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Liposome capable of improving drug release and preparation method of liposome

A technology of liposomes and blank liposomes, which is applied in liposome delivery, drug combination, and pharmaceutical formulations, etc., and can solve problems such as reduced therapeutic effect, low solubility, and slow drug release speed

Inactive Publication Date: 2018-03-27
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For anthraquinone drugs, such as doxorubicin, etc., after the ammonium sulfate gradient method is used to prepare liposomes, although its cardiotoxicity is significantly reduced, but at the same time due to the formation of sulfate radicals and doxorubicin in the internal water phase, the solubility is relatively low. Low precipitation, which makes the drug release rate significantly slowed down, resulting in a significantly reduced therapeutic effect

Method used

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  • Liposome capable of improving drug release and preparation method of liposome
  • Liposome capable of improving drug release and preparation method of liposome
  • Liposome capable of improving drug release and preparation method of liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1: Preparation of drug-loaded liposomes by ammonium sulfate gradient method

[0031] a. Preparation of blank liposomes

[0032] Prepare blank liposomes by ethanol injection method, weigh hydrogenated soybean phospholipids (HSPC) 420mg, cholesterol (Chol) 140mg, polyethylene glycol 2000-distearoylphosphatidylethanolamine (PEG) 2000 -DSPE) 10 mg was dissolved in an appropriate amount of absolute ethanol to obtain a lipid ethanol solution, which was injected into a 0.3 mol / L ammonium sulfate solution at 60°C, stirred at high speed for 5 minutes, and the ethanol was removed by rotary evaporation in a water bath at 60°C. Pass through polycarbonate membranes of 0.8, 0.4, 0.2, and 0.1 μm in sequence at 60°C to reduce particle size and particle size distribution, use pH 6.5 phosphate buffer as the dialysis medium, and dialyze 10 times the volume through an ultrafiltration device To remove the ammonium sulfate in the external water phase, the blank liposomes were obt...

Embodiment 2

[0035] Embodiment 2: Preparation of drug-loaded liposomes by carboxymethylcyclodextrin triethylamine gradient method

[0036] a. Preparation of carboxymethyl-β-cyclodextrin triethylamine salt

[0037] Prepare carboxymethylcyclodextrin triethylamine salt by ion exchange method, weigh 9g carboxymethyl-β-cyclodextrin sodium and dissolve it in an appropriate amount of purified water, load the sample through a cation exchange resin column, elute with purified water, and remove the sodium The salt is replaced by the free carboxylic acid. Measure the conductivity of the eluate or detect the pH of the eluate during the elution process, and collect the components with pH<5. Titrate the collected eluent with triethylamine, monitor the pH of the solution with a pH meter, and titrate to a pH of 5.5-6.0, accurately record the volume of triethylamine, and dilute with purified water. Carboxymethylcyclodextrin triethylamine is produced at a concentration of about 0.1 mol / l.

[0038] b. Prepa...

Embodiment 3

[0042] Example 3: Encapsulation efficiency of drug-loaded liposomes prepared by different gradient methods

[0043] According to the method described in embodiment 1, 2, prepare the liposomes of encapsulating different medicines respectively, and measure the irinotecan hydrochloride liposomes, vincristine sulfate liposomes and doxorubic acid hydrochloride prepared by two kinds of gradient methods respectively See Table 1 below for the encapsulation efficiency of Bixing liposomes.

[0044] Table 1 entraps the drug-loaded liposomes prepared by different preparation methods to entrap different drugs

[0045]

[0046] The results showed that the above three drug-loaded liposomes prepared by carboxymethylcyclodextrin triethylamine gradient method could all achieve higher encapsulation efficiency.

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Abstract

The invention belongs to the field of pharmaceutical preparations and in particular relates to liposome and a preparation method thereof. The liposome comprises a lipid double-molecule layer and an inner water phase, wherein the inner water phase contains carboxymethyl cyclodextrin and an active compound. The carboxymethyl cyclodextrin comprises carboxymethyl-alpha-cyclodextrin, carboxymethyl-beta-cyclodextrin and carboxymethyl-gamma-cyclodextrin. By adopting the liposome provided by the invention, the drug releasing speed of the active compound in the liposome can be improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a liposome with an inner water phase of carboxymethylcyclodextrin salt and a preparation method thereof. The liposome composition can improve the release speed of medicine in the liposome. Background technique [0002] Liposome is a closed vesicular structure of biomembrane structure arranged by lipid bilayer. As a drug carrier, liposome has the characteristics of improving drug efficacy, reducing adverse drug reactions, targeting, and sustained release. Especially when used as a carrier of anti-tumor drugs, it can target the drug to the tumor area and play a role in attenuating and synergizing . [0003] According to the different mechanisms of drug loading, the preparation methods of liposome drugs can be divided into two categories: passive drug loading method and active drug loading method. For fat-soluble drugs with high affinity to phospholipid membr...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/40A61K31/4745A61K31/704A61K31/475A61P35/00
CPCA61K9/127A61K9/1278A61K31/4745A61K31/475A61K31/704A61K47/40
Inventor 周卫吴刚魏悦蕾张亚
Owner CHINA PHARM UNIV
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