Folate-conjugated human serum albumin-encapsulated resveratrol nanoparticles: preparation, characterization, bioavailability and targeting of liver tumors

Abstract

This work investigated the preparation of specific targeted drug delivery systems in cancer chemotherapy by folate conjugated human serum albumin nanoparticles encapsulated resveratrol (RES) nanoparticles (FA-HSA-RESNPs). FA was coupled to HSA, and RES was encapsulated in FA-conjugated HSA by high pressure fluid nano-homogeneous emulsification. The average particle size and polydispersity index of NPs prepared under optimal conditions were 102.1 ± 4.9 nm and 0.001. The drug capsulation efficiency and drug loading efficiency were 98.36 and 14.66%, respectively. The analysis of the results of the physical characterization showed that the RES was present in the FA-HSA-RESNPs in an amorphous state. In vitro drug-release study showed that the NPs can release the drug persistently and slowly. The inhibition rate of FA-HSA-RESNPs and RES was detected using the 3-(4,5-dimethylthiazol-2-yl)-2,5diphenyl-2H-tetrazolium bromide method to be 110.8 and 157.2 lM, respectively. The targeting ability of the FA-HSA-RESNPs for the HepG2 cell was measured by fluorescein isothiocyanate-modified albumin techniques. The uptake rate of FA-HSA-RESNPs was higher than that of the original RES. By using near-infrared imaging, in vivo activity was labeled with Cy5 fluorescent FA-HSA-RESNP confirmed FA-HSA-RESNP tumor-targeting ability. The intravenous administration bioavailability of FA-HSA-RESNPs was about 5.95-fold higher than that of the original RES.

The Potential Use of Resveratrol for Cancer Prevention

“…In addition, bioavailability of RSV-loaded HSA-FA nanoparticles turned out to be six times higher than the free polyphenol and no toxic effects of RSV-loaded HSA-FA nanoparticles were detected on healthy rat organs. In contrast, the decrease in size of the tumor was not mentioned [63].…”

“…The incorporation of a cancer-targeting ligand directly into nanoparticle structures is another way to promote drug release more selectively to cancer cells. Thereby, nanoparticles have been obtained by coupling human serum albumin (HSA), a non-toxic carrier of weakly soluble drugs and folic acid (FA) a cancer-targeting ligand [63]. Antitumoral activities of RSV-loaded HSA-FA nanoparticles were evaluated in in vitro assays of human liver cancer HepG2 cells and in in vivo experiments on H22 tumor-bearing mice.…”

Resveratrol-Based Nanoformulations as an Emerging Therapeutic Strategy for Cancer

“…Multiple studies have shown that resveratrol encapsulated in diverse nanoparticles provides the protection for resveratrol against UV light via improving bioavailability in different targets (Summerlin et al, 2015 ). Furthermore, resveratrol-loaded liposomes have shown to be effective anti-proliferative agents in brain cancer cells such as U-87 MG cells through inhibiting cell growth and inducing apoptosis in nude mice (Teskač and Kristl, 2010 ; Duarte et al, 2015 ; Summerlin et al, 2015 ; Jhaveri et al, 2018 ; Latruffe and Vervandier-Fasseur, 2018 ; Lian et al, 2019 ). In addition, the combination of resveratrol and 5-fluorouracil- (5-FU) loaded ultradeformable liposomes in an ex vivo study showed the ability to penetrate and deposit in the deep porcine skin layer.…”

Formulation of Folate-conjugated, Doxorubicin-loaded Human Serum Albumin Nanoparticles for Promotion of Gene Expression Associated with Apoptosis in Renal Cell Carcinoma

“…Although the utilization of organic solvents to prepare NPs is preferred, many materials are di cult to dissolve in both water and organic solvent. One way to prepare such NPs without applying organic solvents is to use ethanol [23].…”