Pharmacokinetics of curcumin-loaded PLGA and PLGA–PEG blend nanoparticles after oral administration in rats

[Display omitted] ► Curcumin was loaded in PLGA and PLGA–PEG blend nanoparticles. ► The nanoparticles prolonged extensively the curcumin release. ► All curcumin pharmacokinetic parameters were improved by nanoparticles. ► The PLGA–PEG nanoparticles presented the better performance in vivo. ► The ora...

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Published in:Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2013-01, Vol.101 (1), p.353-360
Main Authors: Khalil, Najeh Maissar, Nascimento, Thuane Castro Frabel do, Casa, Diani Meza, Dalmolin, Luciana Facco, Mattos, Ana Cristina de, Hoss, Ivonete, Romano, Marco Aurélio, Mainardes, Rubiana Mara
Format: Article
Language:English
Subjects:
Administration, Oral
Animals
Bioavailability
Biological Availability
Chromatography, High Pressure Liquid
colloids
Curcumin
Curcumin - administration & dosage
Curcumin - pharmacokinetics
Drug Compounding
encapsulation
Excipients
half life
LC–MS/MS
Male
Nanoparticles
oral administration
Particle Size
pharmacokinetics
Polyethylene Glycols
Polyglactin 910
Quality Control
Rats
Rats, Wistar
Reproducibility of Results
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Summary:[Display omitted] ► Curcumin was loaded in PLGA and PLGA–PEG blend nanoparticles. ► The nanoparticles prolonged extensively the curcumin release. ► All curcumin pharmacokinetic parameters were improved by nanoparticles. ► The PLGA–PEG nanoparticles presented the better performance in vivo. ► The oral bioavailability of curcumin was about 55.4-fold enhanced. The aim of this study was to assess the potential of nanoparticles to improve the pharmacokinetics of curcumin, with a primary goal of enhancing its bioavailability. Polylactic-co-glycolic acid (PLGA) and PLGA–polyethylene glycol (PEG) (PLGA–PEG) blend nanoparticles containing curcumin were obtained by a single-emulsion solvent-evaporation technique, resulting in particles size smaller than 200nm. The encapsulation efficiency was over 70% for both formulations. The in vitro release study showed that curcumin was released more slowly from the PLGA nanoparticles than from the PLGA–PEG nanoparticles. A LC–MS/MS method was developed and validated to quantify curcumin in rat plasma. The nanoparticles were orally administered at a single dose in rats, and the pharmacokinetic parameters were evaluated and compared with the curcumin aqueous suspension. It was observed that both nanoparticles formulations were able to sustain the curcumin delivery over time, but greater efficiency was obtained with the PLGA–PEG nanoparticles, which showed better results in all of the pharmacokinetic parameters analyzed. The PLGA and PLGA–PEG nanoparticles increased the curcumin mean half-life in approximately 4 and 6h, respectively, and the Cmax of curcumin increased 2.9- and 7.4-fold, respectively. The distribution and metabolism of curcumin decreased when it was carried by nanoparticles, particularly PLGA–PEG nanoparticles. The bioavailability of curcumin-loaded PLGA–PEG nanoparticles was 3.5-fold greater than the curcumin from PLGA nanoparticles. Compared to the curcumin aqueous suspension, the PLGA and PLGA–PEG nanoparticles increased the curcumin bioavailability by 15.6- and 55.4-fold, respectively. These results suggest that PLGA and, in particular, PLGA–PEG blend nanoparticles are potential carriers for the oral delivery of curcumin.
ISSN:0927-7765
1873-4367
DOI:10.1016/j.colsurfb.2012.06.024