Table 5.
Polymer–lipid hybrid nanoparticle formulations with salinomycin.
| Composition | Preparation Method | Size (nm) | PDI | Zeta Potential (mV) | EE (%) | Drug Loading (%) | In Vitro Release | Biological Effect | Ref. |
|---|---|---|---|---|---|---|---|---|---|
| PLGA, soybean lecithin, DSPE-PEG2000, conjugated with anti-HER2 Fab’ | Nanoprecipitation method | 123.2/135.6 1 | 0.12/0.15 1 | −25.6/−28.3 1 | 59.2/55.4 1 | 8.8/8.0 1 | 50% in PBS and PBS + 10% FBS, at 24 h; 80% in PBS and 90% in PBS + 10% FBS, after 96 h | Encapsulation in NPs promoted cellular delivery of Sali; greater cytotoxicity against HER2-positive breast CSCs and cancer cells, in vitro and in vivo, compared to unconjugated NPs and free Sali | [81] |
| PLGA, phosphatidylcholine, DSPE-PEG, CHOL (57:3:40), conjugated with EGFR and CD133 Fab’ | Emulsion-solvent evaporation method | 107.8 | 0.18 | −14.4 | 78.1 | 9.3 | 60% in PBS and PBS + 10% FBS, at 24 h; 80% after 96 h | Encapsulation in NPs facilitated the cellular delivery of Sali; dual-targeted NPs were more effective against lung cancer than untargeted NPs, single-targeted NPs and free Sali | [82] |
| PLGA, soybean lecithin, DSPE-PEG, conjugated with CD20 aptamers | Nanoprecipitation method | 92.1/96.3 2 | 0.12/0.11 2 | -20.3/-20.9 2 | 69.4/61.8 2 | 7.9/7.8 2 | 60% in PBS and 70% in PBS + 10% FBS, at 24 h; 80% after 96 h | Lower IC50 and increased tumor growth inhibition of melanoma CSCs compared to unconjugated NPs and free Sali | [83] |
| PLGA, phosphatidylcholine, DSPE-PEG, CHOL (57:3:40), conjugated with CD44 Fab’ | Emulsion-solvent evaporation method | 125.6/139.9 3 | 0.13/0.17 3 | −13.4/−17.3 3 | 76.3/74.2 3 | 8.1/8.9 3 | 45% in PBS and PBS + 10% FBS, at 24 h; 80% after 120 h | Specific delivery of Sali to prostate CSCs and greater inhibition of CSCs than unconjugated NPs and free Sali | [84] |
| PLGA, soybean lecithin, DSPE-PEG, conjugated with EGFR aptamer | Nanoprecipitation method | 89.6/95.6 4 | 0.12/0.11 4 | -21.6/-26.4 4 | 66.7/63.1 4 | 7.8/8.9 4 | 50% in PBS pH 7.4 and PBS + 10% FBS, at 24 h; 80% after 120 h | Significantly more effective towards osteosarcoma CSCs than unconjugated NPs and free Sali | [85] |
| PLGA, soybean lecithin, DSPE-PEG, conjugated with CD133 and EGFR aptamers | Solvent emulsion diffusion method | 110.2 | 0.15 | −17.7 | 66.5 | 9.4 | 60% in PBS and PBS + 10% FBS, at 24 h; 80% after 72 h | 3- to 7-fold higher cytotoxicity in osteosarcoma cells and CSCs and significant decrease in tumor growth in osteosarcoma-bearing mice, compared to untargeted NPs, Sali-NPs and free Sali | [86] |
| PLGA, soybean lecithin, DSPE-PEG2000, conjugated with GE11 peptide | Nanoprecipitation method | 132.6 5 | n.r. | -51.2 5 | n.r. | n.r. | n.r. | 3-fold greater cellular uptake and suppression of cell migration for targeted NPs compared to nontargeted NPs in MCF-7 cells; GE11-conjugated Sali-NPs had higher cytotoxic effect against MCF-7 cells in vitro than nontargeted NPs, but similar to free Sali; strongest tumor inhibitory effect in vivo for GE11- conjugated Sali-loaded NPs, compared to controls | [88] |
PDI, polydispersity index; EE, entrapment efficiency; PLGA, poly(lactic-co-glycolic acid); DSPE-PEG2000, 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N- (methoxy(polyethylene glycol)-2000); FBS, fetal bovine serum; NP, nanoparticle; Sali, salinomycin; CSC, cancer stem cell; CHOL, cholesterol; EGFR, epidermal growth factor receptor; n.r., not reported. 1 Data reported for unconjugated and anti-HER2 antibody-conjugated salinomycin-loaded nanoparticles, respectively. 2 Data reported for unconjugated and CD20 aptamers-conjugated salinomycin-loaded nanoparticles, respectively. 3 Data reported for unconjugated and CD44 antibody-conjugated salinomycin-loaded nanoparticles, respectively. 4 Data reported for unconjugated and EGFR aptamer-conjugated salinomycin-loaded nanoparticles, respectively. 5 Data reported for GE11-conjugated salinomycin-loaded nanoparticles.