Amphiphilic Copolymer of Polyhedral Oligomeric Silsesquioxane (POSS) Methacrylate for Solid Dispersion of Paclitaxel

Abstract

Suitable polymers for the homogeneous formulation of drug/polymer mixtures should be selected to correct the structural and physicochemical nature with a rapid dissolution rate. This study aimed to evaluate a copolymer prepared by the radical polymerization of 2-methacryloyloxyethyl phosphorylcholine (MPC) and a polyhedral oligomeric silsesquioxane (POSS) methacrylate bearing an ethyl (C2H5) group (MPC-ran-C2H5-POSS) as a carrier for the solid formulation of paclitaxel (PTX). A single-phase homogeneous formulation of PTX with the mixture of the MPC-ran-C2H5-POSS and polyvinylpyrrolidone (PVP) was prepared by a solvent method. The formulation of MPC-ran-C2H5-POSS/PVP/PTX enhanced the dissolution rate and the dissolved amount (approximately 90% within 40 min) without precipitation. The X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC) analysis confirmed the presence of PTX as an amorphous state. The amphiphilic nature of the MPC-ran-C2H5-POSS contributed to enhancing the aqueous solubility of PTX. The new formulation is applicable for solid dispersion technique via the supersaturation of PTX in an aqueous media.

Copolymers Composed of 2-(Methacryloyloxy)ethyl Phosphorylcholine and Methacrylated Polyhedral Oligomeric Silsesquioxane as a Simple Modifier for Liposomes

“…We studied random and diblock copolymers using MPC and polyhedral oligomeric silsesquioxane (POSS) methacrylate bearing different vertex (R-) groups (ethyl (C 2 ), hexyl (C 6 ), and octyl (C 8 )) as amphiphilic polymers (Figure ). The combination of POSS and its peripheral alkyl chain moiety is a key for controlling intra- and intermolecular interaction to form colloids and solid states. − Recently, the POSS moiety was also applied as a good hydrophobic part to deliver drug molecules and/or photosensitizer. , …”

Controlled Micelle Formation and Stable Capture of Hydrophobic Drug by Alkylated POSS Methacrylate Block Copolymers

“…In our previous studies, investigation on the copolymer developed through random polymerization of methacrylate POSS bearing different alkyl vertex groups as a hydrophobic monomer and MPC as hydrophilic monomer was performed. The POSS moieties enhanced the hydrophobicity of the copolymer at the water–polymer interface, enhanced the solubility of PTX in an aqueous environment, and enhanced the dissolution of PTX from solid formulation . However, the sequence of the POSS methacrylate and MPC cannot be controlled when using the random polymerization technique, so subsequently there was no control to achieve a desired size of polymeric micelles.…”

“…The POSS moieties enhanced the hydrophobicity of the copolymer at the water−polymer interface, 26 enhanced the solubility of PTX in an aqueous environment, 27 and enhanced the dissolution of PTX from solid formulation. 28 However, the sequence of the POSS methacrylate and MPC cannot be controlled when using the random polymerization technique, so subsequently there was no control to achieve a desired size of polymeric micelles.…”