Abstract
2-Methacryloyloxyethyl phosphorylcholine (MPC) polymers have been used as a coating agent on medical devices and as a carrier in drug delivery systems (DDSs). Paclitaxel (PTX) is a water-insoluble anticancer drug whose solubilizer is necessary for administration. Block and random copolymers composed of hydrophilic MPC and butyl methacrylate, named PMB, show different properties, depending on the polymer sequence and MPC content. In the present study, we used amphiphilic MPC polymers comprising hydrophobic dodecyl methacrylate (DMA). The self-assembling properties and PTX solubilization of random and block poly(MPC-co-DMA)s (rPMDs and bPMDs) with different compositions were examined and compared. rPMDs with high DMA content formed large and relatively loose self-assembled structures, which solubilized PTX. However, bPMDs formed small and compact self-assembled structures with poor PTX solubilization. PTX solubilized by PMB with small and loose self-assembled structures showed efficient drug action, similar to free PTX; however, rPMDs fell short of demonstrating PTX efficiency. Our results suggest that the self-assembling properties and the hydrophobicity of amphiphilic MPC polymers largely affect PTX solubilization as well as drug action, which is required to be controlled by the polymer sequence, as well as the structure and composition of the hydrophobic monomer for efficient DDS.
Highlights
2-Methacryloyloxyethyl phosphorylcholine (MPC) polymers have been used as a coating agent on medical devices and as a carrier in drug delivery systems (DDSs)
After the cycle of freezing–degassing–thawing and the bubbling of nitrogen gas, the polymerization was performed at 60 ◦ C for 24 h. rPMDs were purified by the re-precipitation from the mixture of diethyl ether/chloroform, followed by vacuum drying. bPMDs were synthesized in our previous report via reversible addition−fragmentation chain transfer (RAFT) polymerization [13]
After the cycle of freezing–degassing–thawing and the bubbling of nitrogen gas, the polymerization was performed at 60 ◦ C for 6 h. bPMDs were purified by the re-precipitation from the mixture of diethyl ether/chloroform, followed by vacuum drying. rPMDs and bPMDs were characterized by 1 H NMR analysis using ECS-400 and ECX-400 spectrometers (JEOL Ltd., Tokyo, Japan) and gel permeation chromatography (GPC), whose results were presented in our previous report [13]
Summary
2-Methacryloyloxyethyl phosphorylcholine (MPC) polymers have been used as a coating agent on medical devices and as a carrier in drug delivery systems (DDSs). The self-assembling properties and PTX solubilization of random and block poly(MPC-co-DMA)s (rPMDs and bPMDs) with different compositions were examined and compared. Our results suggest that the self-assembling properties and the hydrophobicity of amphiphilic MPC polymers largely affect PTX solubilization as well as drug action, which is required to be controlled by the polymer sequence, as well as the structure and composition of the hydrophobic monomer for efficient DDS. It is known that the self-assembling properties of MPC copolymers depend on the structure and composition of hydrophobic monomers and the sequence in polymers [11,12,13,14,15,16,17]. Our previous report suggests that the self-assembling properties of PMDs are largely affected by the compositions of monomers and sequence in polymers [13].
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