Formulation, Characterization and Cytotoxicity Effects of Novel Thymoquinone-PLGA-PF68 Nanoparticles.

Nurul Shahfiza Noor,Myron R Szewczuk,Shahrul Bariyah Sahul Hamid,Noor Haida Mohd Kaus

doi:10.3390/ijms22179420

Nurul Shahfiza Noor, Myron R Szewczuk + Show 2 more

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https://doi.org/10.3390/ijms22179420

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Abstract

Thymoquinone has anti-cancer properties. However, its application for clinical use is limited due to its volatile characteristics. The current study aims to develop a polymeric nanoformulation with PLGA-PEG and Pluronics F68 as encapsulants to conserve thymoquinone’s (TQ) biological activity before reaching the target sites. Synthesis of nanoparticles was successfully completed by encapsulating TQ with polymeric poly (D, L-lactide-co-glycolide)-block-poly (ethylene glycol) and Pluronics F68 (TQ-PLGA-PF68) using an emulsion–solvent evaporation technique. The size and encapsulation efficiency of TQ-PLGA-PF68 nanoparticles were 76.92 ± 27.38 nm and 94%, respectively. TQ released from these encapsulants showed a biphasic released pattern. Cytotoxicity activity showed that tamoxifen-resistant (TamR) MCF-7 breast cancer cells required a higher concentration of TQ-PLGA-PF68 nanoparticles than the parental MCF-7 cells to achieve IC50 (p < 0.05). The other two resistant subtypes (TamR UACC732 inflammatory breast carcinoma and paclitaxel-resistant (PacR) MDA-MB 231 triple-negative breast cell line) required a lower concentration of TQ-PLGA-PF68 nanoparticles compared to their respective parental cell lines (p < 0.05). These findings suggest that TQ encapsulation with PLGA-PEG and Pluronics F68 is a promising anti-cancer agent in mitigating breast cancer resistance to chemotherapeutics. In future studies, the anti-cancer activity of TQ-PLGA-PF68 with the standard chemotherapeutic drugs used for breast cancer treatment is recommended.

Highlights

Nanotechnology has been gaining research interest in recent years and evolved alongside the growing technological demand to improve therapy [1,2]
TQ-PLGA-PF68 nanoparticles had slightly moved peaks either to a higher or lower wavelength corresponding to the native spectra of PLGA-poly(ethylene glycol) (PEG) or Pluronics F68
There were no TQ absorption bands detected. These results indicate that the TQ was successfully conjugated with the PLGA-PEG polymer and Pluronics F68 in forming TQ-PLGA-PF68 nanoparticles

Summary

Introduction

Nanotechnology has been gaining research interest in recent years and evolved alongside the growing technological demand to improve therapy [1,2]. Nanomedicines are less prone to drug degradation while being transported with improved biocompatibility and increased delivery of drugs to tissues. Nanomedicine exhibits great potential to effectively target and eliminate breast cancer stem cells involved in resistance. Polymer nanoparticles have been developed for an effective drug-delivery of hydrophobic drugs and hormone regulators (taxanes, camptothecin, cisplatin and tamoxifen) [4]. The US Food and Drug Administration (FDA) and European Medicines Agency (EMA) approved the use of biodegradable and biocompatible polymers. These polymers include poly(lactic acid) (PLA), poly(D,L-lactideco-glycolide) acid (PLGA) and poly(caprolactone) (PCL) [6]. The PLGA polymers exhibit physical stability and better biocompatibility for the delivery of drugs, proteins and macromolecules (DNA, RNA and peptides) [8]

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