<p>Evaluation of Intestinal Absorption Mechanism and Pharmacokinetics of Curcumin-Loaded Galactosylated Albumin Nanoparticles</p>

Abstract

BackgroundMost of the oral drugs have the properties of weak intestinal absorption and low bioavailability, which leads to little treatment to diseases. By nanotechnology, these drugs can be efficiently delivered to pass biological barriers and promote the cell uptake ability for the enhancement of the oral bioavailability.MethodsThe present work chose the prepared curcumin-loaded galactosylated albumin nanoparticles (Gal-BSA NPs) as the nano-drug samples to study the intestinal capacity and the oral bioavailability.ResultsThe cell uptake assay showed that the Gal-BSA NPs could promote the internalization of more curcumin into the Caco-2 cells. Moreover, the cell uptake mechanism of Gal-BSA-Cur NPs depended on the clathrin-mediated endocytosis transport. The intestinal permeation assay using one Ussing chamber exhibited that the absorptive amounts of curcumin in Gal-BSA-Cur NPs group were 1.5-fold of pure curcumin group. Meanwhile, the permeation mechanism of Gal-BSA-Cur NPs across the intestine mainly depended on the passive transport. The pharmacokinetics study in vivo suggested that the oral bioavailability of Gal-BSA-Cur NPs was improved by 1.4-fold compared with pure curcumin.ConclusionAll results demonstrated that Gal-BSA NPs could improve the intestinal absorption capacity and oral bioavailability of curcumin through the double absorption mechanisms of the clathrin-mediated endocytosis and the passive transport.

Endocytosis: The Nanoparticle and Submicron Nanocompounds Gateway into the Cell

“…Albumin-based based NPs are widely employed due to properties such as high-water solubility and biocompatibility, and low toxicity and immunogenicity. Furthermore, these NPs have got many carboxylic and amino groups that can be used as binding sites for drugs [29]. These NPs enter the cells mainly by CME, independently of their charge.…”

“…That is the case for electronegative bovine serum albumin (BSA) 150 nm sized NPs loaded with gemcitabine in MIA PaCa-2 and PANC-1 human pancreatic carcinoma cell lines [30]. CME is also the main uptake pathway for electropositive human serum albumin (HSA)-based NPs loaded with lapatinib in SK-BR-3 human breast adenocarcinoma cells, having an approximated size of 140 nm [31] and in modified albumin NPs as galactosylated curcumin-loaded BSA NPs (Gal-BSA-Cur) in human colon adenocarcinoma Caco-2 cells [29]. On the other hand, for electronegative plasmid loaded has-based NPs, having a size of 120 nm, the uptake is carried out mainly by CVME in cultured human retinal pigment epithelial (ARPE-19) cells [32].…”

Geniposide in Gardenia jasminoides var. radicans Makino modulates blood pressure via inhibiting WNK pathway mediated by the estrogen receptors

“…[54] In addition, poloxamer and galactosylated albumin nanoparticles may improve the oral bioavailability of geniposide. [55,56] In regard to tissue distribution after oral administration, the AUC 0 → 4 h values of geniposide were calculated as the order of kidney > spleen > liver > heart > lung > brain. [57] In a metabolic profile experiment, male SD rats were orally administrated with geniposide at 350 mg/kg.…”

Cancer Therapy Challenge: It Is Time to Look in the “St. Patrick’s Well” of the Nature

“…EGCG is also able to repress the androgen receptor (AR) hormone response by the reduction of AR acetylation. This phenomenon determines a reduction of prostate cancer cells’ growth, promoting apoptosis [ 178 ]. Moreover, EGCG has been also described as a potential epigenetic modifier of HDACs, restoring epigenetically silenced genes in cervical and skin tumors.…”