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

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

Inactive Publication Date: 2012-11-21
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 polypeptide (RLT polypeptide)-mediated docetaxel tumor targeting submicroemulsion combined with a low density lipoprotein binding domain in an apolipoprotein B, and a preparation method thereof, which belong to the medical technology field. The submicroemulsion is the tumor targeting submicroemulsion prepared from oil for injection, emulsifying agents, auxiliary emulsifying agents, antioxygen, isoosmotic adjusting agents, bi-stearoyl phosphatidyl ethanolamine-polyethylene glycol 2000-maleimide, RLT polypeptide and docetaxel. The weight volume concentration range of the docetaxel is 0.5-20mg / mL. The tumor targeting submicroemulsion has uniform grain size, and the average grain size is 182nm. The docetaxel submicroemulsion is modified by tumor targeting cells, so that the tumor targeting efficiency is obviously improved, the distribution of medicine in the tumor cells is increased, and other normal medicine dose is reduced. Therefore, due to the RLT polypeptide-mediated docetaxel tumor targeting submicroemulsion, the therapeutic effect of the medicine can be improved, and the toxic and side effects are reduced.

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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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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