Enhanced Cellular Cytotoxicity and Antibacterial Activity of 18-β-Glycyrrhetinic Acid by Albumin-conjugated PLGA Nanoparticles

Abstract

The aim of the present work was to encapsulate 18-β-Glycyrrhetinic acid (GLA) in albumin conjugated poly(lactide-co-glycolide) (PLGA) nanoparticles by a modified nanoprecipitation method. Nanoparticles (NPs) were prepared by different drug to polymer ratios, human serum albumin (HSA) content, dithiothreitol (as producer of free thiol groups) content, and acetone (as non-solvent in nanoprecipitation). NPs with a size ranging from 126 to 174 nm were achieved. The highest entrapment efficiency (89.4±4.2%) was achieved when the ratio of drug to polymer was 1:4. The zeta potential of NPs was fairly negative (-8 to -12). Fourier transform infrared spectroscopy and differential scanning calorimetry proved the conjugation of HSA to PLGA NPs. In vitro release profile of NPs showed 2 phases: an initial burst for 4 h (34-49%) followed by a slow release pattern up to the end. The antibacterial effects of NPs against Staphylococcus aureus, Staphylococcus epidermidis and Pseudomonas aeruginosa were studied by microdilution method. The GLA-loaded NPs showed more antibacterial effect than pure GLA (2-4 times). The anticancer MTT test revealed that GLA-loaded NPs were approximately 9 times more effective than pure GLA in Hep G2 cells.

Physicochemical characterization and antimicrobial evaluation of gentamicin-loaded CaCO3 nanoparticles prepared via microemulsion method

“…It can happen because of an error in actual viscosity in Stokes-Einstein equation for DLS technique[40]. Similar observations have been reported by other researchers[41,42].…”

“…Some mechanisms of nanoparticle-based antimicrobial activity have been reported by investigators [42,79]. Nanoparticles can fuse with the bacterial cell wall and accordingly the antimicrobial agent is released across the cell wall and cell membrane.…”

“…Nanoparticles can also adsorb to the cell wall and act as a drug depot, which continuously release the antimicrobial agent. The released drug can diffuse into the interior compartments of the bacteria [42,79].…”

Ciprofloxacin HCl-loaded calcium carbonate nanoparticles: preparation, solid state characterization, and evaluation of antimicrobial effect against Staphylococcus aureus

“…Nanoparticles can fuse with the bacterial cell wall and subsequently the drug is released across the cell wall and cell membrane. Adsorption of the nanoparticles to the bacterial cell wall can be another mechanism which provides a sustained antimicrobial activity of the incorporated antibiotic against the microorganisms (Darvishi et al 2014, Zhang et al 2010. Antibiotic-loaded nanoparticles can also attract to the infection site and not only release the drug at the infection site but also, after phagocytosis of the pathogen, expose it to the high intracellular drug concentrations (Nokhodchi et al 2012, Salouti andAhangari 2014).…”

18 β-glycyrrhetinic acid exhibits potent antitumor effects against colorectal cancer via inhibition of cell proliferation and migration

“…The 18 β-glycyrrhetinic acid (GRA) ( Fig. 1), a pentacyclic triterpenoid extracted from the root of Licorice, has been shown to display multiple physiological functions, such as anti-microbial (1,2), anti-inflammatory (3,4), anti-viral (5), anti-ulcer (6) and hepatoprotective effects (3). Recently, the antitumor effect of GRA has been extensively investigated in vitro and in vivo in breast (7,8), ovarian cancer (9), promyelocytic leukemia (10), hepatoma and stomach cancer cells (11).…”