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Tiancimycin lipidosome as well as preparation method and application of Tiancimycin lipidosome

A technology of tiancimycin lipid and tiancimycin, which is applied in the application field of liposome and liposome anti-tumor in vivo, can solve the problems of multi-drug resistance, achieve significant targeting, improve poor solubility, The effect of simple preparation method

Active Publication Date: 2020-08-21
HAYAO CIHANG PHARM CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no research on nano-nano drug delivery of Tiancimycin. The use of nanotechnology to deliver Tiancimycin drug provides a new way to develop new anti-tumor drugs and solve the problem of multi-drug resistance in tumors.

Method used

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  • Tiancimycin lipidosome as well as preparation method and application of Tiancimycin lipidosome
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  • Tiancimycin lipidosome as well as preparation method and application of Tiancimycin lipidosome

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Preparation of Tiancimycin Liposome

[0052] Weigh 30 mg of soybean lecithin, 14 mg of hydrogenated soybean lecithin, 15 mg of cholesterol, 10 mg of DSPE-PEG2000, 400 μL of TNMA (methanol mother liquor 1 mg / mL) and dissolve in 5 mL of dichloromethane, place in a rotary evaporating flask, and decompress Uniform film formation by rotary evaporation. Take another 5 mL of PBS aqueous solution, put it in the round-bottomed flask where the film has been formed, rotate to hydrate the film, disperse it ultrasonically in an ice-water bath for 15 min, and centrifuge it in an ultrafiltration centrifuge tube (MW 3500) (4000 rpm) for 15 min. An opalescent liposome solution was obtained. The particle size of the liposome liposome was measured to be 93 nm, and the Zeta potential was -4.5 mV.

Embodiment 2

[0054] Preparation of liposomes targeting Tiancimycin

[0055] Weigh and weigh 30 mg of soybean lecithin, 14 mg of hydrogenated soybean lecithin, 15 mg of cholesterol, 10 mg of DSPE-PEG2000, 6 mg of DSPE-PEG-cRGD, 400 μL of TNM A (methanol mother solution 1 mg / mL) and dissolve in 5 mL of dichloromethane placed in a rotary evaporating flask, and evaporating under reduced pressure to form a uniform film. Take another 5 mL of PBS aqueous solution, put it in the round-bottomed flask where the film has been formed, spin to hydrate the film, disperse it ultrasonically in an ice-water bath for 15 min, and centrifuge it in an ultrafiltration centrifuge tube (MW 3500) (4000 rpm) for 15 min to obtain Opalescent liposome solution. The particle size of liposomes targeted to Tiancimycin was measured to be 99 nm, and the Zeta potential was -5.1 mV.

Embodiment 3

[0057] In Vitro Release Test of Tiancimycin Liposome

[0058] Experimental method: cut small pieces of dialysis bags (MW 3500), boil them in boiling water for 10 minutes, take them out and soak them in pure aqueous solution, take 1.0 ml each of the orthomycin solution and the orthomycin liposome solution, and put them into the pretreated The two ends of the dialysis bag were tied tightly, and the dialysis bag was placed in 20 mL of PBS buffer solution (0.5% SDS) and shaken in a 37°C constant temperature shaker at 200 r / min. Take 1ml of each sample at the designated time points, and detect the content of orthomycin by HPLC. Add 1 ml to the dialysate after each sampling. The results of in vitro release experiments were as follows: figure 1 As shown, the results showed that: the cumulative release of free tiaciline reached 99% in the first 60 h, and the release of tibialcin liposomes (Lip-TNM A) under physiological conditions (pH 7.4, 37°C, 0.5% SDS) No burst release was shown...

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Abstract

The invention discloses Tiancimycin lipidosome as well as a preparation method and application of the Tiancimycin lipidosome. The invention relates to Tiancimycin for drug delivery in a liposome and cRGD peptide modified targeting liposome manner, and preparation and application thereof. The defect of poor water solubility of Tiancimycin can be overcome; the in-vivo anti-tumor effect of Tiancimycin and the effect on treating malignant tumors are improved, and meanwhile, the cRGD peptide modified targeting liposome is good in targeting property and remarkable in anti-tumor effect. The inventionhas the advantages of simple preparation and low economic cost, a new way for promoting the application of benzoanthraquinone enediyne Tiancimycin and the like in clinic is provided, a variety of solutions for solving the problem of tumor drug resistance in clinic are also provided, and wide application to the fields of new drug development and pharmacy can be realized.

Description

technical field [0001] The invention relates to liposomes, in particular to liposomes containing orthomycin and a preparation method thereof. The invention also relates to the application of liposomes containing orthomycin in anti-tumor in vivo, which belongs to the field of biomedicine. Background technique [0002] Cancer is the deadliest human disease in the world, with more than 15 million new cancer cases worldwide every year. Chemotherapy is the main cancer treatment method besides surgery, radiotherapy, immunotherapy and so on. Although these therapeutic agents have shown relatively satisfactory results, they also suffer from a number of disadvantages, including poor pharmacokinetics, nonspecific biodistribution, and low targeting ability. Poor solubility and specificity are considered to be major obstacles for the application of therapeutic drugs in cancer treatment. Therefore, there is an urgent need to overcome these shortcomings in order to improve the efficienc...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/4748A61K47/24A61K47/28A61K47/18A61P35/00
CPCA61K9/127A61K9/0019A61K31/4748A61K47/24A61K47/28A61K47/18A61P35/00
Inventor 段燕文黄勇冯雪琼
Owner HAYAO CIHANG PHARM CO LTD
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