Drug Res (Stuttg) 2015; 65(12): 617-623
DOI: 10.1055/s-0034-1390487
Original Article
© Georg Thieme Verlag KG Stuttgart · New York

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

B. Darvishi
1   Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
2   Nanotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran
,
S. Manoochehri
1   Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
2   Nanotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran
,
M. Esfandyari-Manesh
2   Nanotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran
3   Department of Chemistry, Amirkabir University of Technology, Tehran, Iran
,
N. Samadi
4   Drug and Food Control Department, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
,
M. Amini
5   Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
,
F. Atyabi
1   Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
2   Nanotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran
,
R. Dinarvand
1   Department of Pharmaceutics, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
2   Nanotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran
› Author Affiliations
Further Information

Publication History

received 06 April 2014

accepted 02 September 2014

Publication Date:
21 January 2015 (online)

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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.