<p>Formulation, Cellular Uptake and Cytotoxicity of Thymoquinone-Loaded PLGA Nanoparticles in Malignant Melanoma Cancer Cells</p>

Abstract

Introduction: Thymoquinone (TQ) is the main active compound extracted from Nigella sativa a traditional herb with wide therapeutic applications and recognizable anticancer properties. This study aimed to formulate and characterize TQ-nanoparticles using PLGA as a biocompatible coating material (TQ-PLGA NPs) with the evaluation of its therapeutic properties in human melanoma cancer cells. Methods: The TQ-PLGA NPs were prepared and characterized for size, zeta potential, encapsulation efficiency, and release profile. Results: The particle size was 147.2 nm, with 22.1 positive zeta potential and 96.8% encapsulation efficiency. The NPs released 45.6% of the encapsulated TQ within 3 h followed by characteristic sustained release over 7 days with a total of 69.7% cumulative release. TQ-PLGA NPs were taken up effectively by the cells in a time-dependent manner up to 24 h. Higher cell toxicity was determined within the first 24 h in melanoma cells due to the rapid release of TQ from the NPs and its low stability in the cell culture media. Conclusion: TQ-PLGA NPs is a potential anticancer agent taking advantage of the sustained release and tailored size that allows accumulation in the cancer tissue by the enhanced permeability and retention effect. However, stability problems of the active ingredient were address in this study and requires further investigation.

Recent Findings on Thymoquinone and Its Applications as a Nanocarrier for the Treatment of Cancer and Rheumatoid Arthritis

“…A cubosomal formulation of TQ improved cellular accumulation, which leads to increased apoptotic activity migration in mammary gland carcinoma cell lines (MDA-MB-231 and MCF-7) [ 187 ]. Chitosan-coated TQ-PLGA-NPs accumulated in melanoma cancer cells (A375) by taking advantage of the EPR effect and positive surface charge of chitosan, which facilitate binding with the negatively charged cell membrane and induce cellular retention as well as time-dependent cytotoxicity [ 188 ]. TQ loading into niosomes improved cellular internalizations with controlled release of TQ, which markedly inhibits the migration of pro-inflammatory markers in mammary gland carcinoma with respect to pure TQ [ 10 ].…”

Phyto-Phospholipid Conjugated Scorpion Venom Nanovesicles as Promising Carrier That Improves Efficacy of Thymoquinone against Adenocarcinoma Human Alveolar Basal Epithelial Cells

“…These studies revealed that THQ has a variety of important mechanisms of action in cancer treatment, such as inducing apoptosis in cancer cells by generating reactive oxygen species (ROS), interfering with DNA structure and synthesis, acting as an immunomodulator, and targeting carcinogenic signaling pathways [9][10][11]. Nanotechnology-based delivery platforms have demonstrated promise in the treatment of cancer due to their enhanced permeability and retention (EPR) properties, which facilitate drug targeting to cancerous cells [12].…”

Therapeutic strategies and potential implications of silver nanoparticles in the management of skin cancer

“…Polystyrene-coated AgNP caused few genetic changes compared to uncoated NPs based on cell viability assay, micronucleus test, and DNA microarray analysis [ 187 ]. Thymoquinone PLGA (TQ-PLGA) NPs formulated and characterized using an active compound extracted from Nigella sativa – TQ is a biocompatible coating material (TQ-PLGA NPs) with the evaluation of its therapeutic properties in human melanoma cancer cells with 96.8% encapsulation efficiency [ 188 ]. Other evidence demonstrates that AgNP coatings interfere with normal healthy skin cells.…”