Abstract
Abstract Cisplatin (Cis) is an effective cytotoxic agent, but its administration has been challenged by kidney problems, reduced immunity system, chronic neurotoxicity, and hemorrhage. To address these issues, pH-responsive non-ionic surfactant vesicles (niosomes) by Span 60 and Tween 60 derivatized by cholesteryl hemisuccinate (CHEMS), a pH-responsive agent, and Ergosterol (helper lipid), were developed for the first time to deliver Cis. The drug was encapsulated in the niosomes with a high encapsulation efficiency of 89%. This system provided a responsive release of Cis in pH 5.4 and 7.4, thereby improving its targeted anticancer drug delivery. The noisome bilayer model was studied by molecular dynamic simulation containing Tween 60, Span 60, Ergosterol, and Cis molecules to understand the interactions between the loaded drug and noisome constituents. We found that the platinum and chlorine atoms in Cis are critical factors in distributing the drug between water and bilayer surface. Finally, the lethal effect of niosomal Cis was investigated on the MCF7 breast cancer cell line using 3-(4, 5-Dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide (MTT) assay. Results from morphology monitoring and cytotoxic assessments suggested a better cell-killing effect for niosomal Cis than standard Cis. Together, the synthesis of stimuli-responsive niosomes could represent a promising delivery strategy for anticancer drugs.
Highlights
Cisplatin (Cis) is an effective cytotoxic agent, but its administration has been challenged by kidney problems, reduced immunity system, chronic neurotoxicity, and hemorrhage
Another study evaluated two novel liposomal formulations of Cis as potential therapeutic agents for treating glioma in the F98 rat glioma model. a variety of dose-dependent neuropathologic changes from none to severe were seen at 10 or 14 d following their administration. These findings suggest that further refinements in the design and formulation of Cis-containing liposomes will be required before they can be administered i.c. by convection-enhanced delivery (CED) for the treatment of brain tumors and that a formulation that may be safe when given systemically may be highly neurotoxic when administered directly into the brain [60]
Free Cis and niosomal Cis were applied into the culture medium at increasing concentrations
Summary
Abstract: Cisplatin (Cis) is an effective cytotoxic agent, but its administration has been challenged by kidney problems, reduced immunity system, chronic neurotoxicity, and hemorrhage. To address these issues, pH-responsive non-ionic surfactant vesicles (niosomes) by Span 60 and Tween 60 derivatized by cholesteryl hemisuccinate (CHEMS), a pHresponsive agent, and Ergosterol (helper lipid), were developed for the first time to deliver Cis. The drug was encapsulated in the niosomes with a high encapsulation efficiency of 89%. Results from morphology monitoring and cytotoxic assessments suggested a better cell-killing effect for niosomal Cis than standard Cis. Together, the synthesis of stimuli-responsive niosomes could represent a promising delivery strategy for anticancer drugs
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