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Research Article

Long-circulating poly(ethylene glycol)-coated poly(lactid-co-glycolid) microcapsules as potential carriers for intravenously administered drugs

, , , &
Pages 632-642 | Received 07 Aug 2012, Accepted 07 Jan 2013, Published online: 14 Mar 2013
 

Abstract

The intrinsic advantages of microcapsules with regard to nanocapsules as intravenous drug carrier systems are still not fully exploited. Especially, in clinical situations where a long-term drug release within the vascular system is desired, if large amounts of drug have to be administered or if capillary leakage occurs, long-circulating microparticles may display a superior alternative to nanoparticles. Here, microcapsules were synthesised and parameters such as in vitro tendency of agglomeration, protein adsorption and in vivo performance were investigated. Biocompatible poly(ethylene glycol) (PEG)-coated poly(DL-lactide-co-glycolide) (PLGA) as wall material, solid and perfluorodecalin (PFD)-filled PEG–PLGA microcapsules (1.5 µm diameter) were manufactured by using a modified solvent evaporation method with either 1% poly(vinyl alcohol) (PVA) or 1.5% cholate as emulsifying agents. Compared to microcapsules manufactured with cholate, the protein adsorption (albumin and IgG) was clearly decreased and agglomeration of capsules was prevented, when PVA was used. The intravenous administration of these microcapsules, both solid and PFD-filled, in rats was successful and exhibited a circulatory half-life of about 1 h. Our data clearly demonstrate that PEG–PLGA microcapsules, manufactured by using PVA, are suitable biocompatible, long-circulating drug carriers, applicable for intravenous administration.

Abbreviations
Au=

arbitrary units

DTPA=

diethylenetriaminepentaacetic acid

FITC-dextran=

fluorescein isothiocyanate-dextran

Hb=

haemoglobin

IgG=

immunoglobulin G, F-albumin, albumin-fluorescein isothiocyanate conjugate

F-IgG=

fluorescence-labelled IgG

LSM=

laser-scanning microscopy

PBS=

phosphate buffered saline

PEG=

poly(ethylene glycol)

PFD=

perfluorodecalin

PLGA=

poly(DL-lactide-co-glycolide)

PVA=

poly(vinyl alcohol)

r=

radius

RES=

reticuloendothelial system

SEM=

scanning electron microscopy

SDS=

sodium dodecyl sulphate

v=

volume

Abbreviations
Au=

arbitrary units

DTPA=

diethylenetriaminepentaacetic acid

FITC-dextran=

fluorescein isothiocyanate-dextran

Hb=

haemoglobin

IgG=

immunoglobulin G, F-albumin, albumin-fluorescein isothiocyanate conjugate

F-IgG=

fluorescence-labelled IgG

LSM=

laser-scanning microscopy

PBS=

phosphate buffered saline

PEG=

poly(ethylene glycol)

PFD=

perfluorodecalin

PLGA=

poly(DL-lactide-co-glycolide)

PVA=

poly(vinyl alcohol)

r=

radius

RES=

reticuloendothelial system

SEM=

scanning electron microscopy

SDS=

sodium dodecyl sulphate

v=

volume

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