02832nas a2200205 4500008004100000245015600041210006900197260001800266300001000284490000600294520210500300653001702405653002002422653001702442653003002459100002002489700002602509700002702535856006402562 2017 eng d00aThe Influence of Pluronic F68 and F127 Nanocarrier on Physicochemical Properties, In vitro Release, and Antiproliferative Activity of Thymoquinone Drug0 aInfluence of Pluronic F68 and F127 Nanocarrier on Physicochemica cFebruary 2017 a12-200 v93 a

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.

10acytotoxicity10aMCF-7 cell line10aPluronic F6810aThymoquinone-nanoparticle1 aShaarani, Salwa1 aHamid, Shahrul, Sahul1 aKaus, Noor, Haida Mohd uhttps://phcogres.com/article/2017/9/1/1041030974-8490199774