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Dextran-MLDH-fluorouracil super-molecular skeleton magnetic liposome

A magnetic liposome, fluorouracil technology, applied in the directions of liposome delivery, organic active ingredients, medical preparations of non-active ingredients, etc., can solve the problem of easy torn lipid capsule wall, drug leakage, lack of internal bonding Spatial distribution and other issues to achieve significant magnetic targeting specificity and stable plasma concentration

Active Publication Date: 2013-10-23
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Fe 3 o 4 , There is no internal combination between drug and lipid molecules and ideal space distribution in the capsule, and the phase interface is in a metastable state. Therefore, when the magnetic field is intervened, Fe in the capsule 3 o 4 The magnetic response of nanoparticles easily tears the lipid vesicle wall, leading to drug leakage, Fe 3 o 4 deposition

Method used

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  • Dextran-MLDH-fluorouracil super-molecular skeleton magnetic liposome
  • Dextran-MLDH-fluorouracil super-molecular skeleton magnetic liposome
  • Dextran-MLDH-fluorouracil super-molecular skeleton magnetic liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 Synthesis of DMFL liposomes, particle morphology and particle size distribution of characterization products

[0029] prescription:

[0030] DMF

6mg

Soy Lecithin

30mg

cholesterol

10mg

Chloroform

15mL

double distilled water

30mL

[0031] Preparation Process:

[0032] (1) Synthesis of DMF drug carrier: Weigh 39.76g of ferrous chloride and 27.03g of ferric chloride and put them in a sulfuric acid paper bag for later use; weigh 84g of dextran (DET) and dissolve it in 200mL of water; measure 69mL of 0.145mol L -1 The Fu solution is set aside. Assemble the nitrogen protection reaction system with a pH meter, stirring magnet, precipitant infusion drive system and 1000mL three-necked bottle, add 300mL double distilled water, and 2 1. Add two kinds of iron salts under the condition of magnetic stirring, add the solution after dissolving, stir and mix well, keep the temperature at 45°C and N 2 Under pr...

Embodiment 2

[0039] Example 2 Synthesis of DMFL according to the following prescription, detection of liquid phase pH value and in vitro magnetic targeting

[0040] DMF

6mg

Soy Lecithin

42mg

cholesterol

14mg

Chloroform

l5mL

double distilled water

20mL

[0041] Preparation process: The process flow for the synthesis of DMF and DMFL is the same as in Example 1. The raw materials were prepared according to the prescription list, the lipid film preparation temperature was 50°C, and emulsified for 30 minutes; FU original drug liposomes were prepared under the same prescription and process conditions, and were used as comparison samples for DMFL magnetic targeting verification.

[0042] Detection of liquid phase pH value and magnetic targeting in vitro: the pH value of DMFL was measured with a PHSJ-4A acidity meter. Take the same amount of DMF liposomes and FU liposomes, and pack them in different ampoules, use Φ17×3mm NdFeB perma...

Embodiment 3

[0043] Example 3 Synthesize DMFL according to the following prescription, detect in vitro release performance and cancer cell proliferation inhibition

[0044] DMF

6mg

Soy Lecithin

30mg

cholesterol

10mg

Chloroform

l5mL

double distilled water

3OmL

[0045] Preparation process: The synthesis process of DMF and DMFL is the same as in Example 1. The dosage of each component is shown in the prescription table. The lipid film preparation temperature is 45° C., emulsification for 30 minutes. Four batches of parallel samples of DMFL were synthesized under the same prescription conditions for the tests of encapsulation efficiency and pH; liposomes of FU original drug were prepared under the same conditions for in vitro release performance and tumor cell proliferation inhibitory activity tests as reference substances.

[0046] Determination of the drug encapsulation efficiency of liposomes: determined by dialysis. Precise...

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Abstract

The invention relates to a processing technology for dextran-MLDH-fluorouracil super-molecular skeleton magnetic liposome. The magnetic liposome takes dextran-MLDH-fluorouracil DMF three-grade super-molecular as the core skeleton, soya lecithin and cholesterol as the lipid raw materials, and is prepared by the reverse evaporating method. The DMF magnetic liposome has a typical in-vitro control release ability, a sensitive magnetic responding ability, an excellent cancer cell proliferation inhibiting ability and a special and durable in-vitro drug process. DMF magnetic liposome is prepared through combination of convention liposome technology and DMF, a novel inorganic nano drug delivery system, and a new approach is provided for magnetic target chemotherapy of fluorouracil, a wide-spectrum anti-cancer drug. The dextran-MLDH-fluorouracil super-molecular skeleton magnetic liposome is suitable for the preparation of magnetic drug liposome, which takes magnetic layered composite hydroxide MLDH as the carrier, has the processing advantages of low cost and simple preparation, and has the characteristics of integration of magnetic-target and control-release functions, durable effect, stable curative effect, and little toxic and side effects.

Description

technical field [0001] The invention belongs to the field of development of modern drug delivery systems and preparations thereof, and specifically relates to a magnetic liposome DMFL with the "dextran-MLDH-fluorouracil" supramolecular drug delivery system DMF as the core skeleton, which is suitable for anticancer drug magnetically targeted chemotherapy. Processing and production of magnetic liposomes are required. Background technique [0002] Fluorouracil is a broad-spectrum antineoplastic drug, which is often used in the treatment of gastrointestinal tumors, breast cancer, ovarian cancer and other diseases. Side effects such as bone marrow suppression. [0003] Liposome is a phospholipid bilayer microcapsule similar in structure to the cell membrane. It has the advantages of slow release, low toxicity, biocompatibility, good drug solubility, etc., and the possibility of targeted transformation and comprehensive processing. Therefore, it has become In recent years, the r...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/513A61K47/48A61P35/00
Inventor 苟国敬黄洁徐淑芳
Owner NINGXIA MEDICAL UNIV
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