Construction And Bioactivity Of The Self-assembly Composite Nanodelivery System Loaded With Curcumin And Tetrahydrocurcumin

Natural products have better pharmacological activity and health care functions.They are widely developed to be applied in the fields of drugs,cosmetics and health care products in recent years.However,the shortcomings of water insolubility,low stability and poor bioabailability limits the application of natural products in actual production.This research is dedicated to the development of suitable natural self-assembled nanodelivery system to encapsulate natural molecule drugs,and improving the dispersion and stability of drugs in aqueous solution.Furthermore,the composite self-assembled nano delivery system was constructed by surface-modified through layer-by-layer assembly technology.It has achieved the control of drug release,improved the drug uptake capacity of cells and the in vivo bioavailability of drugs.Thus,it is expected to make a certain contribution to the application of natural products and the exploration of delivery systems.1.To improve the biological activity of tetrahydrocurcumin(THC),THC loaded sodium caseinate(NaCas)inclusion nanoparticles(THC@NaCas)were prepared by self-assembly of NaCas.The encapsulation efficiency of THC@NaCas was 98.02%.TEM and SEM shown that the particle size of nanoparticles was between 250-350 nm,which showing a spherical and irregular spherical structure.The formation mechanism of THC@NaCas was characterized by Zeta potential,XRD,FTIR and FS.At the same concentration,THC@NaCas had better tyrosinase inhibitory activity and intracellular antioxidant activity than free THC.In conclusion,the NaCas nanoparticles depicted a great potential as the delivery system for clinical application of THC.2.A novel composite protein ang inorganic nanodelivery system was built by layer-by-layer assembly technology.(Cur@NaCas)@CaP nanoparticles(NPs)was established using NaCas as a core to increase solubility,CaP as a core to improve stability and Cur as a model bioactive molecule.(Cur@NaCas)@CaP NPs demonstrated a uniform size distribution of 150-200 nm with a distinct core-shell structure.The thermal stability of NPs loaded Cur was enhanced 6.67 fold and the UV-light stability was remarkly improved 8.56 fold than free Cur.More importantly,pH-responsive release was achieved owing to the CaP surface coating.At the same time,(Cur@NaCas)@CaP NPs showed enhanced intracellular antioxidant activity,significantly improvements of cellular uptake and anti-cancer activity.This novel core-shell drug delivery system is very promising for enhancing the application of hydrophobic compounds in drug delivery and cancer treatment.3.As a model drug,Cur was encapsulated in zinc-adenine nanoparticles(Zn-Adenine)based on the self-assembly of the coordination matrix material.Hyaluronic acid(HA)was further functionalized on the surface of Cur@(Zn-Adenine)to realize a tumor-targeted delivery system.The formed Cur@(Zn-Adenine)@HA NPs had a good durg loading efficiency(98.9%)and drug loading rate(18.6%).The morphology was displayed by TEM and zeta potential,and encapsulation mechanism of nanoparticles was researched by XRD and FTIR.Besides,compared to free Cur,(Zn-Adenine)@HA loaded Cur had enhanced pH stability and thermal stability.In particular,Cur@(Zn-Adenine)@HA showed excellent biocompatibility and specificity of cancer cell CD44 protein targeting.When the concentration at 7 ?g/mL,the anti-tumor effect of NPs loaded Cur was enhanced about 2.58 fold than free Cur.Hence,the study offers a potential nano-platfrom and has certain potential for tumor therapy.