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|Title:||Transferrin-conjugated docetaxel-PLGA nanoparticles for tumor targeting: influence on MCF-7 cell cycle|
Cinu, Thomas A.
Shoja, M. H.
Aleykutty, N. A.
|Citation:||Jose, Sajan; Cinu, Thomas A.; Sebastian, Rosmy; Shoja, M. H.; Aleykutty, N. A.; Durazzo, Alessandra; Lucarini, Massimo; Santini, Antonello; Souto, Eliana, Transferrin-conjugated docetaxel-PLGA nanoparticles for tumor targeting: influence on MCF-7 cell cycle. Polymers, 11(11), 1905, 2019|
|Abstract(s):||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 32 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 G2/M phase.|
|Description:||Supplementary Materials: The following are available online at http://www.mdpi.com/2073-4360/11/11/1905/s1, Figure S1. FTIR spectrum of docetaxel trihydrate (DCT) (upper), of physical mixture of docetaxel trihydrate, transferrin (Tf) and PLGA (middle), and of DCT-loaded Tf-conjugated PLGA NPs (lower); Figure S2. DSC thermogram of PLGA (A), transferrin (B), docetaxel trihydrate (C), their physical mixture (D) and of DCT-loaded Tf-conjugated PLGA NPs (E); Figure S3. (A) X-ray diﬀraction pattern of docetaxel trihydrate, (B) physical mixture of docetaxel trihydrate, transferrin and PLGA, and of (C) DCT-loaded Tf-conjugated PLGA NPs. Figure S4. (A) Particle size distribution and average particle size and (B) zeta potential of DCT-loaded Tf-conjugated PLGA NPs.|
|Appears in Collections:||CEB - Publicações em Revistas/Séries Internacionais / Publications in International Journals/Series|
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