Table 3.
Polymeric nanoparticles with salinomycin.
| Composition | Preparation Method | Size (nm) | PDI | Zeta Potential (mV) | EE (%) | Drug Loading (%) | In Vitro Release | Biological Effect | Ref. |
|---|---|---|---|---|---|---|---|---|---|
| PLGA | Emulsion diffusion evaporation method | 187.4 | 0.11 | +51.0 | 97.4 | n.r. | 43% in PBS pH 7.4 + 0.3% sodium azide, at 24 h; 100% after 45 days | Decreased the proliferation and enhanced the apoptosis of MG-63 cells | [10] |
| PCL, modified with PEGylated gelatinase-responsive peptide (PVGLIG) | Single emulsion method | n.r. | n.r. | n.r. | 89.70 | n.r. | n.r. | Inhibitory effects against HeLa CSCs, in vivo; reduced toxicity compared to free Sali | [51] |
| PLGA, conjugated with EGFR and CD133 aptamers | Emulsion/solvent evaporation method | 118.3–152.8 1 | 0.13–0.18 1 | −23.3-(−34.7) 1 | 51.5–58.1 1 | 7.0–9.3 1 | 80% in PBS pH 7.4 and 90% in rat plasma, after 500 h | Greater antitumor effect against HCC of dual conjugated NPs in vitro and in vivo, compared to single-conjugated or unconjugated NPs | [53] |
| PLGA, conjugated with CD133 aptamers | Emulsion/solvent evaporation method | 133.4/159.8 2 | 0.13/0.15 2 | −23.6/−30.1 2 | 55.9/53.1 2 | 7.2/6.8 2 | 50% in PBS pH 7.4 and human plasma, at 24 h; 85% after 12 days | Aptamer-conjugated Sali-NPs were 5 and 2-fold more effective against Saos-2 CD133+ cells than Sali-NPs and Sali; selective cytotoxicity against CD133+ CSCs in vitro and in vivo | [54] |
| PCL, modified with PEGylated gelatinase-cleavable peptide (PVGLIG) | Nanoprecipitation and single emulsion methods | 151.1/235.8 3 | 0.099/0.160 3 | n.r. | 81.51/89.70 3 | 7.40/8.12 3 | 79%/70% in PBS pH 7.4, at 24 h 3 | Higher survival rate of mice compared to free Sali | [70] |
| PLA, functionalized with folate | Nanoprecipitation method | 110/875.0 4 | n.r. | n.r. | 98/99 4,5 | 8.8/8.9 4,5 | n.r. | No difference in cytotoxicity against MG-63 cell compared to free Sali; superior anti-CSC effect for folate-decorated NPs in CSC-enriched culture | [71] |
| PLGA, coated with Polysorbate 80 | Solvent emulsion-evaporation method | 195.3–293.6 6 | 0.259–0.423 6 | n.r. | 57.2–62.9 6 | n.r. | 63.5–95.4% in PBS pH 7.4 + 0.1% sodium azide, after 480 h 6 | Greater targeting ability and decrease in cell viability of T98G cells for Polysorbate 80-coated NPs compared to naked NPs | [72] |
| PLGA, decorated with Herceptin | Solvent emulsion-evaporation method | 194.9–257.5 7 | 0.024–0.297 7 | n.r. | 61.3–91.7 7 | 1.62–19.0 7 | 32.9–79.6% in PBS pH 7.4 + 0.1% sodium azide, after 360 h 7 | Herceptin immobilization favored cellular uptake of Sali-NPs in MCF7 cells | [73] |
| PLGA-PEG, conjugated with CD133 antibody | Emulsion/solvent evaporation method | 139.9/149.2 8 | 0.16/0.18 8 | −19.6/−22.8 8 | 68.3/63.2 8 | 9.9/8.5 8 | 45% in PBS pH 7.4 and PBS + 10% FBS, at 24 h; 80% after 12 days | Enhanced cytotoxicity and anti-CSC effect against OVCAR-3 and PA-1 cells and in vivo antitumor efficacy of antibody-conjugated Sali-NPs, compared to naked Sali-NPs and free Sali | [74] |
| PLGA-TPGS | Nanoprecipitation method | 62.86 | 0.21 | −28.7 | 56.35 | 4.79 | n.r. | Higher Sali solubility and oral bioavailability by incorporation into NPs; superior efficacy against NC stem cells in tumor-bearing mice, compared to free Sali | [77] |
PDI, polydispersity index; EE, entrapment efficiency; PLGA, poly(lactic-co-glycolic acid); n.r., not reported; PCL, polycaprolactone; PEG, polyethylene glycol; CSC, cancer stem cell; Sali, salinomycin; EGFR, epidermal growth factor receptor; HCC, hepatocellular carcinoma; NP, nanoparticle; PLA, poly(lactic acid); FBS, fetal bovine serum; TPGS, d-α-tocopherol polyethylene glycol succinate; NC, nasopharyngeal carcinoma. 1 Data reported for unconjugated, single aptamer-conjugated and dual aptamer-conjugated salinomycin-loaded nanoparticles, respectively. 2 Data reported for native and CD133 aptamers-functionalized salinomycin-loaded nanoparticles, respectively. 3 Data reported for the nanoprecipitation method and single emulsion method, respectively. 4 Data reported for native and folate-functionalized salinomycin-loaded nanoparticles, respectively. 5 Data measured by gel permeation chromatography. 6 Data reported for different nanoparticle formulations, naked or coated with Polysorbate 80, and prepared with different salinomycin concentrations (5 µM and 10 µM). 7 Data reported for different nanoparticle formulations, naked or decorated with Herceptin, and prepared with different salinomycin concentrations (1 µM and 15 µM). 8 Data reported for naked and CD133 antibody-conjugated salinomycin-loaded nanoparticles, respectively.