Folic acid targeted antitumor medicine sustained-releasing carrier and preparation method of same

An anti-tumor drug, folic acid targeting technology, applied in the field of biomedical materials, can solve problems such as unreported research, achieve the effect of wide sources, low price, and inhibition of cancer cell division

Active Publication Date: 2018-03-02
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no report on the use of bioactive glass as a drug carrier and folic acid grafted on the surface as a "signal recognition molecule" for tumor cells.

Method used

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  • Folic acid targeted antitumor medicine sustained-releasing carrier and preparation method of same
  • Folic acid targeted antitumor medicine sustained-releasing carrier and preparation method of same
  • Folic acid targeted antitumor medicine sustained-releasing carrier and preparation method of same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1 Preparation of micro-nano bioactive glass powder (BG)

[0040] Bioactive glass powder was prepared by sol-gel method combined with organic template self-assembly technology. The specific synthesis process was as follows: firstly, 4 g of dodecylamine was added to a mixed solution of 25 ml of deionized water and 80 ml of absolute ethanol, Stir in a water bath at 40°C until completely dissolved; then add 10.87 ml of ethyl orthosilicate and stir for 30 min; add 1.13 ml of triethyl phosphate and stir for 30 min; add 6.87 g of calcium nitrate tetrahydrate; Stirring was continued for 3 h; finally, the glass sol was centrifuged to obtain a white precipitate, which was dried in a 60°C drying oven for 24 h, and then sintered in a muffle furnace at 650°C for 3 h to obtain a micro-nano bioactive glass powder with an average particle size of 480nm.

Embodiment 2

[0041] The preparation of embodiment 2 folic acid targeted antineoplastic drug sustained-release carrier (MTX-BG-FA)

[0042](1) Amino modification of micro-nano bioactive glass surface

[0043] Add 3 g of the micro-nano bioactive glass powder prepared in Example 1 into a mixed solution of 1.5 ml deionized water and 120 ml ethanol, ultrasonically disperse for 30 min, then add 3 ml of APTES drop by drop, and then in the condition of 65 ° C Stir the reaction for 6h, wash with deionized water and absolute ethanol, and dry in a vacuum oven at 60°C to finally obtain the aminated bioactive glass (BG-NH 2 ).

[0044] (2) Activate the carboxyl group of folic acid

[0045] Firstly, 0.14gDCC and 0.12gNHS were dissolved in 40.5mlDMSO. Next, 0.45 g of folic acid was added, stirred and reacted for 24 hours, and then filtered to remove the generated N,N-dicyclohexylurea, and the resulting solution contained folic acid molecules activated with a single carboxyl group.

[0046] (3) Peptid...

Embodiment 3

[0053] Example 3 Preparation of Folic Acid Targeted Antineoplastic Drug Sustained Release Carrier (MTX-BG-FA)

[0054] (1) Amino modification of micro-nano bioactive glass surface

[0055] Add 3 g of the micro-nano bioactive glass powder prepared in Example 1 into a mixed solution of 7.5 ml of deionized water and 120 ml of ethanol, ultrasonically disperse for 30 min, then add 15 ml of APTES drop by drop, and then, under the condition of 65 ° C, Stir the reaction for 6h, wash with deionized water and absolute ethanol, and dry in a vacuum oven at 60°C to finally obtain the aminated bioactive glass (BG-NH 2 ).

[0056] (2) Activate the carboxyl group of folic acid

[0057] Firstly, 0.14gDCC and 0.12gNHS were dissolved in 54mlDMSO. Next, 0.45 g of folic acid was added, stirred and reacted for 24 hours, and then filtered to remove the generated N,N-dicyclohexylurea, and the resulting solution contained folic acid molecules activated with a single carboxyl group.

[0058] (3) Pe...

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Abstract

The invention discloses a folic acid targeted antitumor medicine sustained-releasing carrier and a preparation method of same, and belongs to the field of biomedical materials. The sustained-releasingcarrier is prepared through the steps of: 1) preparing mono-dispersed micro-nano bioactive glass through a sol-gel method with combination of organic template self-assembly technology; 2) modifying the surface of the micro-nano bioactive glass by grafting amino groups via a silane coupling agent; 3) conjugating the amino groups with a gamma-carboxyl group on folic acid; and 4) supporting an antitumor medicine, methotrexate, onto the material through covalent combination. According to the invention, the folic acid is combined with a folate receptor on surface of a tumor cell membrane, and thenthe medicine carrier is transferred into a cell through the endocytosis of the cell membrane; with degradation of the bio-glass, the antitumor medicine is slowly released. The folic acid targeted antitumor medicine sustained-releasing carrier has good biocompatibility and improves efficiency that the carrier enters a tumor cell. The sustained-releasing carrier can be used in the fields of targeted therapy of tumor cells, medicine sustained releasing, bone tissue engineering, etc.

Description

technical field [0001] The invention belongs to the field of biomedical materials, and in particular relates to a sustained-release carrier of folic acid-targeted antitumor drugs and a preparation method thereof. Background technique [0002] Most drugs in traditional chemotherapy for tumor diseases are administered in common dosage forms, which are usually taken up by cells, tissues and organs, and randomly distributed in the body instead of targeted distribution in the lesion area. As a result, oral administration will be degraded and metabolized by enzymes in the gastrointestinal tract epithelial cells and liver, and injection administration will be subject to plasma protein binding and decomposition, and finally only a small part of the drug reaches the tumor lesion area. The two drug administration methods may make the drug concentration not reach the therapeutic effect, and the drug dosage must be increased to achieve the drug effect, which also increases the toxic and...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/54A61K31/519A61P35/00A61L27/54
CPCA61K31/519A61L27/54A61L2300/216A61L2300/412A61L2300/624A61L2430/02
Inventor 陈晓峰陈建辉杨峥宇谭晓君王佳晨陈瑶
Owner SOUTH CHINA UNIV OF TECH
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