Preparation and characterization of protein loaded microspheres based on a hydroxylated aliphatic polyester, poly(lactic-co-hydroxymethyl glycolic acid)

The purpose of this study was to investigate the suitability of a novel hydroxylated aliphatic polyester, poly(lactic-co-hydroxymethyl glycolic acid) (PLHMGA), as controlled release system for pharmaceutical proteins. Dextran Blue (as a macromolecular model compound) and lysozyme-loaded PLHMGA and P...

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Bibliographic Details
Published in:Journal of controlled release 2009-08, Vol.138 (1), p.57-63
Main Authors: Ghassemi, A.H., van Steenbergen, M.J., Talsma, H., van Nostrum, C.F., Jiskoot, W., Crommelin, D.J.A., Hennink, W.E.
Format: Article
Language:English
Subjects:
Biological and medical sciences
Delayed-Action Preparations - chemical synthesis
Delayed-Action Preparations - chemistry
Dextran blue
Dextrans - administration & dosage
Dextrans - chemistry
General pharmacology
Hydroxylated aliphatic polyester
Lactic Acid - chemistry
Lysozyme
Medical sciences
Micrococcus - metabolism
Microspheres
Muramidase - administration & dosage
Muramidase - chemistry
Muramidase - metabolism
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
PLGA
Polyesters - chemical synthesis
Polyesters - chemistry
Polyglycolic Acid - chemistry
Porosity
Protein Conformation
Release
Surface Properties
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Summary:The purpose of this study was to investigate the suitability of a novel hydroxylated aliphatic polyester, poly(lactic-co-hydroxymethyl glycolic acid) (PLHMGA), as controlled release system for pharmaceutical proteins. Dextran Blue (as a macromolecular model compound) and lysozyme-loaded PLHMGA and PLGA (control formulation) microspheres were prepared by a solvent evaporation technique. The Dextran Blue and lysozyme loaded PLHMGA microspheres prepared with 10% polymer solution showed, because of a high porosity, a high burst release (35–75%) and the remaining content was released in a sustained manner for 15–20 days. The microspheres prepared with 15 and 20% polymer solution had a lower porosity and showed a pulsed release after day 8 and in 27 days they released more than 90% of Blue Dextran. The release of lysozyme was incomplete, likely due to aggregation of part of the encapsulated protein. Spectroscopic analysis of the released lysozyme indicated fully preserved secondary/tertiary structure and an enzyme activity assay showed that the specific activity of the released protein was maintained. An in vitro degradation study showed that the release of Blue Dextran and lysozyme is essentially controlled by the degradation of the microspheres. This study shows that microspheres made of the hydroxylated aliphatic polyester, poly(lactic-co-hydroxymethyl glycolic acid), are promising systems for the controlled release of pharmaceutical proteins. Degradation controlled release of lysozyme microspheres prepared form a hydroxylated polyester. [Display omitted]
ISSN:0168-3659
1873-4995
DOI:10.1016/j.jconrel.2009.04.025