Mesoporous silica nanoparticles (MSNs) exhibit the typical characteristics of inorganic materials that make them promising drug delivery carriers for cancer therapy. Their structural properties allow the targeted delivery of chemotherapeutic drugs to enhance drug efficacy and reduce adverse effects. The functionalization of MSNs with targeting ligands to a specific tissue/cell and stimuli‐responsive capping materials to seal drugs inside the MSNs pores are widely studied for biomedical and pharmaceutical applications. Furthermore, multiple stimuli‐responsive MSN‐based drug delivery systems are developed to enhance the delivery of anticancer drugs to their specific target and thereby improve the release of the drugs at the intended site. In addition, several toxicity studies are conducted to evaluate the biosafety and biocompatibility of MSNs. Although MSNs present reduced toxicity compared to colloidal silica, they can induce cytotoxicity associated with oxidative stress by increased reactive oxygen species production and decreased glutathione levels that can ultimately lead to cell death. However, different modifications to control morphology and surface composition can be applied to overcome the biocompatibility concerns. In this review, a comprehensive overview of the controlled synthesis, functionalization, targeting and biocompatibility of MSNs, as well as their biomedical application as a chemotherapeutic delivery system is provided.
Af acile route to Pt II complexes doubly functionalized with bioactive molecules through ab ipyridine-type ligand is described. Initially, ligands L EE (containing two ethacrynic acid units), L EF (ethacrynic acid + flurbiprofen) and L EB (ethacrynic acid + biotin) were obtained in moderate to good yields from 2,2'-bipyridine-4,4'-dicarboxylicacid. Subsequent reaction of the ligands with [PtCl 2 (DMSO) 2 ]a fforded complexes [PtCl 2 (L EE)] (2), [PtCl 2 (L EF)] (3)a nd [PtCl 2 (L EB)] (4)i n high yields. All compounds were fully characterizedb ya nalytical and spectroscopic methods. Complexes 2-4 are highly stable in water/DMSOs olutiona t3 7 8Ca fter 72 h, whereas progressive release of the bioactive fragments was detected in ac ell culture medium. The compounds were assessed for their in vitro antiproliferativea ctivity towards tumorigenic A2780, A2780cisR and Y79 cells and non-tumourigenic HEK293 cells. In particular,t he combinationo fe thacrynic acid and flurbiprofen in 3 overcomes cisplatin-based resistance andp rovides strongc ancerc ell selectivity.E nzyme inhibition assays on human GST P1 and human COX-2 and cross-experiments with complex 1,a nalogous to 2-4 but lackingb io-groups, revealed ac lear synergy between the Pt II frame andt he bioactive organic components.
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