Korean J Physiol Pharmacol.  2021 Sep;25(5):479-488. 10.4196/kjpp.2021.25.5.479.

Docetaxel-loaded PLGA nanoparticles to increase pharmacological sensitivity in MDA-MB-231 and MCF-7 breast cancer cells

Affiliations
  • 1College of Pharmacy, Chungnam National University, Daejeon 34134, Korea

Abstract

This study aimed to develop docetaxel (DTX) loaded poly(lactic-coglycolic acid) (PLGA) nanoparticles (DTX-NPs) and to evaluate the different pharmacological sensitivity of NPs to MCF-7 and MDA-MB-231 breast cancer cells. NPs containing DTX or coumarin-6 were prepared by the nanoprecipitation method using PLGA as a polymer and d-α-tocopherol polyethylene glycol 1000 succinate (TPGS) as a surfactant. The physicochemical properties of NPs were characterized. In vitro anticancer effect and cellular uptake were evaluated in breast cancer cells. The particle size and zeta potential of the DTX-NPs were 160.5 ± 3.0 nm and –26.7 ± 0.46 mV, respectively. The encapsulation efficiency and drug loading were 81.3 ± 1.85% and 10.6 ± 0.24%, respectively. The In vitro release of DTX from the DTX-NPs was sustained at pH 7.4 containing 0.5% Tween 80. The viability of MDA-MB-231 and MCF-7 cells with DTX-NPs was 37.5 ± 0.5% and 30.3 ± 1.13%, respectively. The IC 50 values of DTX-NPs were 3.92- and 6.75-fold lower than that of DTX for MDA-MB-231 cells and MCF-7 cells, respectively. The cellular uptake of coumarin-6-loaded PLGA-NPs in MCF-7 cells was significantly higher than that in MDA-MB-231 cells. The pharmacological sensitivity in breast cancer cells was higher on MCF-7 cells than on MDA-MB-231 cells. In conclusion, we successfully developed DTX-NPs that showed a great potential for the controlled release of DTX. DTX-NPs are an effective formulation for improving anticancer effect in breast cancer cells.

Keyword

Breast cancer; Cell viability; Docetaxel; Nanoparticles

Figure

  • Fig. 1 Transmission electron microscopy of DTX-NPs. DTX-NPs, docetaxel loaded poly(lactic-co-glycolic acid) nanoparticles.

  • Fig. 2 DSC (A) and FTIR spectra (B) of DTX, PLGA, TPGS, and DTX-NPs. DSC, differential scanning calorimetry; FTIR, Fourier-transform infrared spectroscopy; DTX, docetaxel; PLGA, poly(lactic-co-glycolic acid); TPGS, tocopherol polyethylene glycol succinate; DTX-NPs, docetaxel loaded poly(lactic-co-glycolic acid) nanoparticles.

  • Fig. 3 In vitro dissolution release of DTX-NPs in PBS pH 7.4 containing 0.5% Tween 80. Results were represented as mean ± SD (n = 3). DTX, docetaxel; DTX-NPs, docetaxel loaded poly(lactic-co-glycolic acid) nanoparticles; PBS, phosphate-buffered saline.

  • Fig. 4 In vitro anticancer effect of DTX-NPs in MDA-MB-231 (A) and MCF-7 (B) cells. Results were represented as mean ± SD (n = 3). DTX, docetaxel; DTX-NPs, docetaxel loaded poly(lactic-co-glycolic acid) nanoparticles; IC50, half-maximal inhibitory concentration.

  • Fig. 5 Quantitative cellular uptake of coumarin-6-loaded PLGA-NPs in breast cancer cells (MDA-MB-231 and MCF-7 cells). Results were expressed as mean ± SD (n = 3). PLGA-NPs, poly(lactic-co-glycolic acid) nanoparticles. p < 0.05 (*) indicated statistical significance.

  • Fig. 6 Stability of DTX-NPs after 3 months: (A) Particle size, (B) Polydispersity index (PDI), and (C) Zeta potential. Results were represented as mean ± SD (n = 3). DTX-NPs, docetaxel loaded poly(lactic-co-glycolic acid) nanoparticles.


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