Formulation and evaluation of carvedilol microcapsules using Eudragit NE30D and sodium alginate

Abstract

Inclusion complexes of carvedilol(CR) with hydroxyl propyl beta-cyclodextrin (HPBCD) was prepared using co-grinding technique. Then, the inclusion complex was microencapsulated using combinations of Eudragit NE30D (EU) and sodium alginate (SA) utilizing orifice gelation technique. The formulations were analysed by using Scanning electron microscopy (SEM), Fourier Transform Infrared spectroscopy (FTIR), Differential scanning Calorimetry (DSC) and X-ray diffractometer (XRD) and also evaluated for particle size, encapsulation efficiency, production yield, swelling capacity, mucoadhesive properties, zeta potential and drug release. The microcapsules were smooth and showed no visible cracks and extended drug release of 55.2006% up to 12 hours in phosphate buffer of pH 6.8, showing particle size within the range of 264.5-358.5 µm, and encapsulation efficiency of 99.337±0.0100-66.2753±0.0014%.The in vitro release data of optimized batch of microcapsules were plotted in various kinetic equations to understand the mechanisms and kinetics of drug release, which followed first order kinetics, value of "n" is calculated to be 0.459 and drug release was diffusion controlled. The mice were fed with diet for inducing high blood pressure and the in vivo antihypertensive activity of formulations was carried out administering the optimized formulations and pure drug separately by oral feeding and measured by B.P Monwin IITC Life Science instrument and the results indicated that the bioavailability of carvedilol was increased both in vitro and in vivo with the mucoadhesive polymers showing primary role in retarding the drug release.

Formulation and characterization of nanofibers and films with carvedilol prepared by electrospinning and solution casting method

“…An FT-IR spectrum of pure carvedilol showed the peaks 3446 cm −1 (N\ \H, stretching), 2926 cm − 1 (C\ \H, stretching), 2842.60 cm − 1 (C\ \H, stretching) and 1094 cm −1 (C\ \O, stretching). These peaks can be considered as characteristic peaks of carvedilol (Dewan et al, 2012;Bal et al, 2013;Sharma, 2013).…”

Design, Development, and Characterization of Ocimum Basilicum Mucilage-Based, Modified Release Mucoadhesive Gastrospheres of Carvedilol

“…The values of release exponent (n) determined from in vitro DR data of various CRV gastrosphere S3, S4, S6, S7, S8, and S9 follow the anomalous non-Fickian DR (0.61-0.822), i.e., the rate of solvent penetration and DR is in the same range, and S1, S2, and S5 indicating the DR from this gastrosphere followed the Case-II transport mechanism controlled by swelling and relaxation of polymeric blend in gastrosphere matrix. This could be attributed due to O. basilicum mucilage polymer dissolution and enlargement or relaxation of polymeric chain [14,22]. .…”

“…For enhancement of CRVs absorption it has been formulated with a series of polymers from point of view of preventing its oral degradation. Since the drug has less solubility and dissolution rate, several methods are used to improve its dissolution rate such as solid dispersions, cyclodextrin complexes, and microcapsules [14]. CRV has short biological halflife of 2 h. Its main absorption site is proximal small intestine [15].…”

MICROENCAPSULATION of grapefruit oil with sodium alginate by gelation and ionic extrusion: optimization and modeling of crosslinking and study of controlled release kinetics.

“…The concentration of calcium chloride solution and the crosslinking reaction have an effect on the efficiency and yield during the encapsulation process. The matrix obtained after crosslinking can lead to a controlled release (Bal et al, 2013) with a release mechanism of the active components sustained in time (Finch, 2005).…”