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

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.

Nanoformulation of Paclitaxel: Exploring the Cyclodextrin / PLGA Nano Delivery Carrier to Slow Down Paclitaxel Release, Enhance Accumulation in Vivo

“…FTIR spectral analysis of PTX PLGA NPs, and PTX PLGA/CD NPs vibrational modes in their native form and nanoparticle formulations provides insight into the structural integrity and retention of functional groups in the nanoparticles formed 31 . Figure 2 B shows the physical mixture of paclitaxel, paclitaxel and carrier material (physical mixture, PM.…”

“…In contrast, in PLGA nanoparticles and CD/PLGA nanoparticles, the characteristic diffraction of paclitaxel disappeared, and the crystallinity of paclitaxel was reduced in the nanoparticles, and paclitaxel might be completely dissolved or existed in the nanoparticles in an amorphous state, and this state was favorable to improve the stability of the drug. FTIR spectral analysis of PTX PLGA NPs, and PTX PLGA/CD NPs vibrational modes in their native form and nanoparticle formulations provides insight into the structural integrity and retention of functional groups in the nanoparticles formed [31]. Figure 2B shows the physical mixture of paclitaxel, paclitaxel and carrier material (physical mixture, PM.…”

Dual-Targeting Polymer Nanoparticles Efficiently Deliver DNA Vaccine and Induce Robust Prophylactic Immunity against Spring Viremia of Carp Virus Infection

“…Polymers, especially PLGA and chitosan, have been widely used as DNA vaccine carriers. PLGA is a kind of polymeric organic compound with excellent biocompatibility and degradability ( 27 , 28 ). As a DNA vaccine vector, PLGA has the advantages including slow release, targeting, protection of DNA plasmid from destruction, high encapsulation carrying capacity, and easy escape from lysosomes ( 29 ).…”

Self-Micellizing Solid Dispersion of Thymoquinone with Enhanced Biopharmaceutical and Nephroprotective Effects

“…By dissolving 10 mg of TQM with 10 mL methanol in a volumetric flask to achieve a final concentration of 1 mg/mL, a 10 mL stock solution of TQM was created. The Beer-Lambert equation is followed by TQM in the concentration range of 8 to 30 µg/mL, and TQM provides a suitable absorbance value at 257 nm [22]. Therefore, the stock solutions were then diluted sequentially at various concentrations prior to use and the corresponding absorbance was determined at 257 nm using a UV-vis spectrophotometer (UV-1800, Shimadzu Corporation, Japan).…”