Albumin-coated cabazitaxel cationic nano-lipid carrier and preparation method thereof

The technology of a nano-lipid carrier and cabazitaxel is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, which can solve the problems of large dosage, large toxic and side effects, and potential safety hazards, etc. problems, achieve high encapsulation efficiency, uniform particle size, and improve solubility

Active Publication Date: 2021-04-30
CHENGDU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The present invention well solves the problems that the existing cabazitaxel injection has large toxic and side effects, is prone to cause severe hypersensitivity, has large dosage, long time, relatively poor stability and potential safety hazards in drug administration.

Method used

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  • Albumin-coated cabazitaxel cationic nano-lipid carrier and preparation method thereof
  • Albumin-coated cabazitaxel cationic nano-lipid carrier and preparation method thereof
  • Albumin-coated cabazitaxel cationic nano-lipid carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Albumin-coated cationic nano-lipid carrier of cabazitaxel, including the following raw materials: 10 mg of cabazitaxel; 57 mg of stearic acid; 43 mg of glyceryl caprylate; 100 mg of egg yolk lecithin; 400 mg of Brij20; ; Human serum albumin 40mg.

[0037] Its preparation process is as follows:

[0038] Dissolve cabazitaxel, stearic acid, glyceryl caprylate, and egg yolk lecithin in an organic solvent at about 75°C (acetone:ethanol=1:1, 4ml in total), and use it as the oil phase for later use; mix Brij20 and hexadecyl Dissolve trimethylammonium bromide in ultrapure water at about 75°C, and use it as the water phase for later use; at a stirring speed of 1000r / min, use a syringe to absorb the oil phase and inject it into the water phase at a certain speed, and continue stirring and emulsifying at 75°C 1h, while hot, slowly drop the emulsion into pre-cooled ultrapure water, and continue stirring for 1h in an ice-bath environment to obtain Cbz-cNLCs. Take a certain amount ...

Embodiment 2

[0041] Albumin-coated cationic nano lipid carrier of cabazitaxel, including the following raw materials: cabazitaxel 10mg; stearic acid 57mg; caprylic / capric glycerides 43mg; egg yolk lecithin 100mg; Brij20 100mg; Ammonium chloride 10mg; human serum albumin 40mg.

[0042] Its preparation process is as follows:

[0043]Dissolve cabazitaxel, stearic acid, glyceryl caprate, and egg yolk lecithin in an organic solvent at about 75°C (acetone:ethanol=1:1, 4ml in total), and use it as the oil phase for later use; mix Brij20 and hexadecane Dissolve trimethylammonium bromide in ultrapure water at about 75°C, and use it as the water phase for later use; at a stirring speed of 1000r / min, use a syringe to absorb the oil phase and inject it into the water phase at a certain speed, and continue stirring at 75°C After emulsifying for 1 hour, slowly drop the emulsion into pre-cooled ultrapure water while it is still hot, and continue stirring for 1 hour in an ice-bath environment to obtain C...

Embodiment 3

[0046] Albumin-coated cationic nano lipid carrier of cabazitaxel, including the following raw materials: cabazitaxel 10mg; stearic acid 57mg; caprylic / capric glycerides 43mg; egg yolk lecithin 200mg; Ammonium chloride 10mg; human serum albumin 40mg.

[0047] Its preparation process is as follows:

[0048] Dissolve cabazitaxel, stearic acid, caprylic / capric glyceride, egg yolk lecithin in an organic solvent (acetone:ethanol=1:1, 4ml in total) at about 75°C, and use it as the oil phase for later use; Brij20 and ten Hexaalkyltrimethylammonium bromide is dissolved in ultrapure water at about 75°C and used as the water phase for later use; at a stirring speed of 1000r / min, use a syringe to absorb the oil phase and inject it into the water phase at a certain speed, at 75°C, Continue stirring and emulsifying for 1 hour, slowly drop the emulsion into pre-cooled ultrapure water while it is hot, and continue stirring for 1 hour in an ice-bath environment to obtain Cbz-cNLCs. Take a ce...

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Abstract

The invention provides an albumin-coated cabazitaxel cationic nano-lipid carrier and a preparation method thereof. The albumin-coated cabazitaxel cationic nano-lipid carrier is prepared from the following raw materials in parts by weight: 5-10 parts of cabazitaxel, 20-170 parts of solid lipid material; 20-parts of liquid lipid material; 50-300 parts of fat-soluble emulsifiers; 100-600 parts of water-soluble emulsifiers; 4-15 parts of cationic material; and 10-100 parts of albumin material; the cationic material comprises at least one of didecyl dimethyl ammonium bromide, dioleoyl trimethyl ammonium propane, dioleoyl propyl trimethyl ammonium chloride, dioleoyl phosphatidylcholine ether and hexadecyl trimethyl ammonium bromide, and preferably, the cationic material is hexadecyl trimethyl ammonium bromide. The albumin-coated cabazitaxel cationic nano-lipid carrier provided by the invention is uniform in particle size, high in encapsulation efficiency and good in biocompatibility and biodegradability.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a nano-lipid carrier, in particular to an albumin-wrapped cationic nano-lipid carrier of cabazitaxel and a preparation method thereof. Background technique [0002] Cabazitaxel (Cbz) belongs to taxane antineoplastic drugs, which is a semi-synthetic paclitaxel derivative derived from the compound extracted from the needles of taxus. Its mechanism of action is similar to that of other taxane drugs. Tube dimers assemble into microtubules, while preventing the process of depolymerization to stabilize microtubules and inhibit further cell division, thereby inhibiting the mitosis and proliferation of cancer cells. The currently marketed product is cabazitaxel injection. In order to increase the solubility of cabazitaxel and the stability of the preparation, a large amount of surfactants such as polysorbate 80 and dehydrated ethanol are added to the injection prescript...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/337A61K47/42A61K47/14A61K47/24A61K47/10A61P35/00
CPCA61K9/5169A61K9/5123A61K9/5146A61K9/5192A61K31/337A61P35/00
Inventor 李楠张金霞邓盛齐陈宇婷郑林
Owner CHENGDU UNIV
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