Table 2.
Strategies to enhance bioavailability and/or antitumoral effects of curcumin.
| Composition | Outcomes | References |
|---|---|---|
| Polymeric Nanoparticles (NPs) | ||
| PLGA + CUR | Superior anticancer effects respect to free curcumin in cervical cancer cells | [160] |
| PLGA + CUR | Superior cellular uptake and anticancer effects respect to free curcumin in ovarian and breast cancer cells | [161] |
| PLGA + CUR | Superior cellular uptake and anticancer effects respect to free curcumin in prostate cancer cells | [162] |
| NIPAAM+ VP + PEG-A + CUR | Superior cellular absorbition and anticancer effects respect to free curcumin in pancreatic cancer cells | [163] |
| mPEG-PCL + CUR | Superior anticancer effects respect to free curcumin in human lung adenocarcinoma cancer cells | [164] |
| silk fibroin + CUR | Superior cellular uptake and anticancer effects respect to free curcumin in colon cancer cells | [165] |
| zein-chitosan +CUR | High encapsulation efficiencies for curcumin. Superior anticancer effects respect to free curcumin in neuroblastoma cell line |
[166] |
| chitosan +CUR | Enhanced curcumin solubility and bioavailability. Sustained drug release from NPs and anticancer effects with respect to free curcumin in cervical cancer cells |
[167] |
| Solid Lipid Nanoparticles (SLNs) | ||
| SLNs + N-carboxymethyl chitosan+ CUR | Prolonged release in simulated intestinal fluid, greater absorption and oral bioavailability compared to free curcumin. Superior anticancer effects respect to free curcumin in breast cancer cells |
[171] |
| SLNs + CUR, d-α-Tocopheryl polyethylene glycol 1000 succinate-stabilized curcumin (TPGS) + CUR | Superior curcumin plasma levels in mice. Superior anticancer effects respect to free curcumin in Hodgkin lymphoma cells and in Hodgkin’s lymphoma xenograft models |
[172] |
| SLNs + tristearin + PEGylated + CUR | Superior bioavailability, absorption and long-term stability after oral administration in the rats | [174] |
| SLNs + NaCas + NaCas-Lac + CUR | Superior stability at pH acid and antioxidant activity with respect to free curcumin | [175] |
| SLNs + glyceryl monostearate + poloxamer 188 + CUR | Superior stability, solubility, cellular uptake, release and anticancer effects respect to free curcumin in breast cancer cells | [176] |
| Inorganic Nanoparticles | ||
| MNPs + CUR | Superior cellular uptake in vitro. Superior bioavailability in vivo. Superior in vitro and in vivo therapeutic efficacy respect to free curcumin in pancreatic cancer cells and in pancreatic cancer xenografts model |
[180] |
| Folic-acid-tagged aminated-starch-/ZnO-coated iron oxide nanoparticles + CUR | Significant controlled release of curcumin and reduced hepatic and breast cancer cells viability in vitro. Cellular uptake increase in vitro |
[181] |
| PSMNPs + CUR | Aqueous colloidal stability, biocompatibility, high loading affinity for curcumin and better curcumin release in acidic conditions. Superior cellular uptake and anticancer effects respect to free curcumin in breast cancer cells |
[182] |
| MNP@PEG + CUR | Higher drug release in acidic conditions, biocompatibility and low cytotoxicity at physiological pH | [183] |
| Silica + CUR | Good stability in aqueous medium, sustained drug release and greater anticancer properties in cervical cancer cells compared to normal fibroblasts | [184] |
| HA-CUR@AuNPs | Good aqueous solubility, superior cellular uptake and anticancer effects respect to free curcumin in cervical, glioma and colon cancer cells | [185] |
| Liposomes | ||
| Liposome + CUR | Improved curcumin aqueous solubility and bioavailability in tumor-bearing mice | [192] |
| DMPC + CUR | Superior anticancer effects respect to free curcumin in prostate cancer cells | [193] |
| 2-hydroxypropyl-γ-cyclodextrin/ liposome + CUR | Superior in vitro and in vivo anticancer effects respect to free curcumin in osteosarcoma cancer cells | [194] |
| Liposome + doxorubicin + CUR | Superior anticancer effects respect to those loaded with doxorubicin alone in colon cancer cells | [195] |
| Liposome + CUR | Superior anticancer effects respect to free curcumin in endometrial cancer cells | [196] |
