Table 3.
In Vitro and In Vivo Anticancer Potential and Mechanism of Action of Various Curcumin Nanoformulations
| Curcumin Nanoformulations | In Vitro Cytotoxicity Profile | Molecular Mechanism | In Vivo Results | Reference |
|---|---|---|---|---|
| PLGA | IC50 (50% cell growth inhibitory concentration) of curcumin-loaded PLGA nanoparticles was between 20 μM and 22.5 μM while free curcumin ranged from 32 μM to 34 μM, in LNCaP, PC-3, and DU145 cancer cell lines | Inhibition of NF-κB function | Not available | [42] |
| PLGA | IC50 of curcumin nanoparticles was less than 5 μM in human leukemia (KBM-5 and Jurkat), prostate (DU145), breast (MDA-MB-231), colon (HCT116) and esophageal (SEG-1) cancer cells | Do not induce NF-κB activation expression of cyclin D1, MMP-9, and VEGF | Half-life of curcumin NPs (2.5 mg/Kg mice) was 1.75 longer than that of curcumin | [44] |
| PLGA | Nanocurcumin is as effective as curcumin in HeLa cells, SKBr3, and A549 cells | Increased Annexin V staining Cleaved PARP expression Down regulation of the activation of NF-κB |
Not available | [81] |
| MPEG-PCL micelle | IC50 of free curcumin and Cur-MPEG-PCL micelles was 3.95 mg mL−1 and 5.78 mg mg mL−1, respectively | Not available | Up to 2-fold increase in CUR concentration was observed in plasma of rats Inhibited the growth of subcutaneous C-26 colon carcinoma in xenograft mouse model |
[61] |
| β-cyclodextrin self-assembly | IC50 of self-assemblies of curcumin was 16.8 μM and 17.6 μM(C4-2 cells and DU145 cells, respectively) which is slightly lower than free curcumin | Increased cleaved PARP expression | Improved CUR levels serum concentrations up to 2-fold (Unpublished data with Subhash Chauhan Lab) | [87] |
| Poly(β-cyclodextrin) self-assembly | Very close IC50 values for both self-assembly and free curcumin in C4-2, DU145 and PC3 cancer cells | The PARP cleavage caused by PCD30 is much greater than free curcumin | Not available | [88] |
| poly(butyl cyanoacrylate) nano-particles | IC50 was observed approximately 15_μg/mL for HepG2, Bel7402 and Huh7 cells | Down regulation of COX-2 and VEGF expression | 2.2 fold decrease in tumor volume in HepG2 xenograft-bearing mice | [127] |
| Dendrosome | 2-fold reduction in IC50 with dendrosome curcumin in WEHI-164 (16.8 μM and 7.5 μM) and A431 cells (19.2 and 14.3 μM) in 24 and 48 h time | Increased Annexin V stain Cleaved PARP (apoptosis) | Tumor growth was significantly suppressed in mice treated with dendrosomal curcumin | [47] |
| Thermo-sensitive nanocarrier | Formulation showed a specific toxicity cancer cell lines (MCF-7, KB, and PC-3) and non toxic to L929. | Increase apoptosis (PI and Annexin-A binding) Loss of mitochondrial membrane potential |
Not available | [51] |
| Folate-modified self-microemulsifying drug delivery system | 18.27, 36.69, 30.4 μM and 20.57, 38.59, 25.62 μM in Hela and HT-29 cancer cells for folate CUR-nanoemulsion, CUR-emulsion and free curcumin, respectively | Not available | In situ colon perfused rats showed absorption of curcumin increased from 58.41% to 73.38% in 6 h with folate conjugated formulation. | [131] |
| NanoCurc™ | IC50 ranged between 10–15 μM for BxPC3, ASPC-1, PL-11 and XPA-1 | Blocks the activation of NF-κB Downregulation of steady state transcripts of multiple pro-inflammatory cytokines |
5 fold increased concentration was observed in pancreas. 3-fold or no growth in tumor was observed in mice with NanoCurc™ in combination with gemcitabine |
[52, 117] |
| PEG-chlorestrol | Cm/PEG-cholesterol based curcumin system showed IC50 1 μM more than free curcumin | Not available | Not available | [62] |
| NanoCurc™ | Almost no growth was observed in DAOY and D283Med, and the glioblastoma neurosphere lines HSR-GBM1 andJHH-GBM14 | Blocked the STAT3 and Hedgehog signaling G(2)/M arrest and apoptotic induction |
0.5% of the injected material was localized in the brain | [115, 116] |
| Amphiphilic mPEG-palmitic acid polymer | IC50 of curcumin, 14.32 μM, and nanocurcumin, 15.58 μM, were observed in HeLa cells | In vitro enzyme-catalyzed drug release enhances the anticancer activity | Not available | [132] |