Development and evaluation of poly(3-hydroxybutyrate-co-3-hydroxyvalerate) and polycaprolactone microparticles of nimodipine

• Published in: Current pharmaceutical design Vol. 19; no. 41; p. 7264
• Main Authors: Riekes, Manoela K, Junior, Luiz R Olchanheski, Pereira, Rafael N, Borba, Paola A A, Fernandes, Daniel, Stulzer, Hellen K
• Format: Journal Article
• Language: English
• Published: United Arab Emirates 2013
• Subjects: Animals; Drug Evaluation, Preclinical - methods; Female; Microspheres; Nimodipine - administration & dosage; Nimodipine - chemistry; Particle Size; Polyesters - administration & dosage; Polyesters - chemistry; Random Allocation; Rats; Rats, Wistar; X-Ray Diffraction
• ISSN: 1873-4286
• DOI: 10.2174/138161281941131219125657

Polymeric microparticles containing the calcium channel blocker nimodipine were successfully obtained through simple emulsion/ organic solvent evaporating method. The extended release formulations, composed by the polymers poly(3-hydroxybutyrate-co-3- hydroxyvalerate) (PHBV) and polycaprolactone (PCL), were submitted to characterization through X-ray powder diffraction (XRPD), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), thermogravimetric analysis (TG), Fourier transform infrared analysis (FT-IR) and determination of the mean particle diameter. All formulations obtained revealed an amorphous characteristic, proven through XRPD and DSC results. Besides, no chemical interaction was observed between drug and polymer in polymeric microparticles. PHBV-NMP formulation showed a higher drug entrapment, a larger particle size, a thermal degradation behavior similar to that observed for nimodipine and a longer drug release time, being selected for in vivo evaluation. The PHBV-NMP polymeric microparticles were able to keep the pharmacological antihypertensive effect for a longer period of time, becoming a good alternative to control nimodipine release in hypertension treatment.