Design and Fabrication of Anticancer Drug-Loaded Poly(ε-caprolactone)-Poly(ethylene glycol)-Poly(ε-caprolactone) Micelles as Controlled Release System

Abstract

In this study, doxorubicin (DOX) loaded polymeric micelles (PMs) were synthesized based on biodegradable poly(epsilon-caprolactone)-poly(ethylene glycol)-poly(epsilon-caprolactone) (PCEC) triblock copolymers. So four parameters (shaking speed (rpm) X-1, time of contact (hour) X-2, amount of triethylamine (TEA) (mu L) X-3, DOX% X-4) were optimized. Then by adding valspodar (PSC 833) or D-alpha-Tocopherol polyethylene glycol 1000 succinate (TPGS 1000) to the formulations DOX/PSC 833-PMs or DOX/TPGS 1000-PMs were prepared by a nanoprecipitation method. The synthesized micelles exhibited high drug-loading encapsulation efficiency (> 78.98 %), high stability, and pH-dependent drug release. The results showed that the encapsulation efficiencies were not compromised by co-encapsulation of two agents. Finally, it was observed that the association of both DOX and PSC 833 or both DOX and TPGS 1000 within a single micelle formulation elicited the most soluble DOX as compared to DOX loaded formulations (DOX-PMs) while using a lower amount of polymer compared to separated micelle formulations.