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A multifunctional nanometer drug carrier, a taxol type lipid nanoparticle and a preparing method of the nanoparticle

A nano-drug carrier and lipid nanoparticle technology, which is applied in the field of medical technology pharmaceutical preparations, can solve the problems of toxicity, lack of research on AP self-assembly to form micelles or lipid nanoparticles, etc., to improve solubility and increase X hydrophilicity Sexuality and stability, and the effect of reducing adverse reactions

Inactive Publication Date: 2017-11-10
石三军
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The hydrophilic structure of vitamin C and the lipophilic structure of palmitic acid in AP constitute a special amphiphilic structure, which has the potential to self-assemble into lipid nanoparticles, but the current literature reports about AP micelles or lipids The preparation of nanoparticles is formed after appropriate transformation or modification on the basis of the structure of AP. There is a lack of research on the self-assembly of AP to form micelles or lipid nanoparticles, and the modified AP nanoparticles or micelles Will introduce toxic, non-degradable excipients or excipients degrade to produce toxic substances

Method used

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  • A multifunctional nanometer drug carrier, a taxol type lipid nanoparticle and a preparing method of the nanoparticle
  • A multifunctional nanometer drug carrier, a taxol type lipid nanoparticle and a preparing method of the nanoparticle
  • A multifunctional nanometer drug carrier, a taxol type lipid nanoparticle and a preparing method of the nanoparticle

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Experimental program
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Effect test

Embodiment 1

[0042]Preparation of APNPs: Weigh 5mg of AP and place in a 1.5ml centrifuge tube, add 0.2ml of absolute ethanol solution, fully dissolve to obtain a drug-containing organic phase (25mg / ml); take 5ml of purified water and place in a glass vial, Preheat to 40°C as the water phase; inject the organic phase into the water phase, and immediately use a cell ultrasonic breaker to perform ultrasonic crushing with an ultrasonic power of 50W, supersonic for 5s and stop for 5s, and ultrasonic for 10 minutes in total, then transfer the solution in the vial to In a 100ml round-bottomed flask, the organic solvent was removed by rotary evaporation in a 40°C water bath, protected from light, under reduced pressure, and the APNPs solution was obtained. The appearance of the solution is milky white, transparent and full of opalescence, and the laser irradiation has Tyndall phenomenon. The average particle diameter is 280nm, and the average zeta potential is -48.3mV.

Embodiment 2

[0044] Preparation of APNPs: Weigh 10mg of AP and put it in a 5ml centrifuge tube, add 1ml of absolute ethanol solution, fully dissolve to obtain a drug-containing organic phase (10mg / ml); take 5ml of purified water and put it in a glass vial, preheat to 40°C as the water phase; inject the organic phase into the water phase, and immediately use a cell ultrasonic breaker for ultrasonic crushing, with an ultrasonic power of 50W, supersonic for 5s and stop for 5s, ultrasonic for 10min in total, and then transfer the solution in the vial to a 100ml circle In a bottom flask, the organic solvent was removed by rotary evaporation under reduced pressure in a water bath at 40°C in the dark, and the APNPs solution was obtained. The appearance of the solution is milky white, transparent and full of opalescence, and the laser irradiation has Tyndall phenomenon. The average particle size is 312nm, and the average zeta potential is -45mV.

Embodiment 3

[0046] Preparation of APNPs: Weigh 50mg of AP and put it in a 5ml centrifuge tube, add 2ml of absolute ethanol solution, fully dissolve to obtain a drug-containing organic phase (25mg / ml); take 100ml of purified water and put it in a glass vial, preheat to 40°C as the water phase; inject the organic phase into the water phase, and immediately use a cell ultrasonic breaker to perform ultrasonic crushing, with an ultrasonic power of 50W, supersonic for 5s and stop for 5s, ultrasonic for 20min, and then transfer the solution in the vial to a 250ml circle In a bottom flask, the organic solvent was removed by rotary evaporation under reduced pressure in a water bath at 40°C in the dark, and the APNPs solution was obtained. The appearance of the solution is milky white, transparent and full of opalescence, and the laser irradiation has Tyndall phenomenon. The average particle diameter is 303nm, and the average zeta potential is -46.5mV.

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Abstract

The invention provides preparation of a novel ascorbyl palmitate (AP) based multifunctional nanometer drug carrier (APNPs) and a taxol type lipid nanoparticle (X-APNPs) and applications of the carrier and the nanoparticle in the antitumor field. In a preparing process of the APNPs, no auxiliary material is introduced, and the AP is self-assemblied to form the stable lipid nanoparticle by utilizing the amphiphilic structure of the AP and through a physical means. The prepared novel multifunctional APNPs can increase solubility and stability of an insoluble taxol type medicine, increases bioavailability of the medicine, and can be adopted as an antioxidant and a chemotherapeutic drug to prevent oxidation of the medicine and to prevent and treat tumor. The prepared X-APNPs nanoparticle reduces side and toxic effects of the taxol type medicine, and increases solubility and bioavailability of the taxol type medicine. The taxol type medicine X and the AP have synergistic antitumor curative effects.

Description

technical field [0001] The invention relates to a multifunctional nano-medicine carrier, paclitaxel-like lipid nano-particles and a preparation method thereof, which belong to the field of medical technical pharmaceutical preparations. Background technique [0002] Paclitaxel (PTX) is a tetracyclic diterpenoid compound extracted from the bark of the natural plant Taxus genus, which belongs to complex secondary metabolites, and is the only one known to promote microtubule polymerization and drugs that stabilize polymerized microtubules. Isotope tracing showed that paclitaxel only bound to polymerized microtubules and did not react with unpolymerized tubulin dimers. PTX has now become one of the most commonly used anticancer drugs in clinical practice. It has a remarkable therapeutic effect on breast cancer and ovarian cancer. It mainly binds to tubulin, gathers a large amount of tubulin, affects the disintegration of the spindle in mitosis, and blocks tumor cells. mitosis t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K31/337A61K47/22A61K31/375A61P35/00
CPCA61K31/337A61K9/5123A61K31/375A61K2300/00
Inventor 石三军明月姚秋娥陈剑鸿
Owner 石三军
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