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Pharmaceutical carrier, micelle, pharmaceutical preparation, and preparation method and use thereof

A drug and carrier technology, applied in the direction of drug combination, pharmaceutical formula, antineoplastic drugs, etc., can solve the problems of metabolism, poor excretion, clinical use restrictions, small drug loading, etc., and achieve simple operation, simple structure, and simple construction Effect

Active Publication Date: 2021-07-02
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the toxic and side effects in practical application, the clinical use is greatly limited.
[0005] Moreover, since most anticancer drugs in clinical application are hydrophobic drugs, they need to be solubilized by carriers before they can be used. It is urgent to develop safe and effective new preparations and drug-loaded delivery systems.
Many researches based on nanoparticle carriers are facing: 1. The toxicity of the carrier itself, because it can be used as a material for efficient delivery carrier, it often shows the problem of poor metabolism and excretion, resulting in potential carrier toxicity; 2. The selection of suitable carrier construction components, factors such as the composition and volume of the carrier will directly affect the type and amount of the drug loaded, the drug load is too small, the drug effect is too weak, if the drug load required by the constructed carrier If it is too large, it is likely to cause unacceptable side effects in practical applications due to the toxicity of the antitumor drug itself; 3. Stability issues, how to ensure the stability of the carrier itself and the drug-loaded nano-delivery system is also the carrier's problem. Difficult questions that designers and builders often face

Method used

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  • Pharmaceutical carrier, micelle, pharmaceutical preparation, and preparation method and use thereof
  • Pharmaceutical carrier, micelle, pharmaceutical preparation, and preparation method and use thereof
  • Pharmaceutical carrier, micelle, pharmaceutical preparation, and preparation method and use thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0229] Synthesis and characterization of embodiment 1 LMWH-TOS copolymer

[0230] The purpose of this example is to illustrate the synthesis method of LMWH-TOS copolymer and the characterization of LMWH-TOS copolymer. In this example, low molecular weight heparin (LMWH) and tocopheryl succinate (TOS) are illustrated by enoxaparin sodium and D-α-TOS respectively, and the prepared copolymers are also used in the following example 2- 6 in.

[0231] (1) Synthesis of LMWH-TOS copolymer

[0232] like figure 1 As shown, enoxaparin sodium and D-alpha-tocopheryl succinate were linked by synthesizing an ester bond that was cleavable by polyesterase in lysosomes at low pH.

[0233] 1. Preparation of enoxaparin sodium and D-α-tocopheryl succinate copolymer (HT)

[0234] (1) Dissolve the D-alpha-tocopherol succinate (403mg) and activator (EDC 253mg, NHS 152mg, DMAP40mg) in 15ml N,N-dimethylformamide (DMF) solvent, avoid Activation for 4 hours under light nitrogen protection; (2) Disso...

Embodiment 2

[0244] Example 2 Preparation of HT NPs, DT NPs, FT NPs

[0245] 1. Preparation of HT NPs

[0246] (1) Dissolve the D-alpha-tocopherol succinate (403mg) and activator (EDC 253mg, NHS 152mg, DMAP40mg) in 15ml N,N-dimethylformamide (DMF) solvent, avoid Activated for 4h under the condition of light nitrogen protection;

[0247] (2) Dissolve 200 mg of enoxaparin sodium in 8 ml of formamide solvent, and mix the solutions of the above steps (1) and (2). React for 72 hours at 30-33°C under the protection of light and nitrogen. After the reaction, a double-volume acetone precipitation method was used to remove unreacted D-α-tocopheryl succinate and activator to obtain a milky white gel-like precipitate. The above precipitate was dissolved in a small amount of deionized water, put into a dialysis bag with a molecular weight cut-off of 1000, and then lyophilized after dialyzed in deionized water for 48 hours.

[0248] (3) Dissolving the enoxaparin sodium and D-α-tocopheryl succinate ...

Embodiment 3

[0258] The preparation of embodiment 3 PBA-LMWH-TOS micelles

[0259] Taking the targeting molecule 3-aminophenylboronic acid (PBA) as an example, on the basis of the low molecular weight heparin-α-tocopheryl succinate copolymer (LMWH-TOS) prepared as in Example 1, directly through acylation The low molecular weight heparin-α-tocopherol succinate copolymer with targeting components can be prepared by reacting and bonding 3-aminophenylboronic acid (PBA). The specific connection steps are as follows:

[0260] Dissolve 200 mg of the powdered amphiphilic copolymer prepared in Example 1 and an activator (EDC 253 mg / NHS 152 mg) in 8 ml of N,N-dimethylformamide solvent. After activation for 3 hours, add 3-amino 5 mg of phenylboronic acid (PBA) was reacted in the dark under nitrogen protection for 24 hours, the reaction solution was dialyzed in pure water for 72 hours, and freeze-dried to obtain a white powder.

[0261] The white powder prepared above was dissolved in an aqueous mediu...

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Abstract

A drug carrier, micelle, anti-tumor and / or anti-tumor cell metastasis drug preparation, its preparation method and application. The drug carrier and micelles include: a) a hydrophilic part, the hydrophilic part contains a hydrophilic heparin compound; and b) a hydrophobic part, the hydrophobic part contains a hydrophobic vitamin E compound, and the hydrophilic The aqueous heparin compound is connected with the hydrophobic vitamin E compound in a specific way. The drug carrier and the micelle not only have the effect of anti-tumor metastasis, but also can achieve the excellent effect of simultaneously inhibiting tumor and tumor metastasis by further encapsulating anti-cancer drugs. In addition, the drug carrier and micelles have high stability, and the preparation method is simple and convenient for industrial production.

Description

technical field [0001] The present application relates to the field of pharmaceutical preparations, more specifically, to pharmaceutical carriers, micelles, anti-tumor and anti-tumor cell metastasis pharmaceutical preparations, and preparation methods and uses thereof. Background technique [0002] Malignant tumors are still one of the important diseases that threaten human health and cause high mortality worldwide. Despite efforts to remove tumors surgically, as well as chemotherapy, radiotherapy, etc., to try to treat or control related diseases, the survival rate of patients is still very low. Statistics show that within 5 years after resection of rectal cancer, liver cancer, pelvic cavity cancer, ovarian cancer and other patients, more than 50% of the patients still have one or more cancer metastasis. The high mortality rate of cancer-related diseases is largely attributed to tumor metastasis. Clinical data show that about 80% of tumor patients die because of local rec...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K47/36A61K47/22A61K45/00A61P35/00A61P35/04
CPCA61K9/1075A61K45/00A61K47/22A61K47/36
Inventor 何勤龙洋卢正则李曼张志荣
Owner SICHUAN UNIV
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