Preparation and Primary Bioactivity Evaluation of Novel Water-Soluble Curcumin-Loaded Polymeric Micelles Fabricated with Chitooligosaccharides and Pluronic F-68

Abstract

Curcumin (CU) is a bioactive compound extracted from turmeric and has various advantages. However, the benefit of CU is limited by its low water solubility (11 ng/mL). This research aimed to fabricate a water-soluble CU nano-formulation with chitooligosaccharides (COS) and pluronic F-68 (PF) utilizing the polymeric micelle method. The optimized curcumin-loaded chitooligosaccharides/pluronic F-68 micelles (COSPFCU) exhibited high encapsulation efficiency and loading capacity (75.57 ± 2.35% and 10.32 ± 0.59%, respectively). The hydrodynamic diameter of lyophilized COSPFCU was 73.89 ± 11.69 nm with a polydispersity index below 0.3. The COSPFCU could be completely redispersed in water and showed high DPPH scavenging ability. Meanwhile, COSPFCU could significantly reduce the cytotoxicity of the RAW 264.7 cells compared to native CU. Furthermore, COSPFCU improved the inhibition of NO release activity at 72.83 ± 2.37% but 33.20 ± 3.41% for the CU, with a low cytotoxicity concentration in the RAW 264.7 cells.

Gemcitabine-Vitamin E Prodrug-Loaded Micelles for Pancreatic Cancer Therapy

“…The sizes of the Pluronic ® F68/VES-GEM micelles and the Pluronic ® F127/VES-GEM micelles were in the range of 10-80 nm and 50-300 nm, which revealed the most frequent subpopulation and attenuates the weight of the rare but larger particles in intensity mode analysis (Figure 6B,D). The VES-GEM-loaded micelles have a slightly negative surface charge (−5.38 ± 1.60 mV for Pluronic ® F68/VES-GEM and −1.54 ± 1.08 mV for the Pluronic ® F127/VES-GEM conjugate micelles), which is in accordance with values reported in the literature [53,54]. The absorbance spectra for the VES-GEM conjugate in ethanol at different concentrations and the GEM, VES-GEM, and micelle formulations are shown in Figure 6E,F, and the appearance of the non-filtered Pluronic ® F68/VES-GEM and Pluronic ® F127/VES-GEM micelles is depicted in Figure 6G.…”

“…Human blood (treated with citrate dextrose solution) from anonymized healthy donors (written informed consent) in accordance with Spanish legislation (Law 14/2007 on Biomedical Research [ 69 ]) was kindly provided by the Galician Transfusion Center (ADOS). Then, it was diluted with PBS [ 53 ] (final volume of 3.5% v / v ). The Pluronic ® micelle formulations (0.1 mL) were placed in Eppendorf tubes containing diluted blood (0.9 mL), followed by incubation at 37 °C/1 h under gentle shaking (100 rpm) [ 70 , 71 ].…”

“…Their hydrophilic–lipophilic balance (HLB) value is within 20–29 and the PPO chain length of Pluronic ® F127 is twice that of Pluronic ® F68 [ 48 , 49 ]. Recently, mixed Pluronic ® F68 micelles were loaded with docetaxel (20 mg/mL F68, 2% w / v ; 0.8 mg/mL docetaxel, 0.08% w / v ) [ 52 ] and curcumin (5 mg/mL F68, 0.5% w / v ; 1 mg/mL curcumin, 0.1% w / v ) [ 53 ] and Pluronic ® F127 (F127) micelles were investigated for delivery of curcumin (20 mg/mL of F127, 2% w / v ; 0.1 mg/mL, 0.01% w / v curcumin) [ 54 ], alpha-lipoic acid (20 mg/mL of F127, 2% w / v ; 10 mg/mL, 1% w / v ) [ 55 ], hypericin [ 56 ], β-escin (5 mg/mL F127, 0.5% w / v , 5 mg/mL β-escin, 0.5% w / v ) [ 57 ], boron-dipyrromethene dimer [ 58 ], lenvantinib [ 59 ], and a photosensitizer (1.11 mg/mL F127, 0.11% w / v ) [ 60 ], hence comprising biofunctional and suitable delivery systems for loading poorly water-soluble drugs with enhanced stability. Mixed Pluronic ® micelles have also been reported in the literature as a means to increase the solubility profile of poorly water-soluble drugs [ 61 , 62 ].…”

Water soluble curcumin with alkyl sulfonate moiety: Synthesis, and anticancer efficacy

“…Into the bargain, curcumin has been functionalized with a single methacrylate group to create a monomer termed MMC, which is another technique to enhance its limited solubility and quick breakdown in water [ 49 ]. Additionally, polymeric micelle approach cytotoxicity concentration-based water-soluble curcumin nano-formulation using chito-oligosaccharides and pluronic F-68 showed promise as a potential drug delivery mechanism, allowing scientists to circumvent the low curcumin water solubility restriction enhancing suppression of NO release activity and considerably decreased cytotoxicity of leukemia cells as compared to natural curcumin [ 50 ].…”