Preparation method of taxol-loading polylactic acid-hydroxyacetic acid microspheres

A glycolic acid microsphere, glycolic acid technology, applied in microcapsules, capsule delivery, antitumor drugs and other directions, can solve the problems of poor water solubility of paclitaxel injection, low drug utilization rate, obvious adverse reactions in high-concentration treatment, etc. Effects of stability, maintaining drug concentration, prolonging the time of antitumor effect

Inactive Publication Date: 2017-08-18
WUHAN UNIV OF TECH
View PDF3 Cites 13 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, paclitaxel injections commonly used in clinical practice have problems such as poor water solubility, low drug utilization rate, and obvious adverse reactions in high-concentration treatment.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Preparation method of taxol-loading polylactic acid-hydroxyacetic acid microspheres
  • Preparation method of taxol-loading polylactic acid-hydroxyacetic acid microspheres
  • Preparation method of taxol-loading polylactic acid-hydroxyacetic acid microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Accurately weigh 200mg of PLGA (LA / GA=75:25, Mn=17317) and dissolve it in 4ml of dichloromethane solvent with ultrasonic vibration to obtain a 50mg / ml solution. Then accurately weigh 15mg of paclitaxel and dissolve it in it. Probe ultrasonic 40s under condition, every time ultrasonic 8s minute pause 4s, measure 100ml freshly prepared 2wt% PVA aqueous solution with graduated cylinder, under 800rpm room temperature magnetic stirring, organic phase is added dropwise in 100ml continuous phase with 1ml injection needle, forms For the oil-in-water emulsion, continue to stir for 6 hours to fully volatilize the dichloromethane, then centrifuge the paclitaxel PLGA microspheres, wash them four times with deionized water at 4000rpm, then add 2 mL of newly prepared 1 wt% mannitol solution to freeze-dry After 72 hours, paclitaxel-loaded PLGA microspheres were obtained.

Embodiment 2

[0037] Accurately weigh 200mg of PLGA (LA / GA=75:25, Mn=17317) and dissolve it in 4ml of dichloromethane solvent to obtain a 50mg / ml solution, then accurately weigh 20mg of paclitaxel and dissolve it in it. Sonicate the probe for 40s, pause for 4s for 8s each time, measure 100ml of newly prepared 2wt% PVA aqueous solution with a measuring cylinder, and add the organic phase dropwise to 100ml of the continuous phase with a 1ml injection needle under magnetic stirring at 800rpm room temperature to form water packets. For the oily emulsion, continue to stir for 6 hours to fully volatilize the dichloromethane, then centrifuge the paclitaxel PLGA microspheres, wash them four times with deionized water at 4000 rpm, add 2 mL of newly prepared 1 wt% mannitol solution and freeze-dry for 72 hours That is, paclitaxel-loaded PLGA microspheres were obtained.

Embodiment 3

[0039] Accurately weigh 200mg of PLGA (LA / GA=75:25, Mn=17317) and dissolve it in 4ml of dichloromethane solvent to obtain a 50mg / ml solution, then accurately weigh 25mg of paclitaxel and dissolve it in it. Sonicate the probe for 40s, pause for 4s for 8s each time, measure 100ml of newly prepared 2wt% PVA aqueous solution with a measuring cylinder, and add the organic phase dropwise to 100ml of the continuous phase with a 1ml injection needle under magnetic stirring at 800rpm room temperature to form water packets. For the oily emulsion, continue to stir for 6 hours to fully volatilize the dichloromethane, then centrifuge the paclitaxel PLGA microspheres, wash them four times with deionized water at 4000rpm, add 2 mL of newly prepared 1wt% mannitol solution and freeze-dry for 72 hours That is, paclitaxel-loaded PLGA microspheres were obtained.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
degree of polymerizationaaaaaaaaaa
Login to view more

Abstract

The invention belongs to the field of preparation of targeted therapeutic microspheres of slow release formulation and in particular relates to a preparation method of taxol-loading polylactic acid-hydroxyacetic acid (PLGA) microspheres. The preparation method comprises the following steps: dissolving a polylactic acid-hydroxyacetic acid copolymer in an organic solvent, and adding a taxol drug, wherein the polymer and the taxol drug are uniformly dissolved to obtain an organic phase; dropwise adding the organic phase into a fresh polyvinyl alcohol aqueous solution