Methoxy poly(ethylene glycol)-poly(lactide) nanoparticles encapsulating quercetin act as an effective anticancer agent by inducing apoptosis in breast cancer.

Abstract

PURPOSE:

To overcome the therapeutic restrictions offered by hydrophobic quercetin (Qu), this study aims to synthesize MPEG-PLA encapsulated Qu nanoparticle and to evaluate their anticancer efficacy.

MATERIALS AND METHODS:

In vitro anticancer potential and apoptotic studies were done by cell cytotoxicity assay and flow cytometry, respectively. MPEG-PLA-Qu nanoparticles were evaluated for anticancer efficacy in vivo using xenograft mice model. TUNEL assay was performed to observe the frequency of apoptotic cells in vivo.

RESULTS:

The hydrodynamic particle size, polydispersity index, zeta potential and drug loading % of MPEG-PLA-Qu nanoparticle was 155.3 ± 3.2 nm, 0.2 ± 0.05, -3.14 mV and 5.3 ± 1.1%, respectively. Also, MPEG-PLA-Qu showed sustained drug release for 10 days. In vitro results showed that MPEG-PLA-Qu could efficiently induce apoptosis in triple negative breast cancer cell line (MDA-MB-231) with higher amount of quercetin in cell lysate treated with MPEG-PLA-Qu in comparison to free quercetin. In xenograft model for breast cancer, peritumorally injected MPEG-PLA-Qu significantly inhibited the tumor growth. Moreover, TUNEL assay showed more occurrence of apoptotic cells in MPEG-PLA-Qu treated tumors compared to free quercetin at similar dose.

CONCLUSION:

Our data suggest that MPEG-PLA-Qu nanoparticle can have a promising clinical potential for the treatment of breast cancer.

• Authors: Garima Sharma, Jongbong Park, Ashish Ranjan Sharma, Jun-Sub Jung, Haesung Kim, Chiranjib Chakraborty, Dong-Keun Song, Sang-Soo Lee, Ju-Suk Nam
• Journal: Pharmaceutical research (Pharm Res) Vol. 32 Issue 2 Pg. 723-35 (Feb 2015) ISSN: 1573-904X [Electronic] United States
• PMID: 25186442 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antineoplastic Agents
• Drug Carriers
• Polyesters
• methoxy poly(ethylene glycol)-poly(lactide)
• Polyethylene Glycols
• Quercetin

Topics

• Animals
• Antineoplastic Agents (administration & dosage, chemistry)
• Apoptosis (drug effects, physiology)
• Breast Neoplasms (drug therapy, metabolism)
• Cell Line, Tumor
• Drug Carriers (administration & dosage, chemistry)
• Female
• Mice
• Mice, Inbred BALB C
• Nanoparticles (administration & dosage, chemistry)
• Polyesters (administration & dosage, chemistry)
• Polyethylene Glycols (administration & dosage, chemistry)
• Quercetin (administration & dosage, chemistry)
• Xenograft Model Antitumor Assays (methods)