Abstract
Objective: Triblock copolymer of poly(ethylene glycol)-poly(ɛ-caprolactone)-poly(ethylene glycol) (PEG-PCL-PEG, PECE) was applicated as hydrophobic drug. This study aims to optimization and characterization of PECE triblock copolymer as carriers of hydrophobic drug (ketoprofen).
 Methods: Triblock copolymer of PECE was prepared with varying composition ratio of PEG and PCL by ring-opening and coupling reaction. The characteristics of triblock copolymer were characterized using FTIR and DSC. Variation composition ratio of poly(ɛ-caprolactone) (PCL)/poly(ethylene glycol) (PEG) and ratio PECE/drug as factors for optimization using full factorial design. Ketoprofen was loaded into PECE triblock copolymer micelles by emulsification and solvent evaporation method. Responses were measured particle size, entrapment efficiency (EE) and drug solubility.
 Results: The result of this study showed that a higher ratio of PCL/PEG and ratio of PECE/drug, reducing particle size, increasing EE and improving drug solubility. The optimum formula obtained by ratio of PCL/PEG is 2:1 and ratio of PECE/drug is 40:1 with particle size is 356,967±9,142 nm, EE is 57,751±0,437%, drug solubility is 32,648±0,200 µg/ml and zeta potential-18,867±2,578 mV. A full factorial design was applied to determine the optimum formula for the PECE triblock copolymer as drug carriers.
 Conclusion: The PECE triblock copolymer was preparated using ring-opening polymerization method with Sn(Oct)2 as a catalyst and then continued the reaction with HMDI as coupling agent. Ketoprofen was loaded into PECE triblock copolymer using methods emulsification and solvent evaporation.
Highlights
The polymers used in drug formulations is biodegradable polymers that mean they can be degraded by metabolic reaction in the body
Preparation of the poly(ethylene glycol) (PEG)-PCL-PEG (PECE) triblock copolymer: PECE triblock copolymers were prepared by ring-opening polymerization of ɛ-CL using Sn(Oct)2 as catalyst and continued by coupling reaction using hexamethylene diisocyanate (HMDI) as coupling agent is illustrated in fig
Based on the factorial design that the PECE triblock copolymer was prepared with PCL/PEG ratio of 0.5:1 and 2:1, and PECE/drug ratio of 10:1 and 40:1
Summary
The polymers used in drug formulations is biodegradable polymers that mean they can be degraded by metabolic reaction in the body. Polymer in drug formulation can be used in the form of triblock copolymer. Biodegradable polymers that can be used in drug delivery such as poly(ɛ-Caprolactone) (PCL) and poly(ethylene glycol) (PEG) [1]. Triblock copolymers have advantages such as can be applied as a carrier of hydrophilic or hydrophobic drugs, can be varied arrangement of polymer blocks, and can be used for improving drug solubility or controlling drug release [2]. The application of triblock copolymer with the composition of PCL and PEG has existed previously as drug delivery system of drug that has a low solubility (hydrophobic). The triblock copolymer will take the hydrophobic drug into aqueous by forming a nano-sized polymer micelle spontaneously. The hydrophilic block will interact with aqueous solution while the hydrophobic block will be the core-shell that contains hydrophobic drugs so can increase the solubility of the drug [3]
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