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PLGA microspheres for the ocular delivery of a peptide drug, vancomycin using emulsification/spray-drying as the preparation method: in vitro/in vivo studies

Gavini, Elisabetta and Chetoni, Patrizia and Cossu, Massimo and Alvarez, Maria Gemma and Saettone, Marco Fabrizio and Giunchedi, Paolo (2004) PLGA microspheres for the ocular delivery of a peptide drug, vancomycin using emulsification/spray-drying as the preparation method: in vitro/in vivo studies. European Journal of Pharmaceutics and Biopharmaceutics, Vol. 57 (2), p. 207-212. ISSN 0939-6411. Article.

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DOI: 10.1016/j.ejpb.2003.10.018

Abstract

The aim of this study was an in vitro/in vivo investigation on poly(lactide-co-glycolide) (PLGA) microspheres as carriers for the topical ocular delivery of a peptide drug vancomycin (VA). The microspheres were prepared by an emulsification/spray-drying technique that can be proposed as an alternative to the double emulsion method for preparation of peptide-loaded microparticles. The drug encapsulation efficiencies were close to the theoretical values (84.2–99.5%); the average particle size, expressed as dvs, was about 11 μm. The microspheres were able to modulate the in vitro drug release of VA with a behavior dependent on their composition: the highest drug content corresponded to the highest release rate. In vivo studies were carried out by assessing the pharmacokinetic profile of VA in the aqueous humor of rabbits after topical administration of aqueous suspensions of microspheres. High and prolonged VA concentrations and increased AUC values (2-fold) with respect to an aqueous solution of the drug were observed. Increasing the viscosity of the microsphere suspension by addition of a suspending-viscosizing agent (hydroxypropylcellulose) did not produce an increase of the ocular bioavailability. PLGA microspheres can be proposed as a system for ocular delivery of peptide drugs.

Item Type:Article
ID Code:4801
Status:Published
Refereed:Yes
Uncontrolled Keywords:Poly(lactide-co-glycolide), peptide drug, Vancomycin, microspheres, emulsification/spray drying, in vivo studies, ocular delivery, aqueous humor
Subjects:Area 03 - Scienze chimiche > CHIM/09 Farmaceutico tecnologico applicativo
Divisions:001 Università di Sassari > 01 Dipartimenti > Scienze del farmaco
Publisher:Elsevier
ISSN:0939-6411
Copyright Holders: © 2003 Elsevier B.V.
Deposited On:12 Nov 2010 09:37

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