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Preparation method of MnO2 carrier coated drug precursor 5-ALA

A technology of 5-ALA and precursors, applied in the field of biomedical materials, to achieve good clinical application value

Inactive Publication Date: 2018-12-11
HUBEI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the high metabolic level of solid tumors, most tumor cells rely on anaerobic respiration to complete their metabolism, resulting in a hypoxic environment for tumor cells, making photodynamic therapy that relies on oxygen content passive.

Method used

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  • Preparation method of MnO2 carrier coated drug precursor 5-ALA
  • Preparation method of MnO2 carrier coated drug precursor 5-ALA
  • Preparation method of MnO2 carrier coated drug precursor 5-ALA

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] First dissolve 100mg of 5-ALA in 2ml of deionized water, adjust the pH to 7 and store; then take 200μL of 50mg / ml of 5-ALA, 14mg EDC, 9.3mg NHS, 4.8ml of deionized water and 25ml round bottom flask , React at room temperature for 30min; then add 0.486g BSA, react at room temperature for 12h; add 14mg of MnCl 2 And 4H 2 O was dissolved in 1ml of water and added dropwise to the reaction solution of the above step, and the pH of the reaction solution was adjusted to 11 with 1M NaOH; then transferred to a dialysis bag after 2h, and dialyzed with deionized water for 3 days to obtain the final product. Store in the refrigerator. Mn 2+ MnO is formed under the mineralization of blood bovine albumin 2 Thereby catalyzing endogenous H 2 O 2 Oxygen is generated, and the prepared 5-ALA is used as an intermediate product in the final step of biosynthesis of porphyrin, and is selected as a drug-carrying molecule to perform light action. The blood bovine albumin is used as a stabilizer ...

Embodiment 2

[0024] First dissolve 100mg of 5-ALA in 2ml deionized water, adjust the pH to 7 and store; then take 250μL of 50mg / ml 5-ALA, 14mg EDC, 9.3mg NHS, 4.8ml deionized water and 25ml round bottom flask , React at room temperature for 30min; then add 0.486g BSA, react at room temperature for 12h; add 14mg of MnCl 2 And 4H 2 O was dissolved in 1ml of water and added dropwise to the reaction solution of the above step, and the pH of the reaction solution was adjusted to 11 with 1M NaOH; then transferred to a dialysis bag after 2h, and dialyzed with deionized water for 3 days to obtain the final product. Store in the refrigerator. Mn 2+ MnO is formed under the mineralization of blood bovine albumin 2 Thereby catalyzing endogenous H 2 O 2 Oxygen is generated, and the prepared 5-ALA is used as an intermediate product in the final step of biosynthesis of porphyrin, and is selected as a drug-carrying molecule to perform light action. The blood bovine albumin is used as a stabilizer to minera...

Embodiment 3

[0026] First dissolve 100mg of 5-ALA in 2ml of deionized water, adjust the pH to 7 and store; then take 300μL of 50mg / ml of 5-ALA, 14mg EDC, 9.3mg NHS, 4.8ml of deionized water and 25ml round bottom flask , React at room temperature for 30min; then add 0.486g BSA, react at room temperature for 12h; add 14mg of MnCl 2 And 4H 2 O was dissolved in 1ml of water and added dropwise to the reaction solution of the above step, and the pH of the reaction solution was adjusted to 11 with 1M NaOH; then transferred to a dialysis bag after 2h, and dialyzed with deionized water for 3 days to obtain the final product. Store in the refrigerator. Mn 2+ MnO is formed under the mineralization of blood bovine albumin 2 Thereby catalyzing endogenous H 2 O 2 Oxygen is generated, and the prepared 5-ALA is used as an intermediate product in the final step of biosynthesis of porphyrin, and is selected as a drug-carrying molecule to perform light action. The blood bovine albumin is used as a stabilizer ...

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Abstract

The invention discloses a preparation method of a MnO2 carrier coated pharmaceutical precursor 5- ALA. The method comprises the following steps: first, dissolving 100 mg of 5-ALA in 2ml of deionized water to adjust the pH to 7 for storage; then putting 250mu L of 50 mg / ml 5-ALA, 14mg of EDC, 9.3mg of NHS and 4.8ml deionized water into a 25ml round-bottom flask, and reacting at room temperature for30min; then adding 0.486g of BSA, and reacting at room temperature for 12h; dissolving 14mg of MnCl2 and 4H2O in 1ml water, dropwise adding the obtained solution to the reaction solution obtained inthe above step, and adjusting the pH of the reaction solution to 11 with 1M NaOH; then transferring the reaction solution to a dialysis bag after 2h, dialyzing for 3 days in deionized water to obtaina final product, and storing the final product in a refrigerator at 4 DEG C. By using synthetic protein and drug molecular complex, and mineralizing multi-response type MnO2, the MnO2 carrier coated drug precursor not only can be used as a stabilizer to mineralize and synthesize MnO2, but also can be used as a carrier of 5-ALA to enhance the blood circulation time, thereby realizing enhanced photodynamic therapy.

Description

Technical field [0001] The invention relates to the field of biomedical materials, in particular to a multi-response MnO 2 Preparation of carrier-coated drug precursor 5-ALA and its application in photodynamic enhancement. Background technique [0002] Photodynamic therapy is a new method of tumor treatment. In simple terms, it is a method of irradiating a light source of a certain wavelength on the photosensitizer so that it can absorb light to convert local oxygen molecules into highly toxic reactive oxygen species, and induce cell apoptosis or necrosis. The photosensitizer, the light source and the oxygen at the treatment site have become the three essential components of photodynamic therapy. However, due to the high metabolic level of solid tumors, most tumor cells rely on anaerobic respiration to complete their metabolism, resulting in a hypoxic environment at the tumor cells, making photodynamic therapy dependent on oxygen content in a passive situation. However, the cha...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K47/42A61K47/02A61P35/00
CPCA61K41/0061A61K47/02A61K47/42A61P35/00
Inventor 徐祖顺刘佩熊雨轩
Owner HUBEI UNIV
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