Floating Microspheres of Enalapril Maleate as a Developed Controlled Release Dosage Form: Investigation of the Effect of an Ionotropic Gelation Technique.

OBJECTIVES

The purpose of this study was to provide a control drug delivery system through a newly approved work to enhance the absorption and bioavailability of enalapril maleate loaded floating microspheres by ionotropic gelation technique using a hydrophilic carrier.

MATERIALS AND METHODS

Eleven developed formulations of floating microspheres were prepared by ionotropic gelation using different concentrations of sodium alginate, iota-carrageenan, sodium bicarbonate, calcium chloride, and the drug. These microspheres were characterized using a diversity of parameters like micrometric properties, percentage yield, entrapment efficiency, buoyancy, drug release, and kinetics of drug release. The optimum formula was evaluated and identified for drug-excipients compatibility using fourier transform-infrared spectroscopy (FT-IR), surface morphology, powder X-ray diffraction (XRD), and differential scanning calorimetry (DSC).

RESULTS

From the results, F4 was selected as the optimum formula since it provides a faster and premium release of drug from the matrix (91.4%). Kinetics of drug release was found to depend on both diffusion and erosion mechanisms, as the correlation coefficient (R2) was best fitted with Korsmeyer's model and the release exponent (n) was shown to be between 0.43 and 0.84. Scanning electron microscopy images demonstrated spherical, discrete, and freely flowing microspheres with a particle size of 199.4±0.04 μm. Optimum buoyancy properties, percentage yield, and drug entrapment efficiency were achieved. FT-IR showed no interaction between enalapril and the polymers. DSC and XRD showed the miscibility of the drug with the polymers while maintaining the stable crystalline properties of enalapril loaded in the prepared microspheres.

CONCLUSION

The developed floating microspheres of enalapril maleate can be considered a promising controlled drug delivery system, thereby improving patient compliance.