Medicament using rare earth transferring complex compound as vector
A technology of transferrin and complexes, which is applied in the direction of transferrin, drug combinations, animal/human proteins, etc., can solve the problems of increasing the cost of drug transport systems, achieve high drug transport efficiency, reduce costs, and make simple preparations Effect
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Embodiment 1
[0063] Preparation of doxorubicin-rare earth transferrin complex targeted anticancer drug
[0064] Doxorubicin is currently a common antibiotic anticancer drug. In order to improve its targeting type, it can be prepared into a doxorubicin-rare earth transferrin complex drug, and the method is briefly described as follows:
[0065] Preparation of rare earth transferrin: Dissolve transferrin Tf (product of Sigma Inc) (2-20mg / ml) in acetic acid buffer solution (0.1M, pH=5.5) containing EDTA (1-10mM) and Vc (10-50mM) ) at 4°C overnight. Then the reaction solution was passed through a Sephadex G-25 gel column (preliminarily equilibrated with 0.1M Tris-HCl buffer solution, pH=7.4) to collect protein components to obtain apo-transferrin Apo-Tf. Add 1:2-5 rare earth trivalent ions (La, Ce, Pr, Nd, Sm, Eu, Gd, Tb, Dy, Ho, Er, Tm, Yb, Lu, Sc, Y to the above-mentioned Apo-Tf solution ), react at room temperature for 0.5-1 hour, and then pass through a SephadexG-25 gel column to collec...
Embodiment 2
[0071] Rare earth transferrin modified nano-realgar drug
[0072] Arsenic compounds can effectively treat leukemia, and nano-realgar is a substitute for As 2 o 3 promising alternative medicines. However, the absorption of realgar is not good, and the targeting ability in the blood is poor. Rare-earth transferrin can be modified to increase its absorption capacity and targeting, the method is briefly described as follows:
[0073] Rare earth transferrin was prepared by the aforementioned method.
[0074] Rare earth transferrin was dissolved in PBS (0.1mol / L, pH6.3) at a concentration of 2mg / mL. Add S-acetylmercaptosuccinaldehyde at a molar ratio of 1:5. React at room temperature for 1 hour. Then add 0.05 mol / L hydroxylamine, react at 30° C. for 30 minutes (deacetylation) to obtain thiol-activated rare earth transferrin. Diluted to 0.5mg / ml for use.
[0075] Add realgar powder into a ball mill at a ratio of 1 g of realgar: 100 ml of water, and grind at a speed of 500 r / m...
Embodiment 3
[0079] Rare earth transferrin modified albumin nanospheres loaded with cisplatin
[0080] Cisplatin is one of the main anticancer drugs at present. Cisplatin is highly toxic and cannot be used orally. Rare earth transferrin can be used as a carrier to increase its targeting type and improve oral utilization, and the use of nano-microsphere encapsulation can improve its controlled release efficiency. The method is briefly described as follows:
[0081] Low-ratio biotinylated rare-earth transferrin was prepared by the aforementioned method. Dilute to 0.5mg / ml solution.
[0082] Human serum albumin (200g / L) was added to biotin succinic acid imide activated ester BNHS (20mg / ml, DMSO solution) at a molar ratio of 1:2, and reacted at room temperature for 1 hour to obtain biotinylated human serum albumin.
[0083] Prepare cisplatin-loaded albumin nano-microspheres by emulsification polycondensation method [Zhang Ming et al., Acta Pharmaceutica Sinica, 1994, 29: 380], briefly desc...
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