Hydrophilic drug and hydrophobic drug co-loaded target composite nano-drug preparation and preparation method thereof

A nano-drug, hydrophobic drug technology, applied in the direction of drug combination, pharmaceutical formula, non-active ingredient medical preparations, etc., to achieve good therapeutic effect, delay drug resistance, reduce toxicity effect

Inactive Publication Date: 2012-04-04
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Some clinical studies regard the combination of doxorubicin and paclitaxel as the first choice for breast cancer chemotherapy, but there are uncertain factors such as determining the dosage of the d

Method used

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  • Hydrophilic drug and hydrophobic drug co-loaded target composite nano-drug preparation and preparation method thereof
  • Hydrophilic drug and hydrophobic drug co-loaded target composite nano-drug preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0030] 1) Add 150 ml concentrated sulfuric acid and concentrated nitric acid to 50 mgMWCNTs (H2 SO 4 :HNO 3 =3:1) in the mixture was oxidized at 100 °C for 4 h to obtain truncated CNTs, which were centrifuged at 6000 rpm, precipitated in an ultrasonic tank and washed with acetone for 5 times to remove impurities, and then vacuum-dried at 40 °C for 16 h, The obtained black powdery substance is truncated multi-walled carbon nanotubes (CNTs). The as-prepared CNTs have a highly hydrophilic surface and are soluble in aqueous solution because strong acid oxidation not only truncates CNTs but also changes the chemical properties of their surface, i.e., their surface is highly carboxylated. Dissolve 50 mg of CNTs in 50 ml of deionized water, add 3 equivalents of 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride (EDC) to activate at room temperature for 2 h, and then Add 3 equivalents of N-hydroxysuccinimide (NHS) and a certain amount of polyethylene glycol (H 2 N-PEG-NH 2...

Embodiment 2

[0036] Example 2 In vitro experiments on breast cancer cells,

[0037] Using HER-2-positive breast cancer cells SKBR-3, SKBR-3 cells were combined with doxorubicin (ADM)) HER-2-specific monoclonal antibody Fab fragment targeting carbon nanotube drug PEG-CNTs- AntiHER2 Fab-ADM , paclitaxel (Taxol) HER-2 specific monoclonal antibody Fab fragment targeting carbon nanotube drug PEG-CNTs- AntiHER2 Fab -Taxol and HER-2 targeting carbon nanotube loaded hydrophilic drug doxorubicin and hydrophobic The drug preparation of two anticancer drugs paclitaxel (PEG-CNTs-AntiHER2 Fab-ADM-Taxol) was co-cultured for 48h, and the cell viability was detected by MTT. ADM and Taxol single drug group ( p <0.05, n=6).

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Abstract

The invention belongs to the fields of biomedical medical polymer materials, nano-biotechnology and pharmaceutics, and relates to a target carbon nano-tube drug carrier and a preparation method thereof, specifically to a hydrophilic drug and hydrophobic drug co-loaded target composite nano-drug preparation and a preparation method thereof. According to the present invention, high-purity carbon nano-tube is adopted as a carrier, wherein the carbon nano-tube is subjected to pegylation; the carbon nano-tube is conjugated with a Fab fragment of HER-2 specific monoclonal antibody, wherein the Fab fragment of the HER-2 specific monoclonal antibody is adopted as the target molecule; two anticancer agents of hydrophilic adriamycin and hydrophobic paclitaxel are loaded on the target carbon nano-tube drug carrier; with the targeting guidance effect of the Fab fragment of the HER-2 specific monoclonal antibody, the enrichment of the two anticancer agents with two different action mechanisms in breast carcinoma tissues with HER-2 positive expression can be achieved, the complementary tumor cell killing ability is provided, the therapeutic effect is increased, the use amount of the drug and the toxic and side-effects are reduced, and the generation of the drug resistance can be delayed.

Description

technical field [0001] The invention belongs to the fields of biomedical polymer materials, nanobiotechnology and pharmacy, and relates to a targeted carbon nanotube drug carrier and a preparation method thereof, in particular to a targeted composite nanomedicine preparation and its preparation simultaneously carrying hydrophilic and hydrophobic drugs The method particularly relates to a composite nanometer anticancer drug preparation in which hydrophobic and hydrophilic anticancer drugs are jointly loaded on a specific monoclonal antibody Fab fragment targeting carbon nanotube carrier and a preparation method thereof. Background technique [0002] Malignant tumor is one of the diseases that people cannot effectively control at present, and it seriously endangers human health. Chemotherapy is one of the indispensable and important methods in the treatment of malignant tumors. Due to the lack of targeting of the traditional dosage forms of chemotherapy drugs currently used cl...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/34A61K47/04A61K47/42A61K47/48A61K31/704A61P35/00A61K31/337
Inventor 周平汪长春钟玲玲唐越超于建刚
Owner FUDAN UNIV
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