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In vitro and in vivo evaluation of a somatostatin analogue released from PLGA microspheres
Authors: Blanco-Prieto, M.J. (María José)
Besseghir, K. (Kamel)
Zerbe, O. (Oliver)
Andris, D. (Dani)
Orsolini, P. (Piero)
Heimgartner, F. (Fréderic)
Merkle, H.P. (Hans P.)
Gander, B. (Bruno)
Keywords: Somatostatin analogue
Release kinetics
Plasma levels
Issue Date: Jun-2000
Publisher: Elsevier
Publisher version:
ISSN: 0168-3659
Citation: Blanco-Prieto MJ, Besseghir K, Zerbe O, Andris D, Orsolini P, Heimgartner F, et al. In vitro and in vivo evaluation of a somatostatin analogue released from PLGA microspheres. J Control Release 2000 Jun 15;67(1):19-28.
The purpose of this study was to design poly(lactide-co-glycolide) (PLGA) microspheres for the continuous delivery of the somatostatin analogue, vapreotide, over 2–4 weeks. The microspheres were produced by spray-drying and the desired characteristics, i.e. high encapsulation efficiency and controlled release over 2–4 weeks, achieved through optimizing the type of polymer, processing solvent, and co-encapsulated additive. The in vitro release was tested in fetal bovine serum preserved with 0.02% of thiomersal. Furthermore, formulations were injected intramuscularly into rats to obtain pharmacokinetic profiles. Encapsulation efficiency was between 34 and 91%, depending on the particular formulation. The initial peptide release (within 6 h) was lowest, i.e. <20%, when acetic acid was used as processing solvent and highest, i.e. 57%, with dichloromethane. The various co-encapsulated additives generally lowered the encapsulation efficiency by 15–30%. The best formulation in terms of low burst and effective drug serum levels (>1 ng/ml) over 21–28 days in rats was the one made with end-group uncapped PLGA 50:50, the solvent acetic acid and the additive polyethyleneglycol. In conclusion, the optimization of formulation parameters allowed us to produce vapreotide-loaded PLGA microspheres of suitable characteristics for therapeutic use.
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