Docetaxel pH-sensitive liposome and preparation method thereof

A technology of docetaxel and liposome, applied in the field of pH-sensitive liposome and its preparation, can solve problems such as large toxic and side effects, and achieve the effects of low toxic and side effects, high drug therapeutic index and good storage stability

Inactive Publication Date: 2012-03-21
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, after the drug is injected intravenously, the side effects are relatively large, and the common ones are bone marrow suppression, edema, hair loss, weakness, mucositis, arthralgia, muscle pain, hypotension, and injection site reactions, etc.
These toxic and side effects have greatly restricted the clinical application of docetaxel. Therefore, a more effective new dosage form of the drug is sought, so that the drug can prolong the half-life and circulation time of the drug in the body without increasing the dose, and improve the quality of the drug. It is imminent to improve the anti-tumor effect of drugs, reduce the toxic and side effects of drugs, and enhance the clinical applicability of drugs

Method used

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  • Docetaxel pH-sensitive liposome and preparation method thereof
  • Docetaxel pH-sensitive liposome and preparation method thereof
  • Docetaxel pH-sensitive liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Weigh 30 mg of phosphatidylethanolamine, 20 mg of cholesterol, and 30 mg of oleic acid, dissolve them in 15 ml of organic solvent chloroform, and evaporate the mixed solution to dryness under pressure until a uniform lipid film is formed. Add 2ml of docetaxel drug solution (drug concentration: 5mg / ml) with pH=7.4 to dissolve, sonicate to form a uniform suspension, supplement with PBS buffer with pH7.4 to make the final volume 20ml, and hydrate in a water bath at 37°C After 30 minutes, the docetaxel pH-sensitive liposome was ready. The prepared docetaxel pH-sensitive liposome particle size is 277 ± 2nm~303 ± 1nm, and the average particle size is 286.4nm. figure 1 As shown, the particle size distribution is as figure 2 shown.

Embodiment 2

[0021] Docetaxel pH-sensitive liposomes were prepared according to Example 1 above. Utilize the dynamic membrane dialysis method, investigate the release law of preparation in different pHPBS, the obtained release curve is as follows: image 3 As shown, it can be seen that the release rate of the liposome-encapsulated drug is different in different pH environments, and the release rate of the drug is faster in an acidic environment.

Embodiment 3

[0023] Using the docetaxel pH-sensitive liposomes prepared in the above-mentioned Example 1 and the control solution formulated with the docetaxel bulk drug, dynamic membrane dialysis was used to investigate their release in the same pH buffer solution. Law as Figure 4 As shown, it can be seen that preparing the drug into liposomes can delay the release of the drug and improve its bioavailability.

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Abstract

The present invention discloses a docetaxel pH-sensitive liposome which is composed of the following raw materials: docetaxel, phosphatidylethanolamine, cholesterol and oleic acid. The particle size of the pH-sensitive liposome is 277+ / -2nm-303+ / -1nm. A preparation method of the docetaxel pH-sensitive liposome comprises the following steps: weighing 30mg of phosphatidylethanolamine, 20mg of cholesterol and 30mg of oleic acid, dissolving in 15ml of organic solvent, performing pressurizing and evaporating for the mixed solution until a layer of uniform lipid film is formed; then adding 2ml of docetaxel solution, after dissolving, performing ultrasonic treatment for forming uniform suspension, performing hydration at a 37 DEG C water bath state for 30 min, and obtaining the docetaxel pH-sensitive liposome. The preparation method of the docetaxel pH-sensitive liposome has the following advantages: simple preparation process, higher envelope rate and stable performance of the prepared liposome medicine. The prepared docetaxel pH-sensitive liposome has the following remarkable characteristics: passive targeting performance, intelligent controlled release, etc. Furthermore the docetaxel pH-sensitive liposome has the following advantages: high storage stability, high therapeutic index, low toxic and side effect, and capability of being used for treating various neoplastic diseases, etc.

Description

technical field [0001] The invention relates to a pH-sensitive liposome of antitumor drug docetaxel and a preparation method thereof. Background technique [0002] Docetaxel belongs to taxane compound antineoplastic drugs, its mechanism of action is to strengthen the polymerization of tubulin and inhibit the depolymerization of microtubules, resulting in the formation of stable non-functional microtubule bundles, thus destroying the tumor cells. Mitosis prevents tumor cells from proliferating and inhibits tumor cell growth, thus playing an anti-tumor role. Clinically, it is mainly used for the treatment of advanced or metastatic breast cancer that failed prior chemotherapy and the treatment of advanced or metastatic non-small cell lung cancer that failed cisplatin-based chemotherapy. However, after intravenous injection of the drug, the side effects are relatively large, and the common ones are bone marrow suppression, edema, hair loss, weakness, mucositis, arthralgia, musc...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/337A61K47/28A61P35/00
Inventor 林贵梅牟珍珍路侠李瑞莹张芳卢杉杉
Owner SHANDONG UNIV
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