENTATION OF FORMULATION AND CHARACTERIZATION OF SUSTAIN RELEASE MICROBEADS OF TELMISARTAN "
Abstract
Background Hypertension is a significant health concern worldwide, prompting the need for effective pharmaceutical interventions. One emerging approach involves sustained release drug delivery systems, such as microbeads, which offer a novel means of managing hypertension symptoms. These microbeads serve as carriers for antihypertensive drugs, providing controlled release over an extended period.
Main Body n this study, sustained-release microbeads of Telmisartan were developed to ensure prolonged drug action and reduce the need for frequent dosing. Six formulations (F1 to F6) were prepared using varying polymer ratios through the ionotropic external gelation method. Preformulation studies, including melting point, solubility, and FTIR analysis, confirmed no significant interaction between Telmisartan and the polymers.
Characterization of the microbeads post-formulation revealed a uniform particle size range of 425-520 nm and an entrapment efficiency between 61% and 75%. The microbeads exhibited good flow properties with bulk density between 1.158-1.232 g/cm³ and tapped density from 2.112-2.174 g/cm³. The swelling index ranged from 315 to 542, indicating effective swelling and drug release control.
In vitro studies showed cumulative drug release of 82% to 99% over 12 hours, fitting the Higuchi model, which indicates a diffusion-controlled release mechanism. Formulation F1 demonstrated the lowest sustained release (82%) over the 12-hour periodConclusion The research successfully formulated sustained-release microbeads of Telmisartan, providing a controlled and prolonged drug release over 12 hours. Among the six batches, formulation F1 exhibited the lowest sustained drug release at 82%, while others showed a higher release profile up to 99%. The characterization of these microbeads, including their size, entrapment efficiency, and swelling properties, as well as their flow dynamics, supported their potential for consistent and effective drug delivery. The adherence to the Higuchi model in the release kinetics further underscores the robustness of the developed formulations in achieving sustained drug release.