Ultrasound-induced microencapsulation of simvastatin for gastric retention and controlled delivery

Abstract

The objective of this study is to demonstrate an effective technique with potential for commercialization for microsphere production. Ultrasound-assisted ionic gelation of sodium alginate was used to encapsulate simvastatin. Chitosan was used as a mucoadhesive polymer for gastroretention of microsphere. Sodium alginate solution was sonicated using probe sonicator at a frequency of 20±3 KHz and ultrasonic power of 130 W with an input voltage range of 170-270 AC, 50 Hz, at a temperature of 50°. The influence of ultrasound waves on drug entrapment efficiency, yield and particle size dispersion was studied in comparison to mechanical stirring method. Mucoadhesiveness, release pattern and kinetics of drug release were also characterized. Ultrasound treatment caused small fissures and depressions on the surface of alginate as evidenced in SEM. Ultrasound of 20±3 KHz for 12 min duration was the optimum frequency and time in the experimental set up to obtain microspheres with uniform and smaller microparticles. The encapsulation efficiency of simvastatin was directly proportional to the sonication effect, concentration of alginate and extent of its cross linkage with calcium ions. DSC studies revealed that ultrasound treatment did not alter the structural integrity of the drug component. Formulation was found to be dissolution efficient and drug release pattern was concentration-dependent, which followed non-Fickian diffusion mechanism with an ‘n’ value of 0.8. Therefore, it could be concluded that ultrasound can be used as an efficient technology to develop drug-entrapped microsphere for controlled delivery.