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AAPS PharmSciTech. 2007 June; 8(2): E105–E109.
Published online 2007 June 8. doi:  10.1208/pt0802043
PMCID: PMC2750358

Formation of acylated growth hormone-releasing peptide-6 by poly(lactide-co-glycolide) and its biological activity

Abstract

The purpose of this study was to investigate the formation of acylated impurity resulting from a chemical reaction between the growth hormone-releasing peptide-6 (GHRP-6) and poly(lactide-co-glycolide) (PLGA) and the effect of peptide acylation on the in vivo biological activity of GHRP-6. The peptide acylation pattern of GHRP-6 by hydrophilic PLGA polymers with different molecular weights was characterized by reversed-phase high-performance liquid chromatography and matrix-assisted laser desorption/ionization time-of-flight mass spectrometry. Higher levels of acylated GHRP-6 were produced with the higher molecular weight PLGA, which might be due to the slower degradation rate of the polymer. The evaluation of the biological activity in rats showed that the acylated GHRP-6 had a much lower activity than the intact GHRP-6. This finding suggests that the acylation reaction would decrease the effectiveness of the GHRP-6 formulation such as PLGA microspheres. There-fore, a strategy for stabilizing the GHRP-6 will be necessary for the development of a successful formulation of PLGA microspheres.

Keywords: Poly(lactide-co-glycolide), microspheres, peptide acylation, stability, growth hormone releasing peptide-6

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.
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