Folic acid-cyclodextrin conjugate, drug delivery carrier, preparation method and use

A technology for delivering carriers and conjugates, applied in the field of medicine and chemical industry, can solve the problems of neurotoxicity, inability to achieve therapeutic effects, poor targeting, etc., and achieve high hydrophilicity, good external hydrophilicity, and improved targeting. Effect

Inactive Publication Date: 2018-05-22
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the targeting of platinum-based drugs is poor, and the general drug dose cannot achieve the therapeutic effect. Excessive doses will cause a large number of drugs to act on normal cells and tissues, resulting in bone marrow suppression, gastrointestinal reactions, nephrotoxicity, and neurotoxicity after chemotherapy. and other adverse reactions, thus limiting the use of platinum-based chemotherapy drugs

Method used

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  • Folic acid-cyclodextrin conjugate, drug delivery carrier, preparation method and use
  • Folic acid-cyclodextrin conjugate, drug delivery carrier, preparation method and use
  • Folic acid-cyclodextrin conjugate, drug delivery carrier, preparation method and use

Examples

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preparation example 1

[0059] (1) Raw materials:

[0060] Fullerene C 60 : Purchased from Puyang Yongxin Fullerene Technology Co., Ltd., purity ≥ 98%.

[0061] Folic acid: purchased from Sigma, purity ≥ 97%, Lot: 081M1546V.

[0062] γ-cyclodextrin: purchased from Adamas Reagent Company, purity ≥ 98%, Lot: P1064982.

[0063] Carboplatin: purchased from Beijing Ouhe Technology Co., Ltd., purity ≥ 98%, batch number: 120330.

[0064] 1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride: purchased from Adamas Reagent Company, purity ≥ 97%, Lot: P1064982.

[0065] N-Hydroxysuccinimide: purchased from Sinopharm Chemical Reagent Co., Ltd., purity ≥ 97%, batch number: F20101019.

[0066] 5% (w / w) glucose injection: purchased from Shijiazhuang Siyao Group, batch number: 110505702.

[0067] (2) Preparation process: the synthetic route of the pharmaceutical composition (drug delivery system) is as follows figure 1 shown.

[0068] a) Synthesis of folic acid-γ-cyclodextrin conjugate: the synthetic r...

preparation example 2

[0076] Grind 1.5 parts by weight of folic acid-γ-cyclodextrin conjugate and 1 part by weight of pre-adsorbed body in methanol (analytically pure, ≥99.5%) in the dark for 3 hours, collect the ground product, dry it with nitrogen, add 20 mL of double-distilled Stir with water, then centrifuge at 5000r / min for 2min to remove residual C 60 Fragments, stored at 4°C protected from light. Others were the same as in Example 1 to obtain drug delivery system 2.

[0077] The present invention includes but not limited to using carboplatin (C 6 h 12 N 2 o 4 Pt) as the active ingredient of the drug, cisplatin (Pt(NH 3 ) 2 Cl 2 ), oxaliplatin (C 8 h 14 N 2 o 4 Pt), nedaplatin (C 2 h 8 N 2 o 3 Pt), Le Platinum (C 9 h 18 N 2 o 3 Pt), Saite Platinum (C 10 h 22 C l2 N 2 o 4 Pt) and platinum prodrugs and other types of pharmaceutical active ingredients can be used to prepare the medicament of the present invention. Wherein, platinum prodrugs include but not limited to glu...

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Abstract

The invention belongs to the field of pharmaceutical chemicals, and relates to a folic acid-cyclodextrin conjugate, a folic acid-cyclodextrin-fullerene drug delivery carrier, a preparation method and use. Particularly, the folic acid-cyclodextrin conjugate is formed by connecting carboxyl of folic acid to hydroxyl of cyclodextrin; and in particular, the folic acid-cyclodextrin conjugate can be formed by connecting gamma carboxyl of folic acid to 6-position hydroxyls of gamma cyclodextrin. The invention further relates to the drug delivery carrier formed by using the conjugate to embed fullerene C60; in addition, the invention further relates to a folic acid-cyclodextrin-fullerene-platinum pharmaceutical composition, a preparation method and use. The folic acid-cyclodextrin-fullerene-platinum pharmaceutical composition disclosed by the invention has high targeting property to tumour cells, and can be used for inhibiting tumour cell proliferation.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and relates to a folic acid-cyclodextrin conjugate, a drug delivery carrier formed by embedding fullerene in the conjugate, a pharmaceutical composition, a preparation method and an application. Background technique [0002] The active ingredients of drugs often fail to achieve therapeutic purposes or produce toxic side effects because they cannot effectively reach the lesion site or act excessively on normal cells and tissues. For example, platinum-based drugs are typical, which are widely used in ovarian cancer, small cell lung cancer, testicular cancer, head and neck squamous cell carcinoma, cervical cancer, non-small cell lung cancer, bladder cancer, pleural mesothelioma, melanoma and uterine cancer. Chemotherapy for endometrial cancer. However, the targeting of platinum-based drugs is poor, and the general drug dose cannot achieve the therapeutic effect. Excessive doses will ca...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/54A61K47/40A61K45/00A61P35/00C08B37/16
Inventor 刘岩张英鸽孙岚姚红娟
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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