| Liposome + CUR + BLED-PDT therapy | Enhancement of BLED-PDT therapy effect by curcumin liposome in lung cancer cells | [197] |
| Phytosomes | ||
| Curcuminoids + lecithin (Meriva ®) | Improved absorption and clinical efficacy respect to unformulated curcuminoid mixtures | [198] |
| Soluplus® [polyvinyl caprolactam-polyvinyl acetate polyethylene glycol graft copolymer] + CPC | Improved flowability, dissolution rate and oral bioavailability in rats | [203] |
| Micelles | ||
| MePEG-b-PCL + CUR | Improved water solubility | [206] |
| MePEG-b-PCL + CUR | Improved biological half-life with respect to the free curcumin in rat models | [207] |
| Tween-80 micelles + CUR | Improved drug plasma concentration with respect to free curcumin in volunteers | [208] |
| Micellar formulation + CUR (Sol-CUR) | Superior uptake, transepithelial transport, distribution and bioavailability in colon cancer cell model | [209] |
| Micelles + CUR | Enhancement of aqueous solubility, stability, dissolution and permeability of curcumin formulated in micelles compared to free drug | [210] |
| PSBMA + CUR | Greater stability, cellular uptake and tumor cytotoxicity compared to free curcumin | [211] |
| MPEG-P [CL-co-PDO] + CUR | Superior encapsulation efficiency, prolonged drug release profile and antitumor effects respect to free curcumin in prostate cancer cells | [212] |
| Pluronic F-127 + Gelucire® 44/14 micelles + CUR | Controlled curcumin release, superior oral bioavailability in vivo and in vitro antitumor effects in lung cancer cells respect to free curcumin | [213] |
| CUR-MPP-TPGS-MMs | Small size, high drug-loading and sustained release. Improved intestinal absorption and oral bioavailabil-ity in rats |
[214] |
| Curcumin/β-Cyclodextrin (β-CD) and Solid Dispersions (SDs) | ||
| β-CD + CUR | Superior sunlight stability and solubility respect to pure colourant | [218] |
| Liquid-type β-CD + CUR | Improved solubility in water and bioavailability | [220,221] |
| Solid type β-CD + CUR | Improved storage stability and biovailability | [222] |
| CUR-CD-CS | Superior solubility, cellular absorption and antitumor effects compared to free curcumin in skin cancer cells | [223] |
| β-CD + CUR | Improved uptake and therapeutic efficacy in prostate cancer cells | [154] |
| β-CD + CUR | Improved delivery and therapeutic efficacy compared to free curcumin in both in vitro lung carcinoma cell lines and in vivo mouse hepatoma xenograft models | [224] |
| β-CD + CUR | Superior anticancer effects respect to free curcumin in cervical cancer cells | [225] |
| FA-CUR-NPs | Improved drug release rate, cellular uptake efficiency and in vitro and in vivo antitumor activity respect to free curcumin in cervical cancer cells | [226] |
| Hydroxypropyl-β-CD+ CUR+piperine | Improved solubility of the curcumin–piperine system, its permeability through biological membranes, antioxidant and antimicrobial activities and enzymatic inhibition | [227] |
| SDs (with Gelucire®50/13-Aerosil) + CUR | Improved stability, water solubility, dissolution rate, bioavailability and anti-inflammatory activity in rats | [229] |
| Solutol® HS15 SDs + CUR | Improved solubility and bioavailability compared to free curcumin | [231] |
| SDs (with cellulose acetate and mannitol) + CUR | Improved water solubility and oral bioavailability compared to free curcumin | [232] |
| SDs + CUR | Superior water solubility and gastrointestinal absorption in rats | [233] |
| SDs (with Poloxamer 407) + CUR | Improved water dispersibility and cytotoxic effects against breast, lung, cervical and hepatocellular cancer cells | [234] |
| Curcumin Conjugates Formulations | ||
| Piperine + CUR | Curcumin enhanced serum levels, reduced elimination half-life and clearance, increased bioavailability in rats and humans | [236] |
| Piperine + CUR | Curcumin increased bioavailability in epileptic rats | [237] |
| Piperine + CUR | Curcumin enhanced intestinal absorption and bioavailability in rats | [238] |
| BCM-95CG (Biocurcumax®): piperine + lecithin + CUR | Curcumin improved bioavailability and pharmacokinetic profile respect to free drug in healthy subjects | [239] |