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Targeted nanometer microbubble for treating small cell lung cancer as well as preparation method and application thereof

A kind of small cell lung cancer, nano technology, applied in the direction of non-active ingredients of medical preparations, pharmaceutical formulations, anti-tumor drugs, etc., to achieve the effect of reducing toxic and side effects

Inactive Publication Date: 2018-02-06
SHANXI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

(Yan F, Li X, JinQ, et al. Therapeutic ultrasonic microbubbles carrying paclitaxel and LyP-1peptide: preparation, characterization and application to ultrasound-assisted chemotherapy in breast cancer cells, Ultrasound Med Biol, 2011, 37, 768-779.) But SCLC target The research on the drug delivery system has not been reported at home and abroad

Method used

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  • Targeted nanometer microbubble for treating small cell lung cancer as well as preparation method and application thereof
  • Targeted nanometer microbubble for treating small cell lung cancer as well as preparation method and application thereof
  • Targeted nanometer microbubble for treating small cell lung cancer as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0028] Example 1 Preparation of paclitaxel-loaded liposomes: dipalmitolecithin (DPPC) 18mg, distearoylphosphatidylethanolamine (DSPE) 1mg, dipalmitophosphatidic acid (DPPA) 1mg and paclitaxel (PTX) were prepared by film hydration method 1mg was completely dissolved in 4ml of chloroform. Chloroform forms a phospholipid film after evaporation in a fume hood. After film formation, 4 mL of hydration solution (glycerol:PBS=1:9 (volume ratio)) was added and shaken on a shaker at room temperature for 60 min. The hydration solution was evenly mixed with the washed phospholipid membrane, and the mixture was transferred to a 50mL centrifuge tube to form paclitaxel-loaded liposomes.

Embodiment 2

[0029] Example 2 Preparation of paclitaxel-loaded targeting nano-microbubbles: take 10 μg of anti-progastrin-releasing peptide monoclonal antibody diluted to 50 μL with PBS, add 10 μL of EDTA solution (0.5M); ) was dissolved in 500μL PBS, mixed the above antibody and PBS solution, incubated at 37°C for 90min, ultrafiltered 3 times with PBS solution containing 10μL EDTA (0.5M) per 500μL (about 5mL, 3000rpm, 8min, 4°C), and opened Antibody (scAb), incubate the opened antibody with paclitaxel-loaded liposomes prepared above, and then pass into C 3 f 8 Gas, paclitaxel-loaded nano-microbubbles for the targeted therapy of SCLC were obtained by mechanical vibration. Under the transmission electron microscope, they are all spherical in shape, round in shape, evenly distributed, without aggregation, and the particle size is 300-500nm (such as figure 1 shown). The Zeta potential and particle size analyzer measures the particle size of paclitaxel-loaded targeted nano-microbubbles, the...

Embodiment 3

[0030] Example 3 Determination of encapsulation efficiency and drug loading of paclitaxel-loaded targeting nano-microbubbles: Dissolve paclitaxel-loaded targeting nano-microbubbles in 0.1 mL of cyanide, and then add 0.8 mL of phosphate buffer at pH 6.0, fully After mixing for 2 hours, the supernatant was collected by centrifugation (10000rmp, 60min), and analyzed using a high-performance liquid chromatograph with UV analysis. The encapsulation efficiency of paclitaxel-loaded targeting nano-microbubbles was measured to be (70.72±5.38)% , the drug loading was (3.29±0.17)%. Nano-microbubbles have a higher encapsulation efficiency of paclitaxel and a better drug loading capacity.

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Abstract

The invention provides a targeted nano-microbubble for treating small cell lung cancer, a preparation method and application thereof. Targeted nano-microbubbles include a lipid bimolecular shell and an inert gas wrapped inside the lipid bimolecular shell, and the anti-progastrin releasing peptide monoclonal antibody of small cell lung cancer and paclitaxel are connected to the lipid bimolecular shell, The average particle size of nano-microbubbles is 300-500nm. Preparation method: dipalmitolecithin, distearoylphosphatidylethanolamine, dipalmitophosphatidic acid and paclitaxel were completely dissolved in chloroform by film hydration method to prepare paclitaxel-containing liposomes, which are aimed at anti-progastrocytosis of small cell lung cancer The hormone-releasing peptide monoclonal antibody was opened with mercaptoethylamine, incubated with the liposome above to form a stable thioether bond, and then perfluoropropane gas was passed through, and the anti-monogastric antibody targeting small cell lung cancer was obtained by mechanical vibration. Secretin-releasing peptide monoclonal antibody targeting paclitaxel nanomicrobubbles. The targeted nanometer microbubble can be used in the preparation of medicines for treating small cell lung cancer.

Description

technical field [0001] The invention relates to a targeted nano-medicine, in particular to a targeted nano-microbubble for treating small cell lung cancer, a preparation method and application thereof. Background technique [0002] Small cell lung cancer (SCLC) is a type of lung cancer with the lowest differentiation, the highest degree of malignancy, the earliest distant metastasis, and the worst prognosis. At present, there are few effective treatment strategies for SCLC, mainly chemotherapy and radiotherapy, and the two-year survival rate of patients is extremely low. So far, there is no particularly effective treatment plan for SCLC. Effective chemotherapy drugs are urgently needed to improve the treatment status of SCLC, and highly targeted anticancer drugs have become a research hotspot in the field of SCLC treatment. (Satankova M, Brat K, Tomiskova M, et al.Effect of Erlotinib in 2nd and 3rdLine Anticancer Treatment in Patients with Squamous Cell Lung Cancer-CaseSeri...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/68A61K31/337A61P35/00
CPCA61K31/337A61K9/0019
Inventor 王伟王金萍许静梁爱华
Owner SHANXI UNIV
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