Abstract

Spatial distribution of bromobenzene (BrBz) and 4-bromophenol (BrPh) as hydrophobic aromatic compounds incorporated in polymer micelles with vesicular structure consisting of poly(ethylene glycol)-b-poly(tert-butyl methacrylate) (PEG-b-PtBMA) in aqueous solution is investigated by anomalous small-angle X-ray scattering (ASAXS) analyses near Br K edge. Small-angle X-ray scattering (SAXS) intensities from PEG-b-PtBMA micelles containing BrBz and BrPh were decreased as the energy of incident X-ray approached to Br K edge corresponding to the energy dependence of anomalous scattering factor of Br. The analysis for the energy dependence of SAXS profiles from the PEG-b-PtBMA micelles containing BrBz revealed that BrBz molecules were located in hydrophobic layer of PEG-b-PtBMA micelles. On the contrary, it was found by ASAXS that BrPh existed not only in the hydrophobic layer but also in the shell layer. Since ASAXS analysis successfully accomplished to visualize the spatial distribution of hydrophobic molecules in polymer micelles, it should be expected to be a powerful tool for characterization of drug delivery vehicles.

Highlights

  • When amphiphilic block copolymers are dissolved in aqueous solution, they undergo self-assembly into polymer micelles consisting of hydrophobic core and hydrated corona [1]

  • We focus on anomalous small-angle X-ray scattering (ASAXS), which is small-angle

  • K edge edge was was applied applied for for analyses analyses of of the the spatial spatial distribution distribution of of hydrophobic hydrophobic aromatic compounds

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Summary

Introduction

When amphiphilic block copolymers are dissolved in aqueous solution, they undergo self-assembly into polymer micelles consisting of hydrophobic core and hydrated corona [1].The polymer micelles have been expected to be drug carriers in drug delivery system (DDS) because they can uptake hydrophobic drug compounds in their hydrophobic cores in aqueous solution [2,3,4].For the DDS particles, stable retention of drug compounds is the critical issue to reduce side effects [5].The stability of retention of hydrophobic compounds should be related to their spatial distributions in polymer micelles. When amphiphilic block copolymers are dissolved in aqueous solution, they undergo self-assembly into polymer micelles consisting of hydrophobic core and hydrated corona [1]. The polymer micelles have been expected to be drug carriers in drug delivery system (DDS) because they can uptake hydrophobic drug compounds in their hydrophobic cores in aqueous solution [2,3,4]. For the DDS particles, stable retention of drug compounds is the critical issue to reduce side effects [5]. The stability of retention of hydrophobic compounds should be related to their spatial distributions in polymer micelles. It should be important to reveal the spatial distribution of hydrophobic compounds in polymer micelles. We focus on anomalous small-angle X-ray scattering (ASAXS), which is small-angle

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