Abstract

Objective: This study aims to optimize PCL-PEG-PCL (PCEC) triblock copolymer micelles as a hydrophobic drug carrier, simvastatin (SV).
 Methods: PCEC triblock copolymer was prepared by the ring-opening polymerization method (ROP) with different ɛCL/PEG ratio (2 and 5). SV was incorporated into the PCEC triblock copolymer micelles with a concentration of 2.5 and 10 % w/w by the solvent evaporation method (film formation). The influence of the ɛCL/PEG ratio and concentration of SV effect on the responses particle size (PS), polydispersity index (PI) and entrapment efficiency (EE) was assessed using 22 full factorial design method. The test results were analyzed using Design-Expert software to obtain the optimum formula.
 Result: The selection of the optimum formula is based on the desirability value, the formula with the largest desirability value is chosen as the optimum formula. The results showed the optimum formula chosen had a desirability value of 0.860 consisting of a ɛCL/PEG ratio of 5 and SV concentration of 10 % w/w, with the PS, PI dan EE value was 322.1±3.51 nm, 0.471±0.09 and 87.08±1.17 %, respectively.
 Conclusion: The 22 full factorial design has been proven to be used as an optimization method to determine the optimum formula of SV-loaded PCEC triblock copolymer micelles with a good result of the PS, PI and EE responses.

Highlights

  • Polymeric micelles have been received much attention in recent decades as a potential drug carrier

  • The 22 full factorial design has been proven to be used as an optimization method to determine the optimum formula of SV-loaded PCEC triblock copolymer micelles with a good result of the particle size (PS), polydispersity index (PI) and EE responses

  • The result of the analysis showed that the three responses gave significant results (p

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Summary

Introduction

Polymeric micelles have been received much attention in recent decades as a potential drug carrier. Triblock copolymers will form a core-shell structure, where the core as a hydrophobic block will be a place to accommodate the hydrophobic drug, while the shell as a hydrophilic block lining the core will maintain the stability of micellar polymer in an aqueous environment and affect its solubility in water. This type of triblock copolymer can be an ideal drug carrier candidate with the aim of improving poorly drug solubility [1, 2]. This system may improve its solubility as to be expected

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