| Autor: |
Cárdenas PA; Departamento de Farmacia, Universidad Nacional de Colombia, Bogotá, Colombia., Alves IA; Faculdade de Farmácia, Universidade Federal de Bahia, Salvador, BA, Brazil.; Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade do Estado da Bahia, Salvador, BA, Brazil., De Araujo BV; Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, RS, Brazil., Aragón DM; Departamento de Farmacia, Universidad Nacional de Colombia, Bogotá, Colombia. |
| Abstrakt: |
This study aims to evaluated the impact of poly(ε-caprolactone) (PCL) microspheres on the pharmacokinetics and pharmacodynamics (PopPK/PD) of 6-methylcoumarin (6MC). For this, PCL microspheres loaded with 6MC were prepared using the emulsification-evaporation method. Particle size, zeta potential, drug loading, and entrapment efficiency were characterised by dynamic light scattering and UV spectrophotometry. In vitro release and pharmacokinetics in Wistar rats were assessed for free and encapsulated 6MC. Anti-inflammatory activity was evaluated using the carrageenan-induced paw edoema model, with PopPK and PopPK/PD models developed. Microspheres showed diameters between 2.9 and 7.1 µm, zeta potentials of -10 to -15 mV, and drug loading of 0.24 mg/mg. Encapsulation efficiency was 45.5% to 75.9%. PopPK models showed enhanced absorption and distribution, with increased anti-inflammatory potency of encapsulated 6MC. PCL microspheres significantly improved the pharmacokinetic and pharmacodynamic profiles of 6MC, enhancing its therapeutic potential for lipophilic drugs. |
