Formulation, characterization and statistical optimization of enalapril-loaded lipospheres

Abstract

Lipid based polymers have been proved to be as efficient drug carriers to overcome insufficiencies of conventional formulations. Ceresin wax (CSW) was employed to improve permeability, oral bioavailability and patient compliance by preparing Enalapril (EP) loaded lipospheres with simple solvent evaporation method. Box-behnken design with proposed polynomial equations and quadratic model was applied to statistically investigate and validate collective influence of formulation variables on lipospheres. Spherical smooth surface lipospheres having an average size of 55 µm with excellent micromeritics properties were produced. DSC, X-RD and FTIR findings proved the lack of any possible interaction between formulation components. Zeta potential ranged from –5 mV to –20 mV suggested significant stability of lipospheres. The responses like percentage yield (29–68%,), entrapment efficiency (21–53%) and drug release (42–93%) were found to be greatly affected by concentration of lipids, surfactant and stirring speed. Reduce and sustained EP release from lipospheres may lower treatment cost and enhance hypertensive patients’ compliance.