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Thymidylate synthase preparation loaded albumin nano-microsphere and preparation method thereof

A nanotechnology of thymidylate synthase and albumin, which is applied in the direction of medical preparations containing active ingredients, drug combinations, organic active ingredients, etc., to achieve good dispersion, good slow-release effect, in vivo performance, and high solubility

Inactive Publication Date: 2015-01-28
NANJING UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to provide a biocompatible, biodegradable, low systemic toxicity, which can be used as a kind of albumin nanosphere loaded with thymidylate synthase inhibitor for cancer treatment and its preparation Method, solves the problem of delivery of hydrophobic thymidylate synthase inhibitors in vivo

Method used

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  • Thymidylate synthase preparation loaded albumin nano-microsphere and preparation method thereof
  • Thymidylate synthase preparation loaded albumin nano-microsphere and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0034] Example 1 Preparation of Loaded Pemetrexed Modified Bovine Serum Albumin Drug-loaded Nanoparticles

[0035] In a 4mL reactor, dissolve 25mg bovine serum albumin and 6.3mg dithiothreitol in 1mL distilled water, react at 37°C for 0.5h, add sodium hydroxide solution to adjust the pH of the system to 8.0, add dropwise 1.5mg / 1.5 mL pemetrexed acetone solution to form nano-microspheres, add 20 μL of 0.5 mg / mL calcium sulfate solution and react for 15 minutes, react at 60°C for 5 minutes, and rotate at 37°C for 15 minutes. The ultrafiltration centrifuge tube was centrifuged to obtain the aqueous phase dispersion of the modified bovine serum albumin drug-loaded nano-microspheres. Adding 2% mannitol of the total mass of the system to freeze-dry to obtain drug-loaded nano microsphere powder.

Embodiment 2

[0036] Example 2 Preparation of modified bovine serum albumin drug-loaded nanospheres loaded with raltitrexed

[0037]In a 4mL reactor, dissolve 15mg of bovine serum albumin and 4.8mg of dithiothreitol in 1mL of distilled water, react at 37°C for 0.5h, add hydrochloric acid solution to adjust the pH of the system to 5.0, and dropwise add 1.5mg / mL of threitol Tetrexed absolute ethanol solution 1.1mL, form nano-microspheres, add 20 μL of 0.5 mg / mL zinc sulfate solution and react for 15 minutes, add 0.02 mM calcium sulfate solution 100 μL, stir for 2 hours, 37 ° C rotary evaporation for 15 minutes, nano-microspheres Ultracentrifuge at 12,000 rpm for 3 minutes, and redissolve to obtain the aqueous phase dispersion of modified bovine serum albumin drug-loaded nano-microspheres. Adding 2% mannitol of the total mass of the system to freeze-dry to obtain drug-loaded nano microsphere powder.

Embodiment 3

[0038] Example 3 Preparation of modified bovine serum albumin drug-loaded nanospheres loaded with raltitrexed

[0039] In a 4mL reactor, dissolve 15mg of bovine serum albumin and 3.5mg of mercaptoethanol in 1mL of distilled water, react at 37°C for 0.1h, add sodium hydroxide solution to adjust the pH of the system to 9.0, and dropwise add 1.5mg / mL Ratidine Add 1.5 mL of anhydrous ethanol solution of Trexed to form nano-microspheres, add 20 μL of 0.25 mg / mL calcium chloride solution and react for 2 hours, then react at 70°C for 2 minutes, then evaporate at 37°C for 15 minutes, freeze and centrifuge the nano-spheres at 100,000 rpm After 5 minutes, redissolve to obtain the aqueous phase dispersion of modified bovine serum albumin drug-loaded nano-microspheres. Adding 5% of the total mass of glucose to the system is freeze-dried to obtain drug-loaded nano-microsphere powder.

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Abstract

The invention provides a thymidylate synthase preparation loaded albumin nano-microsphere. The nano-microsphere is prepared by the following steps: adding a solution of a thymidylate synthase preparation and an organic solvent into an albumin solution to develop and self-assemble the albumin to form a nano-microsphere; coating the thymidylate synthase preparation in the albumin nano-microsphere to form the thymidylate synthase preparation loaded albumin nano-microsphere, wherein the diameter of the albumin nano-microsphere is 40-500nm, and the thymidylate synthase preparation is 7-20 percent by mass of the albumin nano-microsphere. The nano-microsphere has the advantages of excellent biocompatibility, simple preparation process and stable physiochemical property, is capable of improving the drug stability, has a certain sustained release effect, and has potential application of clinical cancer treatment. The invention further discloses a preparation method of the thymidylate synthase preparation loaded albumin nano-microsphere.

Description

technical field [0001] The invention relates to an albumin nano-microsphere loaded with a thymidylate synthase inhibitor and a preparation method thereof. Background technique [0002] Antimetabolite antineoplastic drugs cause tumor cell death by inhibiting the metabolic pathways necessary for tumor cell survival and replication. Since tumor cells have not yet been found to have a unique metabolic pathway, anti-metabolites are less selective, and are also toxic to normal tissues that proliferate rapidly, such as bone marrow and digestive tract mucosa. The anti-tumor spectrum of anti-metabolism anti-tumor drugs is relatively narrow, and most of them are used to treat leukemia clinically, but they are also effective for some solid tumors. Due to the different action points of anti-metabolite drugs, there is generally no cross-resistance. According to the requirements of the basic theory of anti-metabolism, the structure of anti-metabolites is generally similar to that of met...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/519A61K31/4709A61K47/42A61P35/00
Inventor 蒋锡群武伟张兆恒杨治旻章晓骅
Owner NANJING UNIV
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