Amphiphilic block copolymers from a renewable Ɛ-decalactone monomer: prediction and characterization of micellar core effects on drug encapsulation and release

Here we describe a methoxy poly(ethyleneglycol)-b-poly(ε-decalactone) (mPEG-b-PεDL) copolymer and investigate the potential of the copolymer as a vehicle for solubilisation and sustained release of indomethacin (IND). The indomethacin loading and release from mPEG-b-PεDL micelles (amorphous cores) w...

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Main Authors: Kakde, Deepak, Taresco, Vincenzo, Bansal, Kuldeep Kumar, Magennis, E. Peter, Howdle, Steven M., Mantovani, Giuseppe, Irvine, Derek J., Alexander, Cameron
Format: Article
Published: Royal Society of Chemistry 2016
Online Access:https://eprints.nottingham.ac.uk/39006/
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author Kakde, Deepak
Taresco, Vincenzo
Bansal, Kuldeep Kumar
Magennis, E. Peter
Howdle, Steven M.
Mantovani, Giuseppe
Irvine, Derek J.
Alexander, Cameron
author_facet Kakde, Deepak
Taresco, Vincenzo
Bansal, Kuldeep Kumar
Magennis, E. Peter
Howdle, Steven M.
Mantovani, Giuseppe
Irvine, Derek J.
Alexander, Cameron
author_sort Kakde, Deepak
building Nottingham Research Data Repository
collection Online Access
description Here we describe a methoxy poly(ethyleneglycol)-b-poly(ε-decalactone) (mPEG-b-PεDL) copolymer and investigate the potential of the copolymer as a vehicle for solubilisation and sustained release of indomethacin (IND). The indomethacin loading and release from mPEG-b-PεDL micelles (amorphous cores) was compared against methoxy poly(ethyleneglycol)-b-poly(ε-caprolactone)(mPEG-b-PCL) micelles (semicrystalline cores). The drug–polymer compatibility was determined through a theoretical approach to predict drug incorporation into hydrated micelles. Polymer micelles were prepared by solvent evaporation and characterised for size, morphology, indomethacin loading and release. All the formulations generated spherical micelles but significantly larger mPEG-b-PεDL micelles were observed compared to mPEG-b-PCL micelles. A higher compatibility of the drug was predicted for PCL cores based on Flory–Huggins interaction parameters (χsp) using the Hansen solubility parameter (HSP) approach, but higher measured drug loadings were found in micelles with PεDL cores compared to PCL cores. This we attribute to the higher amorphous content in the PεDL-rich regions which generated higher micellar core volumes. Drug release studies showed that the semicrystalline PCL core was able to release IND over a longer period (80% drug release in 110 h) compared to PεDL core micelles (80% drug release in 72 h).
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spelling nottingham-390062020-05-04T18:09:13Z https://eprints.nottingham.ac.uk/39006/ Amphiphilic block copolymers from a renewable Ɛ-decalactone monomer: prediction and characterization of micellar core effects on drug encapsulation and release Kakde, Deepak Taresco, Vincenzo Bansal, Kuldeep Kumar Magennis, E. Peter Howdle, Steven M. Mantovani, Giuseppe Irvine, Derek J. Alexander, Cameron Here we describe a methoxy poly(ethyleneglycol)-b-poly(ε-decalactone) (mPEG-b-PεDL) copolymer and investigate the potential of the copolymer as a vehicle for solubilisation and sustained release of indomethacin (IND). The indomethacin loading and release from mPEG-b-PεDL micelles (amorphous cores) was compared against methoxy poly(ethyleneglycol)-b-poly(ε-caprolactone)(mPEG-b-PCL) micelles (semicrystalline cores). The drug–polymer compatibility was determined through a theoretical approach to predict drug incorporation into hydrated micelles. Polymer micelles were prepared by solvent evaporation and characterised for size, morphology, indomethacin loading and release. All the formulations generated spherical micelles but significantly larger mPEG-b-PεDL micelles were observed compared to mPEG-b-PCL micelles. A higher compatibility of the drug was predicted for PCL cores based on Flory–Huggins interaction parameters (χsp) using the Hansen solubility parameter (HSP) approach, but higher measured drug loadings were found in micelles with PεDL cores compared to PCL cores. This we attribute to the higher amorphous content in the PεDL-rich regions which generated higher micellar core volumes. Drug release studies showed that the semicrystalline PCL core was able to release IND over a longer period (80% drug release in 110 h) compared to PεDL core micelles (80% drug release in 72 h). Royal Society of Chemistry 2016-09-29 Article PeerReviewed Kakde, Deepak, Taresco, Vincenzo, Bansal, Kuldeep Kumar, Magennis, E. Peter, Howdle, Steven M., Mantovani, Giuseppe, Irvine, Derek J. and Alexander, Cameron (2016) Amphiphilic block copolymers from a renewable Ɛ-decalactone monomer: prediction and characterization of micellar core effects on drug encapsulation and release. Journal of Materials Chemistry B, 44 . pp. 7119-7129. ISSN 2050-750X http://pubs.rsc.org/en/Content/ArticleLanding/2016/TB/C6TB01839D#!divAbstract doi:10.1039/C6TB01839D doi:10.1039/C6TB01839D
spellingShingle Kakde, Deepak
Taresco, Vincenzo
Bansal, Kuldeep Kumar
Magennis, E. Peter
Howdle, Steven M.
Mantovani, Giuseppe
Irvine, Derek J.
Alexander, Cameron
Amphiphilic block copolymers from a renewable Ɛ-decalactone monomer: prediction and characterization of micellar core effects on drug encapsulation and release
title Amphiphilic block copolymers from a renewable Ɛ-decalactone monomer: prediction and characterization of micellar core effects on drug encapsulation and release
title_full Amphiphilic block copolymers from a renewable Ɛ-decalactone monomer: prediction and characterization of micellar core effects on drug encapsulation and release
title_fullStr Amphiphilic block copolymers from a renewable Ɛ-decalactone monomer: prediction and characterization of micellar core effects on drug encapsulation and release
title_full_unstemmed Amphiphilic block copolymers from a renewable Ɛ-decalactone monomer: prediction and characterization of micellar core effects on drug encapsulation and release
title_short Amphiphilic block copolymers from a renewable Ɛ-decalactone monomer: prediction and characterization of micellar core effects on drug encapsulation and release
title_sort amphiphilic block copolymers from a renewable ɛ-decalactone monomer: prediction and characterization of micellar core effects on drug encapsulation and release
url https://eprints.nottingham.ac.uk/39006/
https://eprints.nottingham.ac.uk/39006/
https://eprints.nottingham.ac.uk/39006/