Formulation, Development & Characterization of Floating Microspheres of Novel Calcium Channel Blockers

Abstract The present study was aimed at the development of stomach specific drug delivery systems using various approaches like mucoadhesive. From the stock solution, a suitable concentration (10g/ml) was prepared with pH 1.2 Hydrochloric acid buffer solution and UV scan was taken between 200-400 nm. The absorption maxima of 278 nm was selected and utilized for further studies. From the stock solution, 10, 20, 30, 40, 50, and 60   g/ml solutions of Verapamil hydrochloride were prepared in pH 1.2 hydrochloric acid buffer solution. Weighed quantities of Verapamil Hydrochloride, ethyl cellulose, polyethylene oxide and hydroxy propylmethyl cellulose (HPMC K15M) were dissolved in a mixture of ethanol and dichloromethane (1:1 solvent ratio) at room temperature in a magnetic stirrer at 50 rpm for 50 min. For the DSC the samples were scanned from 400 to 4,000 cm-1 wave number. The dynamic scans were taken in nitrogen atmosphere at the heating rate of 10 °C min-1. The energy was measured as Joules per kilocalorie. USP dissolution test apparatus II by spreading the microspheres (100 mg) on 900 ml of 0.1 N HCl containing 0.02 % v/v tween 80 as surfactant. The entrapment efficiency of F3, F7 & F9 was higher compared to other formulations. These formulations contained Ethyl cellulose (2%) and Polyethylene oxide (1%), HPMC K15M (1%) & Eudragit L100 (1%) respectively. The percentage yield of the microspheres was found to increase with increasing ethyl cellulose concentration, as was true in F3, F7 and F9.The encapsulation efficiency ranged between 53 ± 2.2 to 89 ± 1.9%, and was observed that the encapsulation efficiency increased with increasing amount of polymers in the hollow microspheres. The sphericity factors for all formulations were in the range of 1.01 ± 0.2 to 1.29  ±  0.6  and  the  sphericity  values  of  best  formulations  F3,  F7  and  F9  were 1.05±0.2, 1.07 ± 0.1 and 1.16 ± 0.1 respectively. Systems that are designed as prolonged release can also be considered as attempts at achieving sustained release delivery.

Keywords Formulation & Development, Floating Microspheres, Novel Calcium Channel Blockers, Improve therapy, Mucoadhesive microspheres.

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Updated: January 20, 2024 — 7:16 am