(EC) and methylcellulose (MC) were used for efficient curcumin nanoencapsulation
by the self-assembly of curcumin into monopolymeric carrier (EC) and dipolymeric
carrier (ECMC, a blend of EC and MC) with 50% loading. The nanospheres showed
a dose-dependent cytotoxicity and free radical scavenging activity towards human
breast adenocarcinoma (MCF-7) and HepG2 cells in vitro. The nanosystems were
evaluated in vivo for their adherence to stomach mucosa and their ability to release
curcumin into the circulation via oral administration into mice. The authors reported
that curcumin sustainability in blood was improved by the nanoencapsulation [117].
The aqueous solubility and stability over a wide pH range of curcumin was enhanced
by its nanoencapsulation in a biodegradable polymeric methoxyPEG-palmitate
amphiphilic conjugate. The study also reported that nanoencapsulated curcumin
inhibited human cervical cancer (Hela) cell proliferation (half-maximal inhibitory
concentration, IC 50 ¼ 15.58 mM) comparably to free curcumin (IC 50 ¼ 14.32 mM),
thereby showing its anticancer activity in Hela cells in vitro [118].
It was reported that curcumin has been encapsulated in nontoxic and nonimmunogenic human serum albumin (HSA) nanoparticles. Albumin-bound nanoparticle technology is an easy fabrication process that does not use any toxic
surfactants and is well tolerated in vivo [119, 120]. Curcumin-HSA NPs
(130–150 nm) improved the water solubility of curcumin by 300-fold and enhanced
its in vivo antitumor activity (50–66% tumor growth inhibition) in a tumor xenograft HCT-116 model. Kim et al. suggested that this potent antitumor activity of
curcumin-HSA NPs could be due to the enhanced water solubility, increased
accumulation in tumors, and an ability to traverse vascular endothelial cells
[121]. In another study, fibrinogen was used as a nanocarrier for curcumin.
Curcumin-loaded fibrinogen nanoparticles (CRC-FNPs) were synthesized via a
co-acervation technique with a size distribution of 150–200 nm and 90% loading
efficiency. The in vitro cytotoxicity assay performed using L929 (mouse fibroblast),
PC3 (prostate) and MCF-7 (breast) cancer cell lines confirmed that CRC-FNPs
were comparatively nontoxic to the L929 cell line but toxic to PC3 and MCF-7
cancer cells. The study also proved the apoptotic potential of CRC-FNPs in MCF-7
cells. Significant internalization of CRC-FNPs was observed in MCF-7 and PC3
cells, as monitored by fluorescent microscopy and flow cytometry-based uptake
studies. These results indicated that CRC-FNPs could be a promising therapeutic
agent for prostate and breast cancer treatment [122].
A variety of biodegradable polymers have been studied for nanoencapsulation of
curcumin and the nanoformulations have been evaluated in several in vitro and
in vivo models. Based on the safety profile of poly(lactic-co-glycolic) acid
(PLGA), researchers are interested in nanoformulations based on PLGA. A simple
solid-oil–water solvent evaporation method has been used to prepare curcuminloaded PLGA nanospheres. Curcumin nanospheres (mean particle size 45 nm)
exerted a pronounced effect on prostate cancer cells (LNCaP, PC3 and DU145)
in vitro. Figure 3 illustrates the curcumin-PLGA nanospheres in vitro in prostate
cancer cells [123]. Grabovac and Bernkop [124] studied the effect of surface
functionalization on curcumin-PLGA NPs using thiolated chitosan and Thamake
et al. [125] studied surface-functionalized curcumin-PLGA NPs with a homobifunctional spacer, bis(sulfosuccinimidyl) suberate (BS3), that facilitated
216
S. Maya et al.
by the self-assembly of curcumin into monopolymeric carrier (EC) and dipolymeric
carrier (ECMC, a blend of EC and MC) with 50% loading. The nanospheres showed
a dose-dependent cytotoxicity and free radical scavenging activity towards human
breast adenocarcinoma (MCF-7) and HepG2 cells in vitro. The nanosystems were
evaluated in vivo for their adherence to stomach mucosa and their ability to release
curcumin into the circulation via oral administration into mice. The authors reported
that curcumin sustainability in blood was improved by the nanoencapsulation [117].
The aqueous solubility and stability over a wide pH range of curcumin was enhanced
by its nanoencapsulation in a biodegradable polymeric methoxyPEG-palmitate
amphiphilic conjugate. The study also reported that nanoencapsulated curcumin
inhibited human cervical cancer (Hela) cell proliferation (half-maximal inhibitory
concentration, IC 50 ¼ 15.58 mM) comparably to free curcumin (IC 50 ¼ 14.32 mM),
thereby showing its anticancer activity in Hela cells in vitro [118].
It was reported that curcumin has been encapsulated in nontoxic and nonimmunogenic human serum albumin (HSA) nanoparticles. Albumin-bound nanoparticle technology is an easy fabrication process that does not use any toxic
surfactants and is well tolerated in vivo [119, 120]. Curcumin-HSA NPs
(130–150 nm) improved the water solubility of curcumin by 300-fold and enhanced
its in vivo antitumor activity (50–66% tumor growth inhibition) in a tumor xenograft HCT-116 model. Kim et al. suggested that this potent antitumor activity of
curcumin-HSA NPs could be due to the enhanced water solubility, increased
accumulation in tumors, and an ability to traverse vascular endothelial cells
[121]. In another study, fibrinogen was used as a nanocarrier for curcumin.
Curcumin-loaded fibrinogen nanoparticles (CRC-FNPs) were synthesized via a
co-acervation technique with a size distribution of 150–200 nm and 90% loading
efficiency. The in vitro cytotoxicity assay performed using L929 (mouse fibroblast),
PC3 (prostate) and MCF-7 (breast) cancer cell lines confirmed that CRC-FNPs
were comparatively nontoxic to the L929 cell line but toxic to PC3 and MCF-7
cancer cells. The study also proved the apoptotic potential of CRC-FNPs in MCF-7
cells. Significant internalization of CRC-FNPs was observed in MCF-7 and PC3
cells, as monitored by fluorescent microscopy and flow cytometry-based uptake
studies. These results indicated that CRC-FNPs could be a promising therapeutic
agent for prostate and breast cancer treatment [122].
A variety of biodegradable polymers have been studied for nanoencapsulation of
curcumin and the nanoformulations have been evaluated in several in vitro and
in vivo models. Based on the safety profile of poly(lactic-co-glycolic) acid
(PLGA), researchers are interested in nanoformulations based on PLGA. A simple
solid-oil–water solvent evaporation method has been used to prepare curcuminloaded PLGA nanospheres. Curcumin nanospheres (mean particle size 45 nm)
exerted a pronounced effect on prostate cancer cells (LNCaP, PC3 and DU145)
in vitro. Figure 3 illustrates the curcumin-PLGA nanospheres in vitro in prostate
cancer cells [123]. Grabovac and Bernkop [124] studied the effect of surface
functionalization on curcumin-PLGA NPs using thiolated chitosan and Thamake
et al. [125] studied surface-functionalized curcumin-PLGA NPs with a homobifunctional spacer, bis(sulfosuccinimidyl) suberate (BS3), that facilitated
216
S. Maya et al.