Transferrin-Conjugated Docetaxel-PLGA Nanoparticles for Tumor Targeting: Influence on MCF-7 Cell Cycle

• Type: Article in International Scientific Journal
• Date: 2019

Authors

Jose, S (Author) Other; Cinu, TA (Author) Other; Sebastian, R (Author) Other; Shoja, MH (Author) Other; Aleykutty, NA (Author) Other; Durazzo, A (Author) Other; Lucarini, M (Author) Other; Santini, A (Author) Other; Souto, EB (Author) Other

Journal

Title: Polymers

Vol. 11 No. 5 Article number 923

Final page: 1905

Publisher: MDPI

Indexing

ISI Web of Knowledge - 0 Citations

Scopus - 16 Citations

Other information

Authenticus ID: P-00R-EFC

DOI: 10.3390/polym11111905

Abstract (EN): Targeted drug delivery systems are commonly used to improve the therapeutic index of anti-cancer drugs by increasing their selectivity and reducing systemic distribution and toxicity. Ligand-conjugated nanoparticles (NPs) can be effectively applied for active chemotherapeutic targeting to overexpressed receptors of tumor cells. In this study, transferrin (Tf) was successfully conjugated with poly-l-lactic-co-glycolic acid (PLGA) using ethylene diamine confirmed by NMR, for the loading of docetaxel trihydrate (DCT) into PLGA nanoparticles (NPs). The DCT-loaded Tf-conjugated PLGA NPs were produced by an emulsion-solvent evaporation technique, and a 3(2) full factorial design was used to optimize the nanoparticle formulations. The DCT-loaded Tf-conjugated PLGA NPs were characterized by FTIR spectroscopy, differential scanning calorimetry, powder X-ray diffraction (PXRD), TEM, particle size, and zeta potential analysis. In vitro release kinetics confirmed that release of DCT from the designed formulations followed a zero-order kinetics and a diffusion controlled non-Fickian release profile. The DCT-loaded Tf-conjugated PLGA NPs were evaluated in vitro in MCF-7 cells for bioactivity assessment. Cytotoxicity studies confirmed that the Tf-conjugated PLGA NPs were more active than the non-conjugated counterparts. Cell uptake studies re-confirmed the ligand-mediated active targeting of the formulated NPs. From the cell cycle analysis, the anti-cancer activity of DCT-loaded Tf-conjugated PLGA NPs was shown to occur by arresting the G(2)/M phase.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 20