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Cholesterol Hydrophobic Modification of Pullulan-Donepezil-Polysorbate 80 Nanoparticles and Its Preparation and Application

A pullulan nanometer and hydrophobic modification technology is applied in the preparation field of cholesterol hydrophobically modified pullulan-donepezil-polysorbate 80 nanoparticles, which can solve the problem of no sustained release function, no tissue specificity and poor dissolution. And other issues

Inactive Publication Date: 2019-09-27
HUNAN NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Based on this, it is necessary to provide a cholesterol hydrophobic modified pullulan-donepezil-polysorbate 80 nanoparticles and preparation and application

Method used

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  • Cholesterol Hydrophobic Modification of Pullulan-Donepezil-Polysorbate 80 Nanoparticles and Its Preparation and Application
  • Cholesterol Hydrophobic Modification of Pullulan-Donepezil-Polysorbate 80 Nanoparticles and Its Preparation and Application
  • Cholesterol Hydrophobic Modification of Pullulan-Donepezil-Polysorbate 80 Nanoparticles and Its Preparation and Application

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preparation example Construction

[0046] A preparation method of cholesterol hydrophobically modified pullulan-donepezil-polysorbate 80 nanoparticles, comprising the following steps:

[0047] dissolving cholesterol hydrophobically modified pullulan nanoparticles, donepezil and triethylamine in DMSO, dialyzing to remove DMSO, ultrasonically treating the dialysate, and filtering through a filter membrane to obtain a cholesterol hydrophobically modified pullulan-donepezil nanoparticle solution;

[0048] Add polysorbate 80 to the cholesteric hydrophobically modified pullulan-donepezil nanoparticle solution, and after standing for 1 hour, ultrasonically treat until a uniform dispersion is obtained, and remove impurities by filtration through a filter membrane to obtain cholesteric hydrophobically modified pullulan. Lulan-Donepezil-Polysorbate 80 Nanoparticles.

[0049] Further, the concentration of polysorbate 80 is 0.7 mmol.

[0050] Further, the dialysis process is specifically:

[0051] Transfer the solution i...

Embodiment

[0059] Materials. Constant temperature magnetic stirrer (IKA RCT basic, Germany); Vacuum freeze dryer (Maxi DryLyo Heto-Holten company); Transmission electron microscope (TEM) (JIEM-100S Japan); Nanoparticle size and Zeta potential analyzer (Malvern ZS-90, UK); UV-vis spectrophotometer (JASCO V-560, US); isothermal titration calorimeter (VP-ITC, Microcal, Inc.Northampton, MA); dialysis bag (molecular weight cut-off 8~12KDa, Germany); cholesteryl hydrophobically modified pullulan (self-made); donepezil (Donepezil, Shanghai Ziqi Biotechnology Co., Ltd.); polysorbate 80 (Polysorbate-80, Tianjin Fuchen Reagent Institute); the rest of the reagents were Domestic analytically pure.

[0060] Preparation

[0061] 1. Preparation of CHP and DZP-CHP nanoparticles by dialysis.

[0062] Dissolve 2.5g (6.5mmol) of cholesterol modification and 2.0g (20mmol) of succinic anhydride in 20mL of anhydrous pyridine, react at 50°C for 48h, then stop the reaction, and drop the reaction solution in...

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Abstract

The invention discloses a cholesterol hydrophobic modification pullulan-donepezil-polysorbate 80 nano particle. The nano particle comprises a cholesterol hydrophobic modification pullulan nano particle, donepezil loaded in the cholesterol hydrophobic modification pullulan nano particle and polysorbate 80 adsorbed on the surface of the cholesterol hydrophobic modification pullulan nano particle. The cholesterol hydrophobic modification pullulan-donepezil-polysorbate 80 nano particle has good drug loading capacity, encapsulation efficiency and slow-release effect on the donepezil, and can be used for maintaining blood concentration within a longer time, prolonging medicine taking intervals and improving patient compliance. In addition, as the stability is improved, the dosage, which enters the whole body to circulate, is reduced, more nano particles stride a blood brain barrier before releasing medicine, so that the medicine is enriched at the brain, the release after location is realized, not only is the dosage reduced, but also the toxicity to a peripheral nervous system is reduced.

Description

technical field [0001] The invention relates to the field of nano preparations, in particular to cholesterol hydrophobically modified pullulan-donepezil-polysorbate 80 nanoparticles, in particular to a method for preparing cholesterol hydrophobically modified pullulan-donepezil-polysorbate 80 nanoparticles and apply. Background technique [0002] The dosage forms and administration methods of poorly soluble drugs are research hotspots. Oral solid drugs are released from the preparation and dissolved in body fluids to be absorbed. Therefore, poor dissolution will lead to slow drug absorption and low bioavailability in the body, and cannot reach the therapeutic level of blood drug concentration, resulting in poor clinical efficacy. . Drugs with high fat solubility can easily cross the blood-brain barrier and exert their medicinal effects in the brain. Therefore, when preparing conventional preparations for brain diseases, it is often necessary to add a large amount of excipi...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K31/445A61K47/36A61K47/26A61P25/28A61P25/00
Inventor 陶晓军冯星杨小平朱丽李昱胡倩
Owner HUNAN NORMAL UNIVERSITY
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