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Targeting cisplatin sodium nano-alginate liposome

A technology of sodium alginate and liposome, which is applied in the field of medicine, can solve the problems of restricting the development of preparations, toxic and side effects of patients, and the decline in quality of life, and achieve excellent anti-tumor activity

Inactive Publication Date: 2014-01-22
RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, cisplatin lacks selectivity and has toxic reactions. It often kills normal cells while killing tumor cells, leading to serious side effects and a serious decline in the quality of life of patients.
At the same time, because cisplatin is a non-fat-soluble drug and slightly soluble in water (Chinese Pharmacopoeia, 2010), the development of its preparations is limited, so the cisplatin liposomes currently reported generally have encapsulation efficiency or drug loading (CN201210037920.1 reported an encapsulation rate of 51% and a drug loading capacity of 4.0%; CN201010530655.1 reported an encapsulation rate of 71.25% and a drug loading capacity of 8.81%)

Method used

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  • Targeting cisplatin sodium nano-alginate liposome
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  • Targeting cisplatin sodium nano-alginate liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1: Preparation of the invented cisplatin prodrug (cisplatin sodium alginate linker)

[0053] Precisely measure 20mg of cisplatin and 20mg of sodium alginate, that is, the mass ratio is 1:1. Then dissolved in 20mL DDW, reacted at a constant temperature of 37°C for 24h, and connected to form SA-CDDP. SA stands for sodium alginate, CDDP stands for cisplatin, and DDW stands for double distilled water.

[0054] Fourier transform infrared spectrometer FTIR analysis: Pure CDDP, SA and graft copolymer SA-CDDP were compressed into tablets by KBr, and were measured by Thermo Nicolet380 Fourier transform infrared spectrometer. figure 1 Compare the infrared spectra of SA (c) and SA-CDDP (b) for the infrared spectra of CDDP, SA, and SA-CDDP, which can be seen from c at 3445.90cm -1 The absorption peak at is the stretching vibration peak of OH group; at 1621.74cm -1 and 1417.86cm -1 There will be two absorption peaks nearby, the former is -COO - The antisymmetric stretch...

Embodiment 2

[0055] Embodiment 2: Preparation of the targeted cisplatin nano-sodium alginate liposome of the invention

[0056] Using the thin film dispersion method, accurately measure 10 mg of EPC, 2 mg of CHOL, and 0.3 mg of amine-PEG2000-DSPE, mix and dissolve them in 3 mL of chloroform, and spin-evaporate at 35°C to form a lipid film, and dry it in vacuum overnight. Then take 2mL of the cisplatin prodrug SA-CDDP and 3mL DDW prepared above and add them to the lipid film, mix and hydrate for 30min, sonicate in a water bath for 3min (50W), and probe intermittently sonicate for 1min (100W) to form cisplatin-loaded nanoparticles. Sodium alginate liposomes. Then add 2 mg of cross-linking agent EDC and NHS respectively, and after magnetic stirring at room temperature for 30 min, take 0.5 mg / mL EGF 100 μL and add it to the above solution, keep stirring for 4-6 h in the dark at room temperature, and then put it into a 10K ultrafiltration tube In the process, centrifuge at 4000rpm for 10min to...

Embodiment 3

[0058] In vitro release experiment of targeted cisplatin nano-sodium alginate liposomes invented in Example 3

[0059] Precisely weigh three parts of cisplatin (CDDP), cisplatin-loaded sodium alginate liposome (CS-PEG-Lip), EGF-modified cisplatin-loaded sodium alginate liposome ((CS-EGF-Lip), 2 mL. Put it in a pre-treated dialysis bag, tie both ends of the dialysis bag tightly, suspend in a stoppered Erlenmeyer flask, add 18 mL of PBS (pH=7.4) or MES (pH=5.5) buffer into the Erlenmeyer flask, Place it in a constant temperature water bath shaker (temperature is 37°C ± 0.5°C, 100rpm continuous shaking). ), 4, 5, 6, 7 (d) sampling, draw 2 mL of the solution outside the dialysis bag each time, and then immediately add 2 mL of PBS or MES buffer solution at a temperature of 37 ° C. The 2 mL of the solution taken out is used for inductively coupled plasma Emission spectrometer ICP-OES measurement. The percentage (%) of cumulative drug release is plotted against time (hours), and the...

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Abstract

The invention relates to a targeting cisplatin sodium nano-alginate liposome. The targeting performance of the targeting cisplatin sodium nano-alginate liposome is embodied by that the liposome is modified by targeting molecules, and the liposome has the grain diameter of about 100nm and is composed of phosphatidylcholine, cholesterol, sodium alginate, an anti-tumor drug cisplatin and targeting molecules. The liposome has a high systematic cisplatin carrying rate (15.24%) and a high encapsulation rate (89.92%), can be subjected to specific combination with targeting molecules on surfaces of tumor cells so as to achieve toxicity attenuation and synergism, and is locally and specifically applied to the preparation of drugs for tumor treatment. Particularly, the liposome has more excellent anti-tumor activity to oophoroma resisting.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to the preparation of targeted cisplatin nano-sodium alginate liposome and its application in the treatment of ovarian cancer tumors. Background technique [0002] Ovarian cancer is the most malignant disease among gynecological tumors, and ranks first in the mortality rate of gynecological malignant tumors, seriously threatening women's reproductive health. The onset of ovarian cancer is occult, and it is very prone to invasion and distant metastasis. About 70% to 80% of ovarian cancer patients are diagnosed as stage III / IV, and their five-year survival rate is only about 30%. The treatment of ovarian cancer is mainly based on complete tumor reduction surgery. However, because the metastases are mostly scattered and widely planted in the abdominal cavity, it is still impossible to completely remove the tumor by surgery. chemotherapy. [0003] The most commonly used is platinum-b...

Claims

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Application Information

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IPC IPC(8): A61K33/24A61K47/48A61K47/42A61K9/107A61P35/00A61P15/08
Inventor 狄文王云飞
Owner RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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