PMID- 23010041 OWN - NLM STAT- MEDLINE DCOM- 20130509 LR - 20181202 IS - 1873-4367 (Electronic) IS - 0927-7765 (Linking) VI - 101 DP - 2013 Jan 1 TI - Pharmacokinetics of curcumin-loaded PLGA and PLGA-PEG blend nanoparticles after oral administration in rats. PG - 353-60 LID - S0927-7765(12)00365-7 [pii] LID - 10.1016/j.colsurfb.2012.06.024 [doi] AB - 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 200 nm. 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 C(max) 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. CI - Copyright (c) 2012 Elsevier B.V. All rights reserved. FAU - Khalil, Najeh Maissar AU - Khalil NM AD - Department of Pharmacy, Universidade Estadual do Centro-Oeste/UNICENTRO, Guarapuava, PR, Brazil. FAU - do Nascimento, Thuane Castro Frabel AU - do Nascimento TC FAU - Casa, Diani Meza AU - Casa DM FAU - Dalmolin, Luciana Facco AU - Dalmolin LF FAU - de Mattos, Ana Cristina AU - de Mattos AC FAU - Hoss, Ivonete AU - Hoss I FAU - Romano, Marco Aurelio AU - Romano MA FAU - Mainardes, Rubiana Mara AU - Mainardes RM LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't DEP - 20120628 PL - Netherlands TA - Colloids Surf B Biointerfaces JT - Colloids and surfaces. B, Biointerfaces JID - 9315133 RN - 0 (Excipients) RN - 0 (poly(lactic-glycolic acid)-poly(ethyleneglycol) copolymer) RN - 34346-01-5 (Polyglactin 910) RN - 3WJQ0SDW1A (Polyethylene Glycols) RN - IT942ZTH98 (Curcumin) SB - IM MH - Administration, Oral MH - Animals MH - Biological Availability MH - Chromatography, High Pressure Liquid MH - Curcumin/administration & dosage/*pharmacokinetics MH - Drug Compounding MH - Excipients MH - Male MH - Nanoparticles MH - Particle Size MH - Polyethylene Glycols MH - Polyglactin 910 MH - Quality Control MH - Rats MH - Rats, Wistar MH - Reproducibility of Results EDAT- 2012/09/27 06:00 MHDA- 2013/05/10 06:00 CRDT- 2012/09/27 06:00 PHST- 2012/03/02 00:00 [received] PHST- 2012/06/10 00:00 [revised] PHST- 2012/06/12 00:00 [accepted] PHST- 2012/09/27 06:00 [entrez] PHST- 2012/09/27 06:00 [pubmed] PHST- 2013/05/10 06:00 [medline] AID - S0927-7765(12)00365-7 [pii] AID - 10.1016/j.colsurfb.2012.06.024 [doi] PST - ppublish SO - Colloids Surf B Biointerfaces. 2013 Jan 1;101:353-60. doi: 10.1016/j.colsurfb.2012.06.024. Epub 2012 Jun 28.