A kind of compound micelle of amphotericin b polymer with high drug load and preparation method thereof

A technology of amphotericin and compound micelle, which is applied in the field of medicine and achieves the effects of not easy aggregation, good stability, improved range and convenience

Active Publication Date: 2017-01-11
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The purpose of the present invention is to provide a high drug-loading agent for the nephrotoxicity, hemolytic toxicity and transfusion reactions of existing clinical amphotericin B preparations such as amphotericin B for injection and amphotericin B liposome for injection. Quantitative Amphotericin B Polymer Composite Micelle Drug Delivery System

Method used

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  • A kind of compound micelle of amphotericin b polymer with high drug load and preparation method thereof
  • A kind of compound micelle of amphotericin b polymer with high drug load and preparation method thereof
  • A kind of compound micelle of amphotericin b polymer with high drug load and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1: Preparation of composite micelles of polyethylene glycol 2000-phosphatidylethanolamine and amphotericin B (molar ratio is 0.4:1)

[0046] Weigh 8.4 mg of amphotericin B and 10 mg of polyethylene glycol 2000-phosphatidylethanolamine and dissolve it in 20 ml of methanol, remove the organic solvent by rotary evaporation under reduced pressure in a water bath at 50 ° C, add 10 ml of distilled water, hydrate for 15 minutes, and pass through a micrometer of 0.22 μm Pore ​​membrane filtration, that is, composite micelles. It was measured that the encapsulation efficiency was 95.8%, the drug loading was 44.4%, and the particle size was 57.89nm.

Embodiment 2

[0047] Example 2: Preparation of composite micelles of polyethylene glycol 2000-phosphatidylethanolamine and amphotericin B (molar ratio is 4:1)

[0048] Weigh 0.8mg of amphotericin B and 10mg of polyethylene glycol 2000-phosphatidylethanolamine and dissolve in 10ml of methanol-dimethylsulfoxide (1:1), remove the organic solvent by rotary evaporation under reduced pressure in a water bath at 50°C, and add phosphoric acid 10 ml of buffer salt was hydrated for 20 minutes, filtered through a 0.22 μm microporous membrane, 20 mg of mannitol was added as a freeze-drying protective agent, and freeze-dried. Reconstituted with water for injection, the encapsulation rate was 99.5%, the drug loading was 7.4%, and the particle size was 60.03nm.

Embodiment 3

[0049] Example 3: Preparation of composite micelles of polyethylene glycol 4000-phosphatidylethanolamine and amphotericin B (molar ratio is 0.5:1)

[0050] Weigh 6.6mg of amphotericin B and 10mg of polyethylene glycol 4000-phosphatidylethanolamine and dissolve it in 18ml of methanol, remove the organic solvent by rotary evaporation under reduced pressure in a 60°C water bath, add 10ml of distilled water to hydrate for 15 minutes, and pass through a 0.22μm micropore Membrane filtration to obtain complex micelles. It was measured that the encapsulation efficiency was 98.7%, the drug loading capacity was 39.8%, and the particle size was 62.02nm.

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Abstract

The invention belongs to the field of biotechnology and particularly relates to a high drug-loading capacity amphotericin B polymer composite micelle and a preparation method thereof. According to the invention, polyethylene glycol-phospholipid with clinical application potentials and indissolvable amphotericin B are used to form amphotericin B polyethylene glycol-phospholipid composite micelle; amphotericin B can combine with polyethylene glycol-phospholipid to form the amphotericin B polymer composite micelle with high drug-loading capacity, high encapsulation efficiency and high stability through the electrostatic attraction function and the interaction between carbon chains. The amphotericin B polymer composite micelle is stable in normal saline and plasma and lower in toxicity and infusion reaction, can be diluted by adopting normal saline, and greatly improves the clinical application range and convenience.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a high drug-loading amphotericin B polymer composite micelle and a preparation method thereof, in particular to an intravenously injectable nanometer composite micelle preparation of amphotericin B and a preparation method thereof. Background technique [0002] Amphotericin B is a polyene broad-spectrum antifungal antibiotic. It is mainly used to treat deep fungal infections and has a high curative effect. It has been used clinically for nearly half a century and is known as the "gold standard" for antifungal infections. . [0003] The antifungal mechanism of amphotericin B is to combine with ergosterol on the fungal cell membrane, form micropores on the cell membrane, and make the intracellular substances extravasate, resulting in the death of the fungus. Because amphotericin B has a hydrophobic polyene structure and a hydrophilic polyhydroxyl structure, its critical aggregation...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K9/19A61K47/34A61K31/7048A61P31/10
Inventor 乔明曦崔莹冰陈大为赵秀丽胡海洋
Owner SHENYANG PHARMA UNIVERSITY
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