Stukenkemper, Timo, Dose, Anica, Caballo Gonzalez, Maria, Groenen, Alexander J.J., Hehir, Sarah, Andrés-Guerrero, Vanessa, Herrero Vanrell, Rocio and Cameron, Neil R. (2015) Block copolypeptide nanoparticles for the delivery of ocular therapeutics. Macromolecular Bioscience, 15 (1). pp. 138-145. doi:10.1002/mabi.201400471 ISSN 1616-5187.

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Abstract

Self-assembling block copolypeptides were prepared by sequential ring-opening polymerization of N-carboxyanhydride (NCA) derivatives of γ-benzyl-L-glutamic acid and ε-carbobenzyloxy-L-lysine, followed by selective deprotection of the benzyl glutamate block. The synthesized polymers had number average molecular weights close to theoretical values, and had low dispersities (ĐM = 1.15–1.28). Self-assembly of the amphiphilic block copolymers into nanoparticles was achieved using the “solvent-switch” method, whereby the polymer was dissolved in THF and water and the organic solvent removed by rotary evaporation. The type of nanostructures formed varied from spherical micelles to a mixture of spherical and worm-like micelles, depending on copolymer composition. The spherical micelles had an average diameter of 43 nm by dynamic light scattering, while the apparent diameter of the mixed phase system was around 200nm. Reproducibility of nanoparticle preparation was demonstrated to be excellent; almost identical DLS traces were obtained over three repeats. Following qualitative dye-solubilization experiments, the nanoparticles were loaded with the ocular anti-inflammatory drug dexamethasone. Loading efficiency of the nanoparticles was 90% and the cumulative drug release was 94% over 16 d, with a 20% burst release in the first 24 h.mabi201400471-gra-0001

Item Type:	Journal Article
Subjects:	R Medicine > RE Ophthalmology R Medicine > RS Pharmacy and materia medica
Divisions:	Faculty of Science, Engineering and Medicine > Engineering > Engineering
Library of Congress Subject Headings (LCSH):	Ophthalmic drugs, Eye -- Diseases -- Treatment, Polymerization, Nanoparticles, Polymeric drug delivery systems
Journal or Publication Title:	Macromolecular Bioscience
Publisher:	Wiley - V C H Verlag GmbH & Co. KGaA
ISSN:	1616-5187
Official Date:	January 2015
Dates:	Date Event January 2015 Published 17 December 2014 Available 17 November 2014 Accepted 26 October 2014 Submitted
Volume:	15
Number:	1
Page Range:	pp. 138-145
DOI:	10.1002/mabi.201400471
Status:	Peer Reviewed
Publication Status:	Published
Access rights to Published version:	Restricted or Subscription Access
Date of first compliant deposit:	19 January 2017
Date of first compliant Open Access:	20 January 2017
Funder:	Seventh Framework Programme (European Commission) (FP7)
Grant number:	NMP4-SL-2010-246180

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