Shuqin Yu - PLGA nanoparticles Improve the Oral Bioavailability of Curcumin in Rats: Characterizations and Mechanisms

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        The overall goal of this paper was to develop   poly(lactic-co-glycolic   acid) nanoparticles (PLGA-NPs) of curcumin (CUR), named   CUR-PLGA-NPs, and to study the effect and mechanisms enhancing   the oral bioavailability of CUR. CUR-PLGA-NPs were prepared   according to a solid-in-oil-in-water (s/o/w) solvent evaporation   method and exhibited a smooth and spherical shape with diameters   of about 200 nm. Characterization of CUR-PLGA-NPs showed CUR was   successfully encapsulated on the PLGA polymer. The entrapment   efficiency and loading rate of CUR were 91.96 and 5.75%,   respectively. CUR-PLGA-NPs showed about 640-fold in water   solubility relative to that of n-CUR. A sustained CUR release to   a total of approximately 77% was discovered from CUR-PLGA-NPs in   artificial intestinal juice, but only about 48% in artificial   gastric juice. After oral administration of CUR-PLGA-NPs, the   relative bioavailability was 5.6-fold and had a longer half-life   compared with that of native curcumin. The results showed that   the effect in improving oral bioavailability of CUR may be   associated with improved water solubility, higher release rate in   the intestinal juice, enhanced absorption by improved   permeability, inhibition of P-glycoprotein (P-gp)-mediated   efflux, and increased residence time in the intestinal cavity.   Thus, encapsulating hydrophobic drugs on PLGA polymer is a   promising method for sustained and controlled drug delivery with   improved bioavailability of Biopharmaceutics Classification   System (BCS) class IV, such as CUR.


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