NSAID drugs release from injectable microspheres produced by supercritical fluid emulsion extraction.

Abstract:

:Supercritical fluid emulsion extraction is an innovative technology that uses supercritical carbon dioxide (SC-CO(2)) to extract the dispersed oily phase of an emulsion. This technology was used to produce poly-lactic-co-glycolic acid (PLGA) microspheres charged with two common NSAIDs: piroxicam (PX) and diclophenac sodium (DF). Single (O/W) and double (W/O/W) emulsions were tested and a comparative study between the characteristics of the microspheres obtained by SC-CO(2) extraction and the ones produced by conventional solvent evaporation (SE) is proposed. Varying the droplet dimensions, microspheres with mean diameters (MDs) of 1, 2, and 3 microm were obtained; however, the microspheres produced by SC-CO(2) gave always a better reproduction of the MD of original droplets because aggregation phenomena often modify the mean size and distribution of the microparticles produced by SE. Moreover, very efficient drug loadings (88% w/w of DF in PLGA using W/O/W emulsion and 97% of PX w/w in PLGA starting from O/W emulsion) were measured in the products obtained by SC-CO(2), respectively; whereas, the SE produced a drug loading of 30% in the case of double emulsion and of 70% for single emulsion. Solvent residue of 10 ppm was also measured by SC-CO(2) technology against the 600 ppm of the SE products. The release profiles of the entrapped drugs were also monitored to check the structure of the microspheres produced by this new technology.

journal_name

J Pharm Sci

authors

Della Porta G,Falco N,Reverchon E

doi

10.1002/jps.21920

subject

Has Abstract

pub_date

2010-03-01 00:00:00

pages

1484-99

issue

3

eissn

0022-3549

issn

1520-6017

pii

S0022-3549(15)32729-5

journal_volume

99

pub_type

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