Layer-by-layer self-assembly loaded amphiphilic drug microcapsules and preparation method thereof

A technology of microcapsules and parents, which is applied in microcapsules, capsule delivery, pharmaceutical formulations, etc., can solve the problems of difficult-to-handle soft emulsion cores, micellar cytotoxicity, and harsh solvent requirements, and achieve good degradation characteristics and good biological phases. The effect of capacitive and particle size adjustable

Active Publication Date: 2020-04-10
NORTHWEST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, sustained-release systems such as polymer particles, polymer micelles, polymer microspheres, and polymer vesicles have entered clinical applications, but there are problems with difficult-to-handle soft emulsion cores, micellar cytotoxicity, easily damaged shell walls, necessary oil phases, Defects such as harsh requirements for solvents

Method used

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  • Layer-by-layer self-assembly loaded amphiphilic drug microcapsules and preparation method thereof
  • Layer-by-layer self-assembly loaded amphiphilic drug microcapsules and preparation method thereof
  • Layer-by-layer self-assembly loaded amphiphilic drug microcapsules and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Using stirring co-precipitation method, 5mL 0.33mol / L K 2 CO 3 The aqueous solution was quickly added to 5mL 0.33mol / LCaCl 2 In the aqueous solution, stir vigorously for a certain period of time, and stand at 20°C for 60 minutes.

[0051] Among them, the stirring rate is 2600r / min, the stirring time is 15min, and the 20°C is left standing for 60min, the obtained CaCO 3 Microsphere particle size 1.5-2.5μm, average pore size 30.048nm, specific surface area 7.027m 2 / g, pore volume 0.085cm 3 / g, surface charge +12.6mV.

Embodiment 2

[0053] Weigh 50mg CaCO 3 After the microspheres (prepared in Example 1) were added to 1.5 mL of acetone for ultrasonic dispersion for 10 min, 5 mL of acetone solution in which PLLA (L-PLA) was dissolved was taken and added dropwise to the solution containing CaCO under stirring conditions. 3 In the beaker of the microspheres, seal the beaker, and after adsorbing at 37°C for a certain period of time for 60 minutes, centrifuge at a centrifugal acceleration of 4000×g for 2 minutes, discard the supernatant, and then wash once with acetone (centrifugation for 2 minutes), and the obtained microspheres are immediately mixed with 0.02% PVA aqueous solution (2mL) was mixed by a vortex mixer for 2-3 minutes, centrifuged, the supernatant was discarded, washed with distilled water, and centrifuged twice to obtain CaCO 3 / PLLA microspheres. Dissolve CaCO with 2 mL of 0.1 mol / L HCl solution 3 Centrifuge the inner core at a centrifugal acceleration of 6000×g for 2 minutes, discard the sup...

Embodiment 3

[0058] The CaCO obtained in the previous step 3 / PLLA microspheres (5.14mg) were dispersed in NaCl aqueous solution (5mL) with a concentration of 0.5mol / L and pH=6.5, and the first microsphere dispersion was obtained after ultrasonic dispersion for 10min. A certain concentration of 5mL CHI (chitosan ) solution (2g / L), under stirring condition, add dropwise to CaCO 3 / PLLA microsphere dispersion (first microsphere dispersion), after adsorption at 25°C for 30min, centrifuge at a centrifugal acceleration of 4000×g for 2min, discard the supernatant, and wash with 0.5mol / L, pH=6.5NaCl solution , centrifuged twice. The prepared CaCO 3 / PLLA / CHI microspheres were dispersed in NaCl aqueous solution (5 mL) with a concentration of 0.5 mol / L and pH=6.5 to obtain CaCO 3 / PLLA / CHI microsphere dispersion (second microsphere dispersion), a certain concentration of 5mL CMC (carboxymethyl cellulose, optional sodium salt) solution (2g / L) was added dropwise to CaCO 3 / PLLA / CHI microsphere di...

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Abstract

The invention provides a layer-by-layer self-assembled microcapsule loaded with amphiphilic drugs and a preparation method thereof. The shell of the microcapsule is a PLA layer, and the PLA layer is covered with a controlled release layer. The controlled release layer is made of a cationic polymer. The microcapsule is composed of layers of layers and anionic polymers; the cavity of the microcapsule is filled with hydrophilic drugs, proteins, DNA or RNA, and the PLA layer is coated with hydrophobic drugs. The amphiphilic drug microcapsules are easy to prepare, have good sustained and controlled release, can be made of non-toxic, biocompatible and degradable materials, and can be used for embedding and controlling both fat-soluble and water-soluble drugs. freed.

Description

technical field [0001] The invention belongs to the field of biomedical polymer materials, and relates to a layer-by-layer self-assembly loaded amphiphile drug microcapsule and a preparation method thereof. Background technique [0002] In recent years, the slow-release and controlled-release technology of drugs has developed rapidly. The sustained and controlled release system plays an important role in reducing drug side effects and administration times, reducing blood drug concentration fluctuations and gastrointestinal irritation. At present, sustained-release systems such as polymer particles, polymer micelles, polymer microspheres, and polymer vesicles have entered clinical applications, but there are problems with difficult-to-handle soft emulsion cores, micellar cytotoxicity, easily damaged shell walls, necessary oil phases, Defects such as harsh requirements for solvents. Layer-by-layer self-assembled polymer microcapsules have the advantages of good permeability,...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K47/34A61K47/36A61K47/38A61K47/02A61K45/06A61K31/65A61K31/192
CPCA61K9/5031A61K9/5036A61K9/5042A61K9/5073A61K31/192A61K31/65A61K45/06A61K2300/00
Inventor 郝红蔡杰慧王君刘建连赵夏段延萍
Owner NORTHWEST UNIV
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