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Tumor targeted drug delivery system

A drug delivery system and tumor targeting technology, applied in antitumor drugs, drug combinations, pharmaceutical formulations, etc., can solve problems such as increased difficulty in preparation production, complex targeting carrier design, and uncertainty in preparation stability. It is difficult to control the quality of preparations, improve targeting and anti-tumor effects, and avoid the effects of difficult industrial production

Pending Publication Date: 2021-01-01
ANHUI MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can be seen that the current design of targeting preparations is mainly based on the improvement of the carrier material itself. Although a certain targeting effect has been achieved, there are certain limitations in the design of targeting preparations. In order to further improve the targeting effect, the target The design of vectors is becoming more and more complicated, which makes the production of preparations more difficult and brings uncertainties to the stability of preparations

Method used

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  • Tumor targeted drug delivery system

Examples

Experimental program
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Effect test

Embodiment 1

[0018] A tumor-targeted drug delivery system, comprising the following preparation steps:

[0019] (1) Dissolve 2.5 mg of doxorubicin hydrochloride (DOX HCL) in 1 mL of dimethylformamide (DMF), add 10 μL of triethylamine for dehydrochlorination, stir overnight at room temperature, and then add 10 mg of polyethylene glycol- Polycaprolactone (PEG2k-PCL2k), vortex to dissolve, to obtain a mixed solution, the mixed solution was dropped into 3mL PBS buffer solution with a pH value of 7.4 under stirring, after stirring for 60min, the ice bath was sonicated for 30min, and then purified with pure water Dialyze overnight, centrifuge the dialyzed inner solution (3000r / min for 10min), take the supernatant and filter it with a 0.8μm water membrane to obtain drug-loaded nanomicelles;

[0020] (2) Dilute the drug-loaded nanomicelles to a concentration of doxorubicin of 10 μmol / L, and add platycodon saponin D to make the concentration of platycodon saponin D 5 μmol / L, that is, the ratio of d...

Embodiment 2

[0032] A tumor-targeted drug delivery system, comprising the following preparation steps:

[0033] (1) Dissolve 1 mg of doxorubicin hydrochloride (DOX·HCL) in 1 mL of dimethyl sulfoxide (DMSO), add 10 μL of triethylamine for dehydrochlorination, stir overnight at room temperature, and then add 6 mg of polyethylene glycol-polyethylene glycol Lactic acid (PEG2K-PDLLA2K) was vortexed to dissolve to obtain a mixed solution, and the mixed solution was dropped into 2 mL of PBS buffer solution with a pH value of 7.4 under stirring, after stirring for 60 minutes, ultrasonication in an ice bath for 30 minutes, and then dialyzed with pure water overnight, the Centrifuge the dialyzed inner fluid (3000r / min for 10min), take the supernatant and filter it with a 0.8μm water membrane to obtain nanomicelles;

[0034] (2) Dilute the drug-loaded nanomicelles to a concentration of doxorubicin of 10 μmol / L, and add platycodon saponin D to make the concentration of platycodon saponin D 5 μmol / L, t...

Embodiment 3

[0036] In step (2), the molar concentration ratio of doxorubicin and platycodon saponin D is changed to 4:1, and the rest are the same as in Example 2.

[0037] In the prepared tumor-targeted drug delivery system, the concentration of doxorubicin hydrochloride was 10 μmol / L, and the final concentration of Platycodon saponin D was 2.5 μmol / L.

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Abstract

The invention relates to a tumor targeted drug delivery system, which comprises the following steps: dissolving an antitumor drug in an organic solvent, adding a drug carrier, carrying out vortex dissolution to obtain a mixed solution, the mixed solution is dropped into a PBS buffer solution with the pH value of 7.4 while stirring, stirring for 40-80 min, carrying out ice bath ultrasonic for 20-40min, dialyzing with pure water overnight, centrifuging the dialyzed internal liquid, and filtering the supernatant with a 0.8 mu m water film, the drug-loaded nano-micelle is obtained and diluted tothe concentration of the antitumor drug, adding a channel ushering drug so that the molar concentration ratio of the antitumor drug to the channel ushering drug is (1-10): 1, mixing to obtain the tumor targeted drug delivery system is obtained by mixing uniformly. According to the invention, a channel ushering drug platycodon grandiflorum is combined with a nano-micelle, the operation is simple, the prepared tumor targeted drug delivery system has a very good curative effect, and improves the targeting property and the antitumor effect of antitumor drug tumor cells.

Description

technical field [0001] The invention relates to a tumor-targeted drug delivery system, which belongs to the technical field of medicine. Background technique [0002] Tumor is one of the malignant diseases with the fastest growing morbidity and mortality and the greatest threat to the health and life of the population. Drug therapy is the fastest-growing tumor treatment, which has become one of the important means of clinical treatment of tumors today. The drug resistance of tumor cells and the toxic and side effects of cytotoxic antitumor drugs and preparations exist in the antitumor treatment with chemical drugs, which are one of the main reasons for the failure of chemotherapy. The pharmaceutical solution is to research and develop targeted agents, so that the drugs that enter the body can gather as much as possible in the tumor tissue and effectively enter the tumor cells, reducing the impact on normal cells, tissues or organ functions, so as to improve efficacy and red...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/46A61K47/28A61K31/704A61P35/00
CPCA61K9/1075A61K47/46A61K47/28A61K31/704A61P35/00
Inventor 汤继辉张倩倩鲍健威段体杰何雨婷
Owner ANHUI MEDICAL UNIV
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