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

B. Darvishi; S. Manoochehri; M. Esfandyari-Manesh; N. Samadi; M. Amini; F. Atyabi; R. Dinarvand

doi:10.1055/s-0034-1390487

Drug Research, Table of Contents

Drug Res (Stuttg) 2015; 65(12): 617-623
DOI: 10.1055/s-0034-1390487

Original Article

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

B. Darvishi

¹Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

²Nanotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran

,

S. Manoochehri

¹Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

²Nanotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran

,

M. Esfandyari-Manesh

²Nanotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran

³Department of Chemistry, Amirkabir University of Technology, Tehran, Iran

,

N. Samadi

⁴Drug and Food Control Department, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

,

M. Amini

⁵Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

,

F. Atyabi

¹Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

²Nanotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran

,

R. Dinarvand

¹Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

²Nanotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran

› Author Affiliations

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.

Key words

PLGA nanoparticles - albumin conjugation - 18-β-glycyrrhetinic acid - toxicity - antibacterial effect

Full Text

References

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