Nimodipine/ligustrazine double-load PLGA nanoparticles and preparation method thereof

A dual drug-carrying, nanoparticle technology, applied in pharmaceutical formulations, drug combinations, and non-active ingredients medical preparations, etc., can solve the problems of normal cell or tissue toxicity, short drug half-life, frequent dosing, etc., to avoid Strengthen the liver first-pass effect, reduce toxic and side effects, and delay the effect of drug release

Active Publication Date: 2014-01-08
ZHEJIANG CHINESE MEDICAL UNIVERSITY
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  • Abstract
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Problems solved by technology

Therefore, the combination of TMP and NMD is expected to increase the concentration of NMD in the brain, but the simple combination of NMD and TMP still has the problem of short half-life of...

Method used

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  • Nimodipine/ligustrazine double-load PLGA nanoparticles and preparation method thereof
  • Nimodipine/ligustrazine double-load PLGA nanoparticles and preparation method thereof
  • Nimodipine/ligustrazine double-load PLGA nanoparticles and preparation method thereof

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Embodiment 1

[0019] 1. Instruments and materials

[0020] 1.1 Instruments

[0021] UV-1700 Ultraviolet Spectrophotometer (Shimadzu Corporation, Japan); Agilent1200 High Performance Liquid Chromatograph (Agilent Technology Co., Ltd., USA); 380ZLS Laser Particle Size Analyzer (Nico mp Corporation, USA); JEM-1200EX Transmission Electron Microscope (JEOL Corporation, Japan) ); Labconco freeze dryer (Labconco, USA); Mill-Q ultrapure water device (Millpore, USA); KQ5200DE CNC ultrasonic cleaner (Kunshan Ultrasonic Instrument Co., Ltd.); TGL-16B high-speed desktop centrifuge (Shanghai Anting Scientific Instrument Factory); CP225D Electronic Balance (Beijing Sartorius Scientific Instrument Co., Ltd.); Nitrogen Purge (Hangzhou Aosheng Instrument Co., Ltd.); Dialysis Bag (Shanghai Green Bird Technology Development Co., Ltd., Mw=14000Da); HZ-9212S water bath constant temperature oscillator (Jiangsu Taicang Hualida Experimental Equipment Co., Ltd.).

[0022] 1.2 Drugs and Reagents

[0023] Nimodipi...

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Abstract

The invention relates to nimodipine/ligustrazine double-load PLGA nanoparticles which are prepared through a method comprising the steps that: nimodipine, ligustrazine phosphate and a polylactic acid-glycolic acid copolymer are precisely weight according to a mass ratio of 1:5-20:40-60; the materials are dissolved into acetone, such that an organic phase is obtained; a PVA water solution with a mass concentration of 0.5-1.0% is adopted as an aqueous phase; under stirring, the organic phase is slowly dropped into the aqueous phase; when dropping is finished, the mixture is continued to be stirred for 2-4h under a constant temperature of 40-50 DEG C, such that the organic solvent is volatilized; centrifugation is carried out; a sediment is washed 2-3 timed by using distilled water, and is lyophilized, such that the nimodipine/ligustrazine double-loading PLGA nanoparticles are obtained. According to the invention, PLGA is adopted as a carrier material, and P-gp inhibitors TMP and NMD are applied in combination, such that NMD/TMP-PLGA-NPs are prepared. Therefore, defects of short drug half-life, easy generation of cytotoxicity, and the like of simple combination are avoided, a P-gp efflux effect is inhibited, and NMD distribution to tissues is promoted. Therefore, the nanoparticles have certain advantages over single-load nanoparticles.

Description

(1) Technical field [0001] The invention relates to a nimodipine / ligustrazine double drug-loaded PLGA nanoparticle (NMD / TMP-PLGA-NPs) and a preparation method thereof. (2) Background technology [0002] Nimodipine (NMD) is a class of dihydropyridine calcium antagonists, which treat cerebrovascular diseases by dilating cerebral arterioles and increasing intracerebral blood flow. However, NMD is poorly water-soluble, and the commercially available NMD injection mainly dissolves the drug through ethanol, which is irritating to a certain extent; the clinically used NMD oral preparation has a short biological half-life, strong first-pass effect, and a bioavailability of only 5% to 13%; At the same time, as a substrate of P-glycoprotein (P-gp), NMD is easily affected by the efflux of P-gp on the blood-brain barrier (BBB), resulting in a low concentration in the brain, which limits its use in the brain. Therapeutic effect in the onset of cerebrovascular disease. Ligustrazine (Tet...

Claims

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Application Information

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IPC IPC(8): A61K31/4965A61K9/16A61K47/34A61P9/10A61K31/4422
Inventor 李范珠何雯洁王国伟魏颖慧郭曼曼徐骏军
Owner ZHEJIANG CHINESE MEDICAL UNIVERSITY
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