@article {256, title = {The Influence of Pluronic F68 and F127 Nanocarrier on Physicochemical Properties, In vitro Release, and Antiproliferative Activity of Thymoquinone Drug}, journal = {Pharmacognosy Research}, volume = {9}, year = {2017}, month = {February 2017}, pages = {12-20}, type = {Original Article}, chapter = {12}, abstract = {

Background: This study reports on hydrophobic drug thymoquinone (TQ), an active compound found in the volatile oil of Nigella sativa that exhibits anticancer activities. Nanoformulation of this drug could potentially increase its bioavailability to specific target cells. Objective: The aim of this study was to formulate TQ into polymer micelle, Pluronic F127 (5.0 wt \%) and Pluronic F68 (0.1 wt \%), as a drug carrier to enhance its solubility and instability in aqueous media. Materials and Methods: Polymeric micelles encapsulated TQ were prepared by the microwave-assisted solvent evaporation technique. Fourier transform infrared spectroscopy and ultraviolet-visible spectrophotometer were utilized for qualitative confirmation of micelles encapsulation. The surface morphology and mean particle size of the prepared micelles were determined by using transmission electron microscopy (TEM). Cytotoxicity effect was studied using 3-(4,5-dimethylthiazol-2-yl)-5-(3- carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (MTS) assay. Results: Dynamic laser light scattering (DLS) technique showed hydrodynamic size distribution of optimized micelles of 50 nm, which was in close agreement with the mean particle size obtained from TEM of about 51 nm. Drug release study showed the maximum percentage of TQ release at 61\% after 72 h, while the entrapment efficiency of TQ obtained was 46\% using PF127. The cytotoxic effect of PF127-encapsulated TQ was considerably higher compared to PF68-encapsulated TQ against MCF7 cells, as they exhibited IC50 value of 8 μM and 18 μM, respectively. Conclusion: This study suggests higher molecular weight Pluronic polymer micelles (F127) with hydrophilic-hydrophobic segments which could be used as a suitable candidate for sustainable delivery of TQ. However, comprehensive studies should be carried out to establish the suitability of Pluronic F127 as a carrier for other drugs with similar challenges as TQ.

}, keywords = {cytotoxicity, MCF-7 cell line, Pluronic F68, Thymoquinone-nanoparticle}, doi = {10.4103/0974-8490.199774}, author = {Salwa Shaarani and Shahrul Sahul Hamid and Noor Haida Mohd Kaus} } @article {665, title = {Cellular Responses with Thymoquinone Treatment in Human Breast Cancer cell line MCF-7}, journal = {Pharmacognosy Research}, volume = {5}, year = {2013}, month = {May 2013}, pages = {200-206}, type = {Original Article }, chapter = {200}, abstract = {

Background:Nigella sativa\ or black seed extract has been reported to show various medicinal benefits. Thymoquinone which is an active compound of its seed has been reported to contain anti-cancer properties.\ Objective:\ The study addressed the anti-cancer efficiency of long-term\ in vitro\ treatment with thymoquinone towards human breast cancer cell lines MCF-7.\ Materials and Methods:\ Cell proliferation was determined with CellTiter 96 Aqueous. Non-Radioactive Cell Proliferation Assay Kit. It was followed with trypan blue exclusion test to determine the percentage of viable cells. The study incorporated cell cycle assay to distinguish cell distribution at various cell cycle phases using Cycletest Plus DNA Reagent Kit. The apoptosis detection kit was used to determine the percentage of apoptotic and necrotic cells using flow cytometry.\ Results:\ The 50\% inhibitory concentration (IC\ 50\ ) value determined using the proliferation assay was 25 μM thymoquinone. Late apoptotic cell percentage increased rapidly when treatment duration was increased to 24 h with 25 and 100 μM thymoquinone. Further analysis using cell cycle assay showed thymoquinone inhibition of breast cancer cell proliferation at minimal dose 25 μM and led to S phase arrest significantly at 72 h treatment (P\ = 0.009). It was also noted elevation sub-G\ 1\ peak following treatment with 25 μM thymoquinone for 12 h. Increase in thymoquinone to 50 μM caused G\ 2\ phase arrest at each time-point studied.\ Conclusion:\ In general thymoquinone showed sustained inhibition of breast cancer cell proliferation with long-term treatment. Specificity of phase arrest was determined by thymoquinone dose.

}, keywords = {Apoptosis, cytotoxicity, Long-term Exposure, MCF-7 cell line, Thymoquinone}, doi = {10.4103/0974-8490.112428}, author = {Marjaneh Motaghed and Faisal Muti Al-Hassan and Shahrul Sahul Hamid} }