Construction Of A System Of Methyl Cellulose Mixed With Food Derived Polysaccharides For The Delivery Of Curcumin And Its Bioavailability

With the progress of the times,people had more demand for healthy food.Bioactive substances have a variety of physiological characteristics,so they are favored.However,some bioactive substances,such as curcumin,have strong hydrophobicity and extremely low solubility,resulting in poor effect of their individual administration.Therefore,delivery methods such as solid dispersion system,nano-embedding technology,microcapsule encapsulation technology and liposome encapsulation technology came into being.Hydrophobic drugs in the solid dispersion were dispersed in the hydrophilic polymer matrix in an amorphous form,increasing the solubility and bioavailability.Methylcellulose(MC)is a kind of non-ionic cellulose ether,which has been used in cosmetics,medicine and food industry.However,MC aqueous solution is not decomposed by enzymes in the range of p H 2～12,which made the solid dispersion flocculate and precipitate in the gastrointestinal fluid,and the combination of other biological molecules could alleviate this characteristic.In this study,curcumin solid dispersions(Cur SDs)were prepared from carboxymethyl cellulose(CMC),fenugreek gum(FG),fenugreek extract and methylcellulose for encapsulation and transportation of curcumin.The specific research results were as follows:1.CMC improved the wettability and solubility of Cur SDs and endows Cur SDs with the characteristics of controlled release.DSC results showed that curcumin was successfully embedded.Pyrene fluorescence probe showed that curcumin had hydrophobic binding with hydrocolloid carrier.The results of infrared and Raman spectroscopy showed that MC and curcumin were bound by hydrogen bond or hydrophobic interaction,and CMC enhanced the interaction,and curcumin was enol structure.The antioxidant activity test showed that CMC increased the antioxidant activity of Cur SDs to the same level as free curcumin,and had a beneficial effect on the result protection of curcumin.In the cell experiment,the antiproliferation effect of Cur SDs on HT-29 cells increased with the increase of CMC.According to SPSS 22.0,IC50 of M-CUR,C1-CUR,C3-CUR to C5-CUR(with increasing CMC addition)were 178.685 μg/m L,9.883 μg/m L,6.585 μg/m L and 1.751 μg/m L respectively.It showed that the hydrophilicity of CMC helped Cur SDs dispersed more evenly in water and released curcumin,thus enhancing the absorption of drugs by cancer cells.2.CMC in the previous chapter had greatly improved the hydrophilicity of Cur SDs,but the drug loading of curcumin had not been significantly improved.In this chapter,FG compound MC was used to increase the drug loading of Cur SDs to 50%.XRD analysis showed that curcumin in the prepared Cur SDs was amorphous.The infrared spectrum also showed that the OH group in curcumin formed hydrogen bond or hydrophobic interaction with the hydroxyl group of MC or FG.At this time,curcumin was enol type.The change of peak intensity ratio of pyrene fluorescence probe indicated that there was a competitive hydrophobic interaction between curcumin and pyrene probe in the carrier,and the hydrophobic interaction between FG and MC did not exist or dominate.Antioxidant activity test showed that the structure of curcumin was well protected by the embedding of MC and FG.The anti-proliferation effect of Cur SDs on HT-29 cells increased with the increase of FG.F3-CUR and F4-CUR with high FG content at low concentration(10 μg/m L),the inhibition rate was 85.9% and 95.6%.3.Because the anti-solvent method is not applicable in industrial production.And the fenugreek extract also contains a variety of small molecular substances including cucurbitacin,which can improve the absorption and utilization of curcumin in the body.Therefore,in this chapter,Cur SDs encapsulated in fenugreek extract and MC were prepared by p H shift method,and compared with products in the same market.The results showed that fenugreek extract improved the solubility of Cur SDs in water.The effect of highly concentrated fenugreek extract was better and similar to the market sample.The dissolution curve in HCl solution and PBS solution showed that the they were controlled release systems.The infrared spectrum showed that the OH group and C=O in curcumin formed hydrogen bonds with the OH groups of MC or fenugreek extract.The antioxidant activity test found that the antioxidant activity of F10-CUR was significantly higher than that of market samples,similar to free curcumin.That is,the lower concentration of fenugreek extract combined with MC had better protective effect.Both the research sample and the market sample had anti proliferative effects on HT-29 cells,with the market sample having slightly stronger effects.