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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

Authors

Deepak Kakde

Kuldeep Kumar Bansal

E. Peter Magennis

DEREK IRVINE derek.irvine@nottingham.ac.uk
Professor of Materials Chemistry



Abstract

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).

Citation

Kakde, D., Taresco, V., Bansal, K. K., Magennis, E. P., Howdle, S. M., Mantovani, G., …Alexander, C. (in press). 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, https://doi.org/10.1039/C6TB01839D

Journal Article Type Article
Acceptance Date Sep 28, 2016
Online Publication Date Sep 29, 2016
Deposit Date Nov 28, 2016
Publicly Available Date Nov 28, 2016
Journal Journal of Materials Chemistry B
Print ISSN 2050-750X
Electronic ISSN 2050-750X
Publisher Royal Society of Chemistry
Peer Reviewed Peer Reviewed
Volume 44
DOI https://doi.org/10.1039/C6TB01839D
Public URL http://eprints.nottingham.ac.uk/id/eprint/39006
Publisher URL http://pubs.rsc.org/en/Content/ArticleLanding/2016/TB/C6TB01839D#!divAbstract
Copyright Statement Copyright information regarding this work can be found at the following address: http://eprints.nottingham.ac.uk/end_user_agreement.pdf

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Kakde et al JMC 2016 AAM.pdf (840 Kb)
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Copyright Statement
Copyright information regarding this work can be found at the following address: http://eprints.nottingham.ac.uk/end_user_agreement.pdf





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