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Herceptin modified paclitaxel-carried targeting nanoparticle transfer system

A trastuzumab, targeting nanoparticle technology, applied in the directions of antineoplastic drugs, inactive components of polymer compounds, powder delivery, etc., can solve the problems of single nanoparticle carrier material, etc. Good stability and improved ingestion efficiency

Inactive Publication Date: 2015-08-05
JILIN UNIV
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Problems solved by technology

[0005] The present invention provides a paclitaxel-loaded targeting nanoparticle delivery system modified by trastuzumab, which is a paclitaxel-loaded targeting nanoparticle delivery system modified by trastuzumab specifically targeting HER2 overexpression tumor cells, It solves the defects of the current paclitaxel preparation and the single defect of the nanoparticle carrier material

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  • Herceptin modified paclitaxel-carried targeting nanoparticle transfer system
  • Herceptin modified paclitaxel-carried targeting nanoparticle transfer system
  • Herceptin modified paclitaxel-carried targeting nanoparticle transfer system

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Embodiment Construction

[0034] specific implementation plan

[0035] The present invention is described in detail below in conjunction with specific embodiment, but protection scope of the present invention is not limited thereto:

[0036] Example 1 ：

[0037] 1. Weigh 10 mg of paclitaxel and 60 mg of PLGA 1A and dissolve in 2.4 mL of acetone, weigh 20 mg of DPPC and 10 mg of DSPE-PEG2000-Mal and dissolve in 1.6 mL of ethanol. Mix the acetone-ethanol solution to form a binary organic phase (O phase), add 15 mL of 1.0–2.0% poloxamer 188 aqueous solution (W phase), and disperse at 0–4°C with intermittent ultrasound (100 W, 150 s) to prepare O / W emulsion, add 15 mL of 1.0-2.0% poloxamer 188 aqueous solution, stir at low speed at room temperature (150 rpm), evaporate overnight to remove binary organic phase, filter with 0.22 μm microporous membrane, and centrifuge to collect nanoparticles (18000 rpm, 15 min), freeze-dried;

[0038]2. Take 20 μL, 6 mg / mL Traut's Reagent, add 1 mL, 1 mg / mL Trastuzu...

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Abstract

The invention discloses a herceptin modified paclitaxel-carried targeting nanoparticle transfer system and a preparation method thereof. Nanoparticles (PLNs) with PLGA / Lipid core-shell structures are prepared by an improved classical emulsion solvent evaporation method, paclitaxel-carried polymer lipid nanoparticles are prepared by a binary organic solvent method, and herceptin modified paclitaxel-carried targeting nanoparticles (T=PCNs) are built by a chemical modification method. The prepared T=PCNs release drugs in vitro, sudden release rate within 24h is 41.2%, cumulative release rate within 120h is 73.4%, and cancer therapy is facilitated by drug release level. Cell experiment results indicate that the T=PCNs are fine in targeting property for highly expressed HER2 cancer cells and have an obvious killing function for the cancer cells. Safety and the targeting property of paclitaxel are greatly improved.

Description

technical field [0001] The invention discloses a targeting nanoparticle delivery system loaded with paclitaxel modified by trastuzumab, and provides a preparation method of the system, belonging to the technical field of tumor targeting and sustained release drug delivery systems. Background technique [0002] Paclitaxel is an anti-tumor drug widely used clinically. It can induce and promote tubulin polymerization, prevent depolymerization, stabilize tubulin, inhibit mitosis, and exert anti-tumor effects. Paclitaxel has high efficiency, low toxicity and broad-spectrum anticancer activity, especially has a unique curative effect on breast and ovarian cancer. Its injection is the first-line drug for the treatment of solid tumors such as breast cancer, ovarian cancer and lung cancer. However, due to the poor water solubility of paclitaxel, it is difficult to make injection preparations. Paclitaxel injection (Taxol), which is commonly used in clinical practice, uses polyoxyethy...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/337A61K47/42A61K47/34A61P35/00
Inventor 李又欣于崆峒周毓麟张尊凯滕乐生
Owner JILIN UNIV
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