Synthesis and Characterization of PLGA-PEG Thymoquinone Nanoparticles and Its Cytotoxicity Effects in Tamoxifen-Resistan
Introduction: Drug resistance has been a continuous challenge in cancer treatment. The use of nanotechnology in the development of new cancer drugs has potential. One of the extensively studied compounds is thymoquinone (TQ), and this work aims to compare
- PDF / 961,114 Bytes
- 18 Pages / 504.567 x 720 pts Page_size
- 51 Downloads / 189 Views
Synthesis and Characterization of PLGAPEG Thymoquinone Nanoparticles and Its Cytotoxicity Effects in TamoxifenResistant Breast Cancer Cells Rozaina Ahmad, Noor Haida Mohd Kaus, and Shahrul Hamid Abstract
Introduction: Drug resistance has been a continuous challenge in cancer treatment. The use of nanotechnology in the development of new cancer drugs has potential. One of the extensively studied compounds is thymoquinone (TQ), and this work aims to compare two types of TQ-nanoformulation and its cytotoxicity toward resistant breast cancer cells. Method: TQ-nanoparticles were prepared and optimized by using two different formulations with different drugs to PLGAPEG ratio (1:20 and 1:7) and different PLGAPEG to Pluronic F68 ratio (10:1 and 2:1). The morphology and size were determined using TEM and DLS. Characterization of particles was done using UV-VIS, ATR-IR, entrapment efficiency, and drug release. The effects of drug, polymer, and surfactants were compared between the two formulations. Cytotoxicity assay was performed using MTS assay. R. Ahmad and S. Hamid (*) Oncological and Radiological Sciences Cluster, Advanced Medical and Dental Institute, Universiti Sains Malaysia, Bertam, Penang, Malaysia e-mail: [email protected]; [email protected] N. H. M. Kaus School of Chemical Sciences, Universiti Sains Malaysia, Minden, Penang, Malaysia e-mail: [email protected]
Results: TEM finding showed 96% of particles produced with 1:7 drug to PLGAPEG were less than 90 nm in size and spherical in shape. This was confirmed with DLS which showed smaller particle size than those formed with 1:20 drug to PLGA-PEG ratio. Further analysis showed zeta potential was negatively charged which could facilitate cellular uptake as reported previously. In addition, PDI value was less than 0.1 in both formulations indicating monodispersed and less broad in size distribution. The absorption peak of PLGA-PEG-TQNps was at 255 nm. The 1:7 drug to polymer formulation was selected for further analysis where the entrapment efficiency was 79.9% and in vitro drug release showed a maximum release of TQ of 50%. Cytotoxicity result showed IC50 of TQ-nanoparticle at 20.05 μM and free TQ was 8.25 μM. Conclusion: This study showed that nanoparticle synthesized with 1:7 drug to PLGAPEG ratio and 2:1 PLGA-PEG to Pluronic F68 formed nanoparticles with less than 100 nm and had spherical shape as confirmed with DLS. This could facilitate its transportation and absorption to reach its target. There was conserved TQ stability as exhibited slow release of this volatile oil. The TQ-nanoparticles showed selective cytotoxic effect toward UACC 732 cells compared to MCF-7 breast cancer cells.
R. Ahmad et al.
Keywords
Breast cancer · Drug resistance · Nanoparticle · Thymoquinone
Abbreviations ATRIR DLS EE ER HER2 IC50 MDR1 MRP4 MTS
PDI RPMI TEM TQ UVVIS β-actin
1
Attenuated Total Reflectance-Infrared Spectroscopy Dynamic Light Scattering Entrapment Efficiancy estrogen receptor Human Epidermal Growth Factor Receptor 2 Half maximal inhibitory concentration Mul
Data Loading...
