Treatment of breast cancer with engineered novel pH-sensitive triaryl-(Z)-olefin niosomes containing hydrogel: an in vitro and in vivo study.

Abstract

Triaryl-(Z)-olefin (TZO) was synthesized as a Tamoxifen (TMX) analogue for breast cancer treatment to avoid developing the resistance and toxicity of TMX. TZO was synthesized using McMurry olefination reaction and has anti-cancer activity better than TMX by two folds. In this paper, in situ pH-sensitive TZO-loaded noisome hydrogel was prepared for delivering and targeting TZO to its site of activity. Equi-molar of cholesterol and span 60 was used to prepare TZO-loaded niosomes using the Hand Shaking Method. The central composite experimental design was used to prepare differently in situ pH-sensitive TZO-loaded niosomes formulae. The formulae were done by incorporated TZO-loaded niosomes into different concentrations of chitosan and Glyceryl monooleate (GCM). Increasing the chitosan and GCM concentrations resulted in significantly increasing the viscosity and significantly decreasing the release of TZO from different formulae. The formula composed of (0.61% w/v) of chitosan and (0.23% w/v) of GCM was chosen as an optimum formula to evaluate the efficacy of TZO using Ehrlich carcinoma mice model. A significant anti-tumour effect was shown in comparison with TMX. Briefly, in situ pH-sensitive TZO-loaded niosomes could be an effective treatment for breast cancer.

• Authors: Heba F Salem, Rasha M Kharshoum, Amr Gamal F, Fatma I Abo El-Ela, Khaled R A Abdellatif
• Journal: Journal of liposome research (J Liposome Res) Vol. 30 Issue 2 Pg. 126-135 (Jun 2020) ISSN: 1532-2394 [Electronic] England
• PMID: 30935273 (Publication Type: Journal Article)

Chemical References

• Alkenes
• Antineoplastic Agents
• Hydrogels
• Liposomes

Topics

• Alkenes (chemical synthesis, chemistry, pharmacology)
• Animals
• Antineoplastic Agents (chemical synthesis, chemistry, pharmacology)
• Breast Neoplasms (diagnostic imaging, drug therapy, pathology)
• Carcinoma, Ehrlich Tumor (diagnostic imaging, drug therapy, pathology)
• Cell Proliferation (drug effects)
• Cell Survival (drug effects)
• Dose-Response Relationship, Drug
• Drug Screening Assays, Antitumor
• Female
• Hydrogels (chemical synthesis, chemistry, pharmacology)
• Hydrogen-Ion Concentration
• Liposomes (chemistry)
• Mice
• Molecular Structure
• Particle Size
• Structure-Activity Relationship
• Surface Properties
• Tomography, X-Ray Computed
• Viscosity