RETRACTED: Lipidic Nano-Sized Emulsomes Potentiates the Cytotoxic and Apoptotic Effects of Raloxifene Hydrochloride in MCF-7 Human Breast Cancer Cells: Factorial Analysis and In Vitro Anti-Tumor Activity Assessment

Abstract

Raloxifene hydrochloride (RLX), an antiosteoporotic agent, has been utilized for guarding against breast cancer and recently, for the disease management owing to its estrogen antagonist activity. Nevertheless, RLX exhibits poor bioavailability that could be attributed to reduced water solubility and first pass metabolism. To overcome these challenges, this study aimed at formulating and optimizing RLX emulsomes (RLX-EMLs) to enhance the drug antitumor activity. A 4131 factorial design was employed for assessing the effect of lipoid: solid lipid ratio and solid lipid type on the emulsomes characteristics. The anticancer potential of the optimized formulation and apoptotic parameters were assessed. Vesicle size, entrapment, and release efficiency were significantly influenced by both variables, while zeta potential was influenced by lipoid: solid lipid at p < 0.05. The optimal formulation exhibited vesicle size of 236 ± 8.6 nm, zeta potential of −18.6 ± 0.7 mV, drug entrapment of 98.9 ± 4.9%, and release efficiency of 42.7 ± 1.8%. MTT assay showed concentration-dependent inhibition of MCF-7 cells viability. In addition, cells treated with RLX-EMLs showed significant arrest at G2/M phase associated with significant increase in apoptotic and necrotic cells. The enhanced cytotoxic and anti-proliferative effect of RLX-EMLs relative to raw drug was authenticated through increased Bax/Bcl-2 ratio, caspase-9 activation and depletion of mitochondrial membrane potential.

Inclusion of a Phytomedicinal Flavonoid in Biocompatible Surface-Modified Chylomicron Mimic Nanovesicles with Improved Oral Bioavailability and Virucidal Activity: Molecular Modeling and Pharmacodynamic Studies

“…ANOVA statistical analyses were used to consider the main effects and the significance of each of the variables under examination. The optimal formulation with the superior desirability value was selected for further investigations [ 25 ].…”

Design, Green Synthesis and Tailoring of Vitamin E TPGS Augmented Niosomal Nano-Carrier of Pyrazolopyrimidines as Potential Anti-Liver and Breast Cancer Agents with Accentuated Oral Bioavailability

“…Statistical analysis of the data was conveyed utilizing Design Expert ® 7 software. In addition, the proceeded statistical analysis conducted via ANOVA was implemented to highlight the prime impacts of the variables under exploration; the significance of each variable was analyzed, and the best formula with the superior desirability value was picked for further assessments [ 55 ].…”

“…Statistical analysis of the data was conveyed utilizing Design Expert ® 7 software. In addition, the proceeded statistical analysis conducted via ANOVA was implemented to highlight the prime impacts of the variables under exploration; the significance of each variable was analyzed, and the best formula with the superior desirability value was picked for further assessments [55]. The solidification of the optimum TPGS-modified niosomal formula was obtained via the lyophilization technique (Alpha 2-4, CHRIST, Osterodeam Harz, Germany), where mannitol (5% w/v) was utilized as a cryoprotectant to prohibit the lysis of the vesicles.…”

Design and Synthesis of Newly Synthesized Acrylamide Derivatives as Potential Chemotherapeutic Agents against MCF-7 Breast Cancer Cell Line Lodged on PEGylated Bilosomal Nano-Vesicles for Improving Cytotoxic Activity

“…Drug stock solution of 1 mg/mL in methanol was prepared, and a calibration curve was constructed utilizing six dilutions that were prepared in concentrations of 100, 200, 400, 600, 800 and 1000 µg/mL. All solutions were filtered using 0.22 µm syringe filter and then 10 µL was subjected to HPLC analysis using Waters-2690 Alliance ® HPLC system (WatersTM, Milford, MA, USA), and HPLC conditions were in mobile phase: water (50:50); flow rate: 1 mL/min [46]. A distinct peak of the drug was observed at 254 nm.…”

“…Statistical analysis of the data was performed by utilizing Design Expert ® 7 software. In addition, the statistical analysis conducted via ANOVA was implemented to highlight the prime impacts of the variables under exploration; the significance of each variable was analyzed, and the best formula with the superior desirability value was picked for further assessments [46].…”