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摘要
6-methylcoumarin (6MC) has demonstrated promising anti-inflammatory activity. However, its low aqueous solubility has limited in vivo studies, as is difficult to administer to experimental animals. The aims of this work were to develop polycaprolactone microparticles loaded with 6MC to find the best processing conditions to obtain good features of the microparticulate system, and to evaluate the anti-inflammatory activity of the free and microencapsulated drug. Polycaprolactone microparticles loaded with 6MC (6MC-MP) were prepared by the solvent emulsification-evaporation method. Using the Plackett-Burman experimental design as a tool, the best variables of the process were selected. The anti-inflammatory activity of the resulting 6MC-MP was evaluated in carrageenan-induced paw edema in Wistar rats, at a dose of 200 mg/Kg administered by the intraperitoneal route. The best variables to obtain microparticles with a process yield of 77%, encapsulation efficiency of 67%, burst effect of 33% and particle size of 8.3 m were selected. At the 3rd, 5th, 7th, and 24th h 6MC-MP exhibited significant anti-inflammatory activity (inhibition between 50 and 70%), while free 6-methylcoumarin reached only 40% inhibition at 3rd hour. 6MC shows a significant anti-inflammatory effect while the anti-inflammatory activity observed for 6MC-MP was almost double. This fact can be attributed to the low aqueous solubility of 6MC, since the drug must be dissolved before being absorbed and reach systemic circulation. This results support the use of 6MC-MP as a drug delivery system that improves the anti-inflammatory activity of 6MC.
- 出版日期2014
