RLT polypeptide-mediated docetaxel tumor targeting submicroemulsion and preparation method thereof

A technology of docetaxel and submicroemulsion, which is applied in the field of preparation of docetaxel tumor-targeting submicroemulsion, which can solve the problems of low targeting efficiency, unfavorable drug uptake, high toxicity, etc., and achieve quality control , Improve the therapeutic effect, the effect of high drug loading

Inactive Publication Date: 2014-07-16
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the docetaxel submicroemulsion disclosed in the two patents is a passive targeting preparation. After intravenous injection, it is phagocytized by macrophages and enriched in the liver, kidney and spleen. Due to the few macrophage systems distributed in tumors and other tissues, This is not conducive to the uptake of drugs by tumor tissues, the targeting efficiency is low, and the toxicity of drugs to other normal organs is still relatively high

Method used

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  • RLT polypeptide-mediated docetaxel tumor targeting submicroemulsion and preparation method thereof
  • RLT polypeptide-mediated docetaxel tumor targeting submicroemulsion and preparation method thereof
  • RLT polypeptide-mediated docetaxel tumor targeting submicroemulsion and preparation method thereof

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Effect test

Embodiment 1

[0029] 1. Preparation of RLT polypeptide-mediated docetaxel tumor-targeting submicroemulsion raw materials and raw material ratio are shown in Table 1.

[0030] The RLT polypeptide is glutamic acid-lysine-leucine-lysine-glutamic acid-alanine-phenylalanine-arginine-leucine-threonine-arginine -Lysine-Arginine-Glycine-Leucine-Lysine-Leucine-Alanine-Cysteine.

[0031] 2. The method for preparing the RLT polypeptide-mediated docetaxel tumor-targeting submicroemulsion is as follows:

[0032] (1) Preparation of oil phase: at 55°C, mix emulsifier, docetaxel, antioxidant vitamin E, octadecylamine, distearoylphosphatidylethanolamine-polyethylene glycol 2000-maleimide Add vegetable oil for injection into absolute ethanol and dissolve; at 30°C, remove ethanol under reduced pressure, heat to 55°C, stir evenly, and form an oil phase;

[0033] (2) Preparation of water phase: at 55°C, add co-emulsifier, glycerin, etc. into water for injection, and stir evenly to form a water phase;

[0034...

Embodiment 2

[0038] 1. Preparation of RLT polypeptide-mediated docetaxel tumor-targeting submicroemulsion raw materials and raw material ratio are shown in Table 1.

[0039]The RLT polypeptide is glutamic acid-lysine-leucine-lysine-glutamic acid-alanine-phenylalanine-arginine-leucine-threonine-arginine -Lysine-Arginine-Glycine-Leucine-Lysine-Leucine-Alanine-SH.

[0040] 2. The method for preparing the RLT polypeptide-mediated docetaxel tumor-targeting submicroemulsion is as follows:

[0041] (1) Preparation of oil phase: at 60°C, mix emulsifier, docetaxel, antioxidant vitamin E, octadecylamine, distearoylphosphatidylethanolamine-polyethylene glycol 2000-maleimide Add vegetable oil for injection into absolute ethanol and dissolve; at 35°C, remove ethanol under reduced pressure, heat to 60°C, stir evenly, and form an oil phase;

[0042] (2) Preparation of water phase: at 60°C, add co-emulsifier, glycerin, etc. into water for injection, and stir evenly to form a water phase;

[0043] (3) P...

Embodiment 3

[0047] 1. Preparation of RLT polypeptide-mediated docetaxel tumor-targeting submicroemulsion raw materials and raw material ratio are shown in Table 1.

[0048] The RLT polypeptide is cysteine-glutamic acid-lysine-leucine-lysine-glutamic acid-alanine-phenylalanine-arginine-leucine-threonine Acid - Arginine - Lysine - Arginine - Glycine - Leucine - Lysine - Leucine - Alanine.

[0049] 2. The method for preparing the RLT polypeptide-mediated docetaxel tumor-targeting submicroemulsion is as follows:

[0050] (1) Preparation of oil phase: at 65°C, mix emulsifier, docetaxel, antioxidant vitamin E, stearylamine, distearoylphosphatidylethanolamine-polyethylene glycol 2000-maleimide Add vegetable oil for injection into absolute ethanol and dissolve; at 35°C, remove ethanol under reduced pressure, heat to 65°C, stir evenly, and form an oil phase;

[0051] (2) Prepare the water phase: Add co-emulsifier, glycerin, etc. into the water for injection at 65°C, and stir evenly to form the w...

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Abstract

The invention relates to a docetaxel tumor-targeting submicroemulsion mediated by a polypeptide (RLT polypeptide) bound to a low-density lipoprotein binding domain in apolipoprotein B and a preparation method thereof, belonging to the technical field of medicine. The submicron emulsion is prepared with injection oil, emulsifier, co-emulsifier, antioxidant, isotonic regulator, distearoylphosphatidylethanolamine-polyethylene glycol 2000-maleimide, RLT polypeptide and poly Tumor-targeting submicroemulsion prepared by paclitaxel. The weight volume concentration of docetaxel ranges from 0.5 to 20 mg / mL. The particle size of the tumor-targeting submicron emulsion is uniform, with an average particle size of 182nm. Modification of docetaxel submicroemulsion by tumor-targeting molecules significantly improves tumor-targeting efficiency, increases the distribution of drugs in tumor tissues, and reduces the amount of other normal drugs. Therefore, the tumor-targeting submicroemulsion of docetaxel mediated by the RLT polypeptide can improve the therapeutic effect of the drug and reduce the toxic and side effects.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to the preparation of the anticancer drug docetaxel with appropriate pharmaceutical auxiliary materials into an RLT polypeptide-mediated docetaxel tumor-targeting submicroemulsion, and the invention also relates to a preparation method of the preparation. Background technique [0002] Docetaxel is a taxane antineoplastic drug, which mainly interferes with the microtubule network required during cell mitosis and division to achieve antitumor effects. Its adverse reactions are mainly manifested in allergic reactions, thrombocytopenia, and transient cardiac arrest. Tachy, hypotension, neurotoxicity, gastrointestinal tract and skin toxicity, etc. Docetaxel has low water solubility, and the commercially available taxotere is solubilized by Tween-80 and ethanol, which will cause hemolytic reaction and has poor safety. How to reduce its side effects and improve clinical effica...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/337A61K47/42A61P35/00
Inventor 赵永星华海婴阿有梅张雪晓孙倩
Owner ZHENGZHOU UNIV
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