Abstract
Objective: This study aims to synthesize, characterize, and optimize biodegradable polycaprolactone-polyethylene glycol-polycaprolactone (PCL-PEG-PCL) triblock copolimeric micelles as a nanocarrier for hydrophobic drug solubility enhancer of ketoprofen (K).
 Methods: PCL-PEG-PCL (PCEC) triblock copolymers was obtained from the synthesis of ɛ-caprolactone (ɛ-CL) and PEG by ring opening polymerization (ROP) method at different PCL: PEG ratio (2-5:1). The K-loaded PCEC triblock copolymeric micelles was obtained by solvent evaporation method. Optimization of PCEC triblock copolymers and analysis of the effect of PCL: PEG ratio factors on the responses toward particle size (PS), polydispersity index (PdI), and entrapment efficiency (EE), were carried out through the design of experiments (DoE) approach of the 22 full factorial design method using the Design-Expert software to obtain the optimum formula.
 Results: The higher the PCL: PEG ratio, the ZP value tends to be smaller while the PS, PdI, EE, and drug solubility may be increased, but the addition of hydrophobic blocks to some extent does not affect the EE and drug solubility. The optimum K-loaded PCEC triblock copolymeric micelles with a PCL: PEG 2.0:1 ratio has a zeta potential (ZP) of-24.07±0.35 mV, the particle size of 235.70±6.03 nm, polydispersity index of 0.30±0.06, entrapment efficiency of 87.08±0.06%, and the solubility of the K increases by 10.60 times.
 Conclusion: The 22full factorial design has been proven to be the suitable optimization method to determine the optimum condition that yields to the optimum results of the PS, PdI, and EE of the of the K-loaded PCEC triblock copolymer micelles.
Highlights
Biodegradable polymers such as polycaprolactone (PCL) and polyethylene glycol (PEG) are often used in drug formulations because they are degraded by metabolic reactions in the body so that they are safe to use and are not toxic after hydrolyzing [1, 2]
The FTIR spectra of the synthesized PCEC triblock copolymers based on parameters of functional groups is displayed in fig
The formation of PCEC triblock copolymers is indicated by the detection of several functional groups namely the ether group (C-O-C) and the alkaline group (C-H) from the bonding of PEG and PCL units with the peak of the band that appears in the frequency region of 1050-1300 cm-1 and of 28502970 cm-1, as well as the carbonyl ester group (C=O) and hydroxyl group (O-H) of the PCL unit bonding with the peak of the band that appears in the frequency region of 1690-1760 cm-1 and of 3200-3600 cm-1 [12, 14]
Summary
Biodegradable polymers such as polycaprolactone (PCL) and polyethylene glycol (PEG) are often used in drug formulations because they are degraded by metabolic reactions in the body so that they are safe to use and are not toxic after hydrolyzing [1, 2]. This polymer can be used in the form of triblock copolymers as carriers of drugs with the aim of increasing the low solubility of drugs in water (hydrophobic drugs) [3]. This system is expected to be able to increase the solubility of K [5, 6]
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