Preparation Of Transferrin Modified Curcumin Liposomes And The Study Of Neuroprotective Effect

The incidence rate of neurodegenerative diseases in the elderly population is increasing,but the current therapeutic effect is not satisfactory.Due to the existence of the blood brain barrier,most drugs can not enter the brain smoothly,which increases the difficulty of treatment.Curcumin is a type of traditional Chinese medicine monomer,which was mainly extracted from Curcumae longae Rhizhoma and Curcumae Rhizhoma.Curcumin has the effects of antioxidation,anti-inflammation,lipid-lowering,anticoagulant,tumor growth inhibition,anti-aging and free radical elimination,and anti-atherosclerosis,etc.,especially has significant effects on antioxidation and neuroprotection.However,curcumin has poor water solubility and can not enter the brain through the blood brain barrier,that makes less accumulation of drugs in the brain.It is clinically prepared into nanoparticles,microspheres and other dosage forms,however,most of the excipients are difficult to be metabolized,and long-term medication is likely to cause toxic side effects.In this experiment uses natural excipients were used,which not only improves the water solubility of curcumin,but also weakens the side effects caused by excipients;Install transferrin on the liposome surface and binds to the transferrin receptor on the blood brain barrier so as to propel the therapeutic effect.Screening of preparation methods,curcumin liposomes were prepared by the ethanol injection method,and optimize the preparation process was optimized;The average encapsulation efficiency of Cur-Lips was 88.91%,the drug loading was 1.88%;The average leakage rate at 30 d was 2.39%;the average particle size was 96.11±4.74 nm(n=3),and the average potential was-20.8±1.6 mV(n=3).Tf-Cur-LCL was prepared and optimize the preparation process was optimized;The average encapsulation efficiency of Tf-Cur-LCL was 90.72%,the average connection efficiency of Tf was 60.55%,the average particle size was 110.5±3.6 nm(n=3),and the average potential was-28.2±0.75 mV(n=3);the lyophilized protectant was 10% mannitol,when Tf-Cur-LCL was reconstituted,the encapsulation efficiency decreased by 3.11±1.45%;the cumulative release rate of Tf-Cur-LCL 72 h was 80.81%.The protective effect to PC-12 cells was the strongest when the concentration of Cur was 15?g/mL,Tf-Cur-LCL has stronger protective effect on PC-12 cells.In the targeted evaluation,after 10 hours of administration,Cur can hardly pass the extracorporeal blood brain barrier model,the transmittance of Cur-Lips is 12.73%,the transmittance of Tf-Cur-LCL is 37.34%.It is proved that the installation of Tf makes Tf-Cur-LCL more easily pass through the blood-brain barrier,has a certain degree of brain targeted,the aim is to increase the accumulation of drugs in the brain and achieved therapeutic effect.