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Paclitaxel nanoemulsion inhalation preparation for targeted therapy of lung cancer and preparation method of paclitaxel nanoemulsion inhalation preparation

A technology for targeted therapy and inhalation preparations, which is applied in the field of preparation of paclitaxel nano-preparations, can solve problems such as toxic side effects, blood drug concentration approaching or exceeding the poisoning level, etc., achieve simple preparation methods, increase encapsulation efficiency and drug loading, Reduce the effect of the initial burst

Pending Publication Date: 2022-07-15
BEIJING XINLINGXIAN MEDICAL TECH DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The sudden release at the initial stage of administration may cause the blood drug concentration to approach or exceed the toxic level, resulting in obvious toxic side effects

Method used

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  • Paclitaxel nanoemulsion inhalation preparation for targeted therapy of lung cancer and preparation method of paclitaxel nanoemulsion inhalation preparation
  • Paclitaxel nanoemulsion inhalation preparation for targeted therapy of lung cancer and preparation method of paclitaxel nanoemulsion inhalation preparation
  • Paclitaxel nanoemulsion inhalation preparation for targeted therapy of lung cancer and preparation method of paclitaxel nanoemulsion inhalation preparation

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Weigh about 1 mg of paclitaxel and 0.800 g of PLGA and dissolve in 2 mL of dichloromethane as the organic phase; 250 μL of 1.0% poloxamer and 250 μL of water are mixed as the inner aqueous phase. After emulsification, inject the mixed solution (10 mL of 0.5% PVA+0.5 mL of 2% chitosan solution), stir at room temperature to evaporate the organic solvent, stir at low speed at 5000 rpm for 20 min to remove insoluble matter, and wash with water 3 times.

Embodiment 2

[0036] Comparison of encapsulation efficiency of chitosan-modified PLGANA nanoemulsion in poloxamer inner aqueous phase and PLGA nanoemulsion with water as inner aqueous phase.

[0037] Precisely weigh 10 mg of nanoemulsion lyophilized powder, dissolve in PBS, re-disperse by ultrasonic treatment for 100w 3min, and transfer the PLGA nanoemulsion into an ultrafiltration tube. High-speed refrigerated centrifugation at 7000rpm for 30 minutes at 4°C to separate nanoparticles and supernatant. The content of the drug in the ultrafiltrate was determined by high performance liquid chromatography, and then the encapsulation rate and release rate were calculated. The encapsulation rate results are shown in figure 2 , the release rate results see image 3 .

Embodiment 3

[0039] The curative effect of the inhalation injection of the present invention was compared with the mouse model transplanted with mouse-derived Lewis lung cancer cells. The tumor-receiving mice were divided into three groups, and one group was given conventional paclitaxel injection (45 mg / kg) through the tail vein, once every two weeks and twice. One group was administered with a self-made inhalation applicator (10 mg / kg), once every two weeks, twice. The positive control group was not administered by any means. Compared the results, it was found that the survival time of the mice in the intravenous administration group and the inhalation administration group was not much different, about 21-23 days, and the mice in the non-administration group only survived for 11.5 days. The dosage of the inhalation preparation of the present invention is small, and the administration effect of the inhalation preparation is equivalent to that of the injection in a large dosage.

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Abstract

The invention provides a preparation method of a paclitaxel nano preparation, which is characterized in that the plasma half-life period of paclitaxel is prolonged, and the toxicity of paclitaxel is reduced. The paclitaxel nano preparation is composed of paclitaxel, poloxamer, chitosan, a polylactic acid-glycolic acid copolymer, an emulsifier and other pharmaceutic adjuvants. The inner water phase is composed of a poloxamer aqueous solution, after the poloxamer aqueous solution and the paclitaxel-containing PLGA organic phase form primary emulsion, the primary emulsion is injected into a chitosan-containing PVA solution to form multiple emulsion, stirring is performed at the room temperature to volatilize an organic solvent, insoluble substances are removed through centrifugation, and washing and freeze drying are performed to obtain the paclitaxel-containing poloxamer hydrogel. According to the preparation method of the paclitaxel nano preparation, paclitaxel is dissolved in an organic phase containing PLGA, a hydrophobic environment is provided, the stability of paclitaxel is improved, the half-life period of plasma is prolonged, and the dosage of paclitaxel is reduced. The invention provides a targeted drug delivery inhalation preparation for treating lung cancer, which prolongs the half-life period of the drug and reduces the continuous damage of high-dose drugs to human bodies.

Description

technical field [0001] The present invention relates to a preparation method of paclitaxel nano preparation. Background technique [0002] Paclitaxel can debalance tubulin and tubulin dimers that make up microtubules, induce and promote tubulin polymerization, microtubule assembly, and prevent depolymerization, thereby stabilizing microtubules and inhibiting cancer cell mitosis and triggering Cell apoptosis, and then effectively prevent the proliferation of cancer cells, play an anti-cancer effect. Paclitaxel has been reported in the literature as a first-line drug for the treatment of lung cancer, but intravenous infusion is transported through the blood to the lesion site, and it also has a certain damage effect on the non-lesion site. The advantage of pulmonary administration is that the drug can be directly targeted to the airway surface, rather than being absorbed through the gastrointestinal tract and distributed throughout the body, so that only a small fraction of t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K9/107A61K47/34A61K47/36A61K47/10A61K31/337A61P35/00
CPCA61K9/0078A61K9/1075A61K47/34A61K47/36A61K47/10A61K31/337A61P35/00
Inventor 李应锋赵德千
Owner BEIJING XINLINGXIAN MEDICAL TECH DEV CO LTD
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