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Liquid crystal nanoparticle precursor microparticle, self-assembled liquid crystal nanoparticle and preparation methods thereof

A liquid crystal precursor and nanoparticle technology, which is applied in nanotechnology, nanotechnology, nanomedicine, etc., can solve the problems of liquid crystal nanoparticle drug leakage, unstable dispersion system, and low encapsulation efficiency, achieving good application prospects and improving The effect of complete release degree and high encapsulation rate

Active Publication Date: 2017-02-15
GUANGZHOU NEWORLD PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Based on this, the present invention provides a kind of preparation method of liquid crystal nanoparticle precursor particle, in the process of preparation avoiding the dispersion solution of unstable liquid crystal nanoparticle, the prepared liquid crystal nanoparticle precursor particle is prepared and stored The stability is good during the process, and it can self-assemble to form in-situ liquid crystal nanoparticles after contact with water, which solves the problems of liquid crystal nanoparticles prepared by traditional methods such as drug leakage, low encapsulation efficiency, and unstable dispersion system.

Method used

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  • Liquid crystal nanoparticle precursor microparticle, self-assembled liquid crystal nanoparticle and preparation methods thereof
  • Liquid crystal nanoparticle precursor microparticle, self-assembled liquid crystal nanoparticle and preparation methods thereof
  • Liquid crystal nanoparticle precursor microparticle, self-assembled liquid crystal nanoparticle and preparation methods thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0059] Example 1: Preparation of Liquid Crystal Nanoparticle Precursor Particles Loaded with Hydroxycamptothecin

[0060] (1) Preparation of liquid crystal precursor solution

[0061] Take by weighing three parts of dimethylacetamide (DMAC), every part of 39.0g, add respectively 0.01g, 0.05g, 0.10g insoluble drug hydroxycamptothecin (the mass fraction of medicine in the obtained liquid crystal nanoparticle precursor microparticle respectively 1%, 5% and 10%), three parts of drug solutions are obtained; in every part of drug solutions, 0.4g of PYT and 0.6g of diluent PVPVA64 (that is, PYT in the obtained liquid crystal nanoparticle precursor particles) are added to melt at 50°C. / PVPVA64 ratio is 4 / 6), vortexed and mixed to obtain three liquid crystal precursor solutions with good fluidity.

[0062] (2) Preparation of liquid crystal nanoparticle precursor particles

[0063] The uniform liquid crystal precursor solution is solidified and dispersed into liquid crystal nano part...

Embodiment 2

[0075] Example 2: Preparation of Liquid Crystal Nanoparticle Precursor Particles Loaded with Docetaxel

[0076] (1) Preparation of liquid crystal precursor solution

[0077] Weigh three parts of absolute ethanol, each part is 24.0g, add 0.04g insoluble drug docetaxel respectively (that is, the mass fraction of the drug in the obtained liquid crystal nanoparticle precursor particles is respectively 4%) to obtain three parts of drug solutions; GMO and 0.6g, 0.7g and 0.8g of the diluent PVP K30 (that is, the GMO / PVP in the obtained liquid crystal nanoparticle precursor particles) were added respectively in three parts of drug solutions at 47°C of 0.4g, 0.3g and 0.2g. The ratio of K30 is 4 / 6, 3 / 7 and 2 / 8), vortexed and mixed to obtain three liquid crystal precursor solutions with good fluidity.

[0078] (2) Preparation of liquid crystal nanoparticle precursor particles

[0079] The uniform liquid crystal precursor solution is solidified and dispersed into liquid crystal nano par...

Embodiment 3

[0085] Example 3: Preparation of Liquid Crystal Nanoparticles by Dissolution Cleavage and Self-Assembly of Liquid Crystal Nanoparticle Precursor Particles Loaded with Docetaxel

[0086] Weigh 0.01g liquid crystal nanoparticle precursor particles (GMO / PVP / DTX=4 / 6 / 0.04, the preparation method is the same as in Example 2), vortex mix with 0.05g water, when the liquid crystal nanoparticle precursor particles contact with water At the same time, the liquid crystal nanoparticle precursor particles begin to dissolve and crack, and at the same time, the liquid crystal material and water undergo hydration and start to self-assemble to form dispersed liquid crystal nanoparticles.

[0087] The new suspension obtained in this example was scanned by a transmission electron microscope to observe the structural changes in the process of liquid crystal nanoparticle precursor particles being dissolved and cracked and self-assembled to obtain liquid crystal nanoparticles. Use a pipette gun to d...

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Abstract

The invention relates to a liquid crystal nanoparticle precursor microparticle, a self-assembled liquid crystal nanoparticle and preparation methods thereof. The preparation method of the liquid crystal nanoparticle precursor microparticle comprises dissolving an agent in a solvent, adding a molten liquid crystal material and a diluent into the solution, uniformly mixing the solution and drying the solution. The liquid crystal nanoparticle precursor microparticle comprises 0.5-20wt% of the agent and a ratio of the liquid crystal material, the diluent to the solvent is 1: 1-7: 40-150. The liquid crystal nanoparticle precursor particles and water undergo a hydration reaction so that the liquid crystal nanoparticle precursor particles are cracked and self-assembled to form the self-assembled liquid crystal nanoparticles. The liquid crystal nanoparticles are processed to form the liquid crystal nanoparticle precursor precursor microparticle solids so that formation of an unstable liquid crystal nanoparticle dispersed solution is avoided and the traditional method problems of leakage of liquid crystal nanoparticle agents, low encapsulation efficiency and dispersion system instability are solved.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a self-assembled liquid crystal nanoparticle precursor particle and a preparation method thereof. Background technique [0002] Most pharmaceutically active compounds face the problem of low solubility. Research shows that 40% of marketed drugs and 70% of drugs under research are poorly soluble drugs. The slow dissolution rate and low dissolution degree of poorly soluble drugs lead to low bioavailability of the drug and can not achieve ideal clinical efficacy. The drug must be delivered to the treatment site at a certain speed and reach a therapeutic concentration in order to exert its curative effect in time. This process requires the use of pharmaceutical preparations to increase the dissolution rate and solubility of the drug, thereby increasing the bioavailability of the drug and improving the clinical efficacy. The rate and extent of drug dissolution and release f...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/10A61K47/14A61K47/24A61K47/26B82Y5/00A61K31/4745A61K31/337
CPCA61K47/10A61K47/14A61K47/24A61K47/26A61K9/146A61K31/337A61K31/4745B82Y5/00
Inventor 潘昕梅丽玲杨蓓蓓吴传斌黄莹谢业城
Owner GUANGZHOU NEWORLD PHARMA CO LTD
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