The in vitro stability of air-filled polybutylcyanoacrylate microparticles.
Different methods of manufacturing permitted the production of air-filled PBCA microparticles (af-pbca-mp) with different physical properties such as size and wall thickness. These differences led to distinctions with respect to mechanical stability and, at the same time, to different levels of biochemical stability when incubated in biofluids. Microparticles, designed as they are to be mechanically more stable (composed of larger nanoparticles resulting in thicker shell wall, no surface hydrolysis), persist longer under in vitro conditions in biofluids such as serum, plasma and whole blood than do the more fragile ones. It was possible when using the measurement of ultrasound attenuation to characterize af-pbca-mp degradation with respect to the disappearance of the ultrasound properties of the particles and therefore to find out how long different formulations can be expected to be active as contrast agents under simulated in vivo conditions. The present examination showed that using either serum, plasma or whole blood leads to results with the same tendencies in terms of the stability and durability of af-pbca-mp in the media, mimicking in vivo conditions. It was thus possible to validate successfully the use of either serum or plasma as substitutes for whole blood. Further studies dealing with the in vitro in vivo correlation will be needed to find out if the situation in this in vitro assay corresponds to the situation in the body.
Schering AG, Research Laboratories, Müllerstrasse 178, D-13342, Berlin. carsten.olbrich@schering.de
Carsten
C
Olbrich
Peter
P
Hauff
Frank
F
Scholle
Wolfgang
W
Schmidt
Udo
U
Bakowsky
Andreas
A
Briel
Michael
M
Schirner
D000388:Air; D001672:Biocompatible Materials / Q000737:chemistry / Q000493:pharmacokinetics; D001673:Biodegradation, Environmental; D001769:Blood; D002214:Capsules; D003287:Contrast Media; D004355:Drug Stability; D004659:Enbucrilate / Q000737:chemistry / Q000493:pharmacokinetics; D006801:Humans; D066298:In Vitro Techniques; D008422:Materials Testing; D008855:Microscopy, Electron, Scanning; D010316:Particle Size
D001672:Biocompatible Materials; D002214:Capsules; D003287:Contrast Media; D004659:Enbucrilate