Enhanced Cellular Cytotoxicity and Antibacterial Activity of 18-β-Glycyrrhetinic Acid by Albumin-conjugated PLGA Nanoparticles
| Autor: | Rassoul Dinarvand, Fatemeh Atyabi, Behrad Darvishi, Saeed Manoochehri, Mehdi Esfandyari-Manesh, Nasrin Samadi, Mohsen Amini |
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| Rok vydání: | 2015 |
| Předmět: |
Antineoplastic Agents
Microbial Sensitivity Tests chemistry.chemical_compound Differential scanning calorimetry Polylactic Acid-Polyglycolic Acid Copolymer Albumins Drug Discovery Zeta potential medicine Organic chemistry Humans Lactic Acid Fourier transform infrared spectroscopy Drug Carriers Chemistry technology industry and agriculture Albumin General Medicine Hep G2 Cells Human serum albumin Anti-Bacterial Agents Hep G2 PLGA Drug Liberation Glycyrrhetinic Acid Nanoparticles Drug Screening Assays Antitumor Antibacterial activity Polyglycolic Acid Nuclear chemistry medicine.drug |
| Zdroj: | Drug research. 65(12) |
| ISSN: | 2194-9387 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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