Paclitaxel loaded liposome bacterium inhalation preparation for treating lung cancer

An inhalation preparation and paclitaxel lipid technology, which is applied in the field of medicine, can solve the problems of poor long-term efficacy, difficult local control, and drug systemic distribution in patients with middle and advanced stages, and achieve the effects of improving utilization, reducing drug degradation, and improving targeting.

Active Publication Date: 2019-12-13
ACADEMY OF MILITARY MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Clinically, surgery, chemotherapy and radiotherapy are the main methods for the treatment of non-small cell lung cancer, but the long-term curative effect of the middle and advanced patients is still poor, and the main causes of death are difficulty in local control and distant metastasis
In recent years, traditional chemotherapy is mainly administered orally or intravenously, and the drug will be distributed throughout the body, resulting in a small amount of effective drug reaching the lung cancer site, and the drug reaching the normal tissue is likely to cause toxic and side effects. These serious side effects and low Treatment rates cause great suffering for lung cancer patients

Method used

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  • Paclitaxel loaded liposome bacterium inhalation preparation for treating lung cancer
  • Paclitaxel loaded liposome bacterium inhalation preparation for treating lung cancer
  • Paclitaxel loaded liposome bacterium inhalation preparation for treating lung cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1. Paclitaxel liposome and its lyophilized solid

[0044] Prepare paclitaxel liposomes by film dispersion method: weigh 0.553g of soybean lecithin and 0.05g of cholesterol in a beaker, add 5mL of ethanol for ultrasonic dissolution, accurately weigh 0.04g of paclitaxel and add to the above-mentioned ethanol solution to dissolve, transfer to a rotary evaporator, After rotary evaporation at 50° C. to obtain a uniform film, add 20 mL of water, continue to rotate and disperse evenly under water bath conditions, and obtain paclitaxel liposomes.

[0045] Add 1.2g of mannitol to the above 20mL paclitaxel liposome, dissolve, and freeze-dry in a freeze dryer to obtain a loose solid, pass through a 180 mesh sieve to obtain a white powder, which is used as a paclitaxel liposome solid.

[0046] Get an appropriate amount of paclitaxel liposome solid and disperse it in the phosphate buffered saline solution of pH7.0, obtain the liquid of light blue opalescence ( figure 1 )...

Embodiment 2

[0047] Example 2. Paclitaxel-loaded liposome bacterial inhalation preparation

[0048] Thaw competent Escherichia coli on ice, add the paclitaxel liposome solid in Example 1, and incubate on ice for about 5 minutes to fully dissolve and disperse; set the parameters of the electroporator, including r=550V, d= 60ms, s=50 pieces, i=100ms; electroporation operation was performed on the above liquid for a total of 20 times, and paclitaxel-loaded liposome bacterial inhalation preparation was prepared.

[0049] Escherichia coli in the above preparation process is replaced by Lactobacillus casei, and the paclitaxel-loaded liposome bacterial inhalation preparation is also obtained.

experiment example 1

[0050] Experimental Example 1. Properties of Paclitaxel Liposome Bacterial Inhalation Preparation

[0051] Sample: Paclitaxel liposome prepared in Example 1; Paclitaxel-loaded liposome bacterial inhalation preparation prepared in Example 2; Escherichia coli (E.coli); Lactobacillus casei (L.casei).

[0052] Under the transmission electron microscope, the bacterial wall after electroporation has obvious pores ( Figure 4 ), which can facilitate the entry of drugs into the bacteria.

[0053] The high-performance liquid phase detection shows that the drug encapsulation efficiency of the liposome bacteria loaded with paclitaxel after electroporation is higher than 95%.

[0054] In the in vitro environment, paclitaxel liposomes had no significant effect on the survival of bacteria, and at low to high concentrations (0.635-5mmol / L paclitaxel), the number of colonies had no significant difference compared with the blank control group, that is to say, paclitaxel Liposomes have no ant...

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Abstract

The invention discloses a paclitaxel loaded liposome bacterium inhalation preparation, and the inventor finds that the paclitaxel loaded liposome bacterium inhalation preparation has special effects on treating lung cancer. According to the preparation, firstly paclitaxel liposomes are prepared, then through an electroporation technique, bacteria such as escherichia coli or lactobacillus casei areintroduced, medicine administration is directly performed on the lungs, the bacteria loaded with medicines directly target and act on lung tumor, and the effects of being efficient and safe are achieved.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a paclitaxel-loaded liposome bacterial inhalation preparation for treating lung cancer. Background technique [0002] Paclitaxel (PTX) is a complex compound extracted from the bark of Yew brevifolia, with a molecular weight of 853. Chloroform, etc.; hardly soluble in water, insoluble in petroleum ether. [0003] Paclitaxel is an anti-microtubule drug, which inhibits cell division and proliferation by inhibiting cells from forming spindles and filaments during mitosis, making cells stagnate in G2 and M phases, and exerting anti-tumor effects. PTX has been widely used clinically. In addition to advanced ovarian cancer, lung cancer, and uterine cancer, paclitaxel is also widely used in the clinical chemotherapy of blood diseases and various solid tumors. Clinically, paclitaxel is mostly used in the treatment of small cell lung cancer after relapse, but it is expensive, absorbed into the bl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K47/46A61K35/74A61K31/337A61P35/00
CPCA61K9/007A61K31/337A61K35/74A61K47/46A61P35/00A61K2300/00Y02A50/30
Inventor 金义光张萌萌杜丽娜
Owner ACADEMY OF MILITARY MEDICAL SCI
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