Drug-containing nanoparticles
By using nanoparticle technology to deliver pioglitazone to unstable plaques, the shortcomings of existing drug-eluting stents in preventing acute coronary syndromes are solved, achieving effective treatment of atherosclerotic diseases and reducing systemic side effects.
- Summary
- Abstract
- Description
- Claims
- Application Information
AI Technical Summary
Problems solved by technology
Method used
Examples
preparation example Construction
[0044] Although the preparation method of the nanoparticles of the present invention is not particularly limited as long as it can process pioglitazone or a salt thereof and a biocompatible polymer into particles having an average particle size of less than 1,000 nm, a spherical crystallization method can preferably be used (spherical crystallization method), which is a non-high shear force particle preparation method.
[0045] The spherical crystallization method is a method of designing spherical crystal particles by controlling the crystal formation / growth process at the final stage of compound synthesis, and processing the particles by directly controlling their properties. One of spherical crystallization methods is an emulsion solvent diffusion method (ESD method).
[0046] The ESD method is a technique for preparing nanospheres by the following principle. In this method, two kinds of solvents are used: a good solvent that can dissolve lactic acid-glycolic acid copolyme...
Embodiment 1
[0102] Preparation of PLGA nanoparticles containing pioglitazone
[0103] An aqueous solution of 0.5 wt% polyvinyl alcohol (Gosenol EG-05 (registered trademark), manufactured by The Nippon Synthetic Chemical Industry Co., Ltd.) was prepared and used as a poor solvent. Separately, lactic acid-glycolic acid copolymer (PLGA7520, lactic acid / glycolic acid=75 / 25, weight average molecular weight 20,000, Wako Pure Chemical Industries, Ltd.) (1 g) was dissolved in acetone (40 mL), and mixed with methanol ( 20 mL) of pioglitazone hydrochloride (40 mg), and this mixture was used as a polymer solution. At 40° C., the solution was added dropwise to the previously obtained poor solvent at 4 mL / min while stirring at 400 rpm to obtain a PLGA nanoparticle suspension containing pioglitazone. Under reduced pressure, acetone and methanol were evaporated for 1.5 hours, and the residue was freeze-dried to obtain pioglitazone-containing PLGA nanoparticle powder.
[0104] The obtained powder had g...
Embodiment 2
[0209] (1) Preparation of chitosan-modified PLGA nanoparticles comprising pioglitazone
[0210] PLGA (PLGA7520, lactic acid / glycolic acid=75 / 25, weight average molecular weight 20,000, manufactured by Wako Pure Chemical Industries, Ltd.) (2 g) was dissolved in acetone (20 mL), and pioglitazone dissolved in methanol (10 mL) was added Hydrochloride (100 mg) to give a polymer solution. This solution was added dropwise to an aqueous solution (50 mL) of 2 wt% polyvinyl alcohol (PVA, manufactured by KURARAY CO., LTD.) at a constant rate of 4 mL / min at 40°C while stirring. At this time, nano-sized emulsion droplets are prepared because of self-emulsification caused by turbulence generated on the surface of emulsion droplets by interdiffusion of acetone, methanol, and water. Thereafter, acetone and methanol were evaporated, and the obtained PLGA nanoparticle suspension was centrifuged (centrifugal acceleration 41000G, -20°C, 20min) to obtain a PLGA nanoparticle precipitate, which was...
PUM
| Property | Measurement | Unit |
|---|---|---|
| size | aaaaa | aaaaa |
| diameter | aaaaa | aaaaa |
| length | aaaaa | aaaaa |
Abstract
Description
Claims
Application Information
Login to View More