Encapsulation and release characteristics of DCTN/PLGA microspheres

Abstract

In the present study, poly (D,L-lactic-co-glycolic)-acid microspheres containing trans-Dehydrocrotonin (DCTN) were prepared by the double emulsion method. The hypoglycemic activity of DCTN-loaded microspheres was monitored in normal glycemic mice after administration of a daily dose of DCTN (50 mg kg⁻¹ body weight) for 7 days. Spherical microspheres with two populations of particles with 3.20 ± 0.10 and 7.60 ± 0.70 µm mean diameter size µm were observed. The encapsulation efficiency of DCTN was 85.5 ± 3.9%. The in vitro kinetic profile of DCTN from PLGA-microspheres was initially fast (burst effect of 19.4% at 2 h). Such a burst step was maintained until achieving 35.7±2.0% at 7h, followed by a gradual release of DCTN attaining a maximum drug release at 55.7 ± 2.6% within 30 h. DCTN was able to reduce glucose levels (14.3%) of normal glycemic animals and this effect was improved by its encapsulation into microspheres (26.8%). The optimum glucose levels in the blood of animals treated with DCTN suspension and DCTN-loaded microspheres were 119.21 ± 19.75 mg dL⁻¹ at day 5 and 103.08 ± 18.88 mg dL⁻¹ at day 7, respectively. DCTN-loaded microspheres are thus offered as a potential delivery system for the treatment of metabolic diseases characterized by hyperglycemia.

• Trans-dehydrocrotonin
• Croton cajucara
• PLGA
• microspheres
• hypoglycemic activity