A preparation method of layer-by-layer self-assembled nano-targeting carrier containing camptothecin

A layer-by-layer self-assembly and camptothecin technology, which is applied to medical preparations containing active ingredients, medical preparations with non-active ingredients, drug combinations, etc., can solve the problem of inability to accurately identify tumor cells, lung tumor cells, and normal cells damage, side effects and other issues, to achieve good targeting of liver cancer cells, to achieve controlled release, and strong biodegradability

Active Publication Date: 2018-08-14
NAT INST OF ADVANCED MEDICAL DEVICES SHENZHEN
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chemotherapy drugs used in clinical practice are not highly targeted and cannot accurately identify tumor cells or lung tumor cells
During the course of treatment, it not only kills tumor cells, but also may cause damage or death of normal cells that proliferate rapidly in the body, resulting in serious side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Preparation of targeted nanocapsules containing 3-layer capsule wall self-assembly layer by layer:

[0023] a. Preparation of reduction-sensitive chitosan derivatives: Take 50 g ε-caprolactone (ε-CL) as a monomer, 10 g benzyl alcohol as an initiator, and add 1 g Sn (Oct) 2 , at N 2 Stir continuously under the condition of 80°C in the environment, and continue to react for 12 hours to obtain polycaprolactone (PCL-OH). Add 0.8 g PCL-OH to 10 mL DCM solution, and dissolve 0.8 g p-nitrophenyl chloroformate (NPC) in 10 mL DCM, mix the two solutions, and react at room temperature for 24 hours to generate PCL-NPC . Dissolve 0.5 g cystamine and 2 mL triethylamine in 20 mL methanol, and after 10 min, dissolve 10 mL di-tert-butylmethyl dicarbonate (Boc 2 O) (0.4 g) methanol solution was slowly added dropwise to the above solution, N 2 Cys-Boc-Mono was formed by reaction at ambient room temperature for 6 hours. Dissolve 0.4 g PCL-NPC, 0.2 g Cys-Boc-Mono, and 0.4 mL triethylam...

Embodiment 2

[0030] Preparation of self-assembled targeted nanocapsules containing 5 layers of capsule walls:

[0031] The difference between this embodiment and embodiment 1 is that steps d and c are repeated once on the basis of having three layers of capsule walls. In addition, iota-carrageenan was dissolved in 2% acetic acid during the preparation process. The stirring reaction time was increased to 30 min for one-layer and two-layer sample preparation.

[0032] The targeted nanocapsules prepared in this example have a particle size of about 380 nm and a narrow particle size distribution. The cellular uptake rate of the nanocapsules reached 85.1%, and the HepG 2 Cell growth inhibition experiments were carried out on the nano-microcapsules loaded with HCPT, and the results showed that after 48 hours of culture, the tumor cell death rate was 85.2%.

Embodiment 3

[0034] Preparation of self-assembled targeted nanocapsules containing 5 layers of capsule walls:

[0035] The difference between this embodiment and embodiment 1 is that steps d and c are repeated once on the basis of having three layers of capsule wall. In addition, iota-carrageenan was dissolved in 0.5% acetic acid during the preparation process. The stirring reaction time was increased to 30 min for one-layer and two-layer sample preparation.

[0036] The particle size of the targeted nanocapsules prepared in this example is about 420 nm, and the particle size distribution is relatively narrow. The cellular uptake rate of the nanocapsules reaches 80.5%, and the HepG 2 Cell growth inhibition experiments were carried out on the nano-microcapsules loaded with HCPT, and the results showed that after 48 hours of culture, the tumor cell death rate was 78.3%.

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Abstract

The invention discloses a preparation method of a layer-by-layer self-assembled targeting nano-carrier containing camptothecin. According to the method, HCPT (hydroxycamptothecine) is taken as a model drug, chitosan which is a natural, non-toxic and degradable biomaterial is taken as a base material, a glycyrrhetinic acid receptor-mediated tumor active targeting technology is used, and layer-by-layer self-assembled nanoparticles capable of responding to special redox and pH environment of tumor tissue and tumor cells are prepared. Targeting nano-capsules prepared with the method have high monodispersion, controllable capsule wall thickness and cavity volume and reduction responsiveness, can control and release anti-tumor drugs in inner cavities into a microenvironment of the tumor cells, can be taken as a targeting transport tool for the anti-tumor drugs and have great application prospect in the field of targeted tumor therapy.

Description

technical field [0001] The invention belongs to the technical field of polymer drug carriers, and relates to a preparation method of a layer-by-layer self-assembled nano-targeting carrier containing camptothecin. Background technique [0002] In China, an average of more than three million new cancer cases are diagnosed each year, and the average annual death rate is as high as 2.7 million. Researchers are eager to explore effective methods to treat malignant tumors. The current effective treatment methods are still surgery, chemotherapy and radiotherapy. Chemotherapy drugs used in clinical practice are not highly targeted and cannot accurately identify tumor cells or lung tumor cells. During the course of treatment, it not only kills tumor cells, but also may cause damage or death of normal cells that proliferate rapidly in the body, resulting in serious side effects. [0003] Biomedical polymer materials are a field where the development trend of functional polymers is v...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K31/4745A61K47/36A61K47/02A61P35/00
CPCA61K9/0002A61K9/5115A61K9/5161A61K31/4745
Inventor 贺金梅颜廷胜程凤刘长瑜
Owner NAT INST OF ADVANCED MEDICAL DEVICES SHENZHEN
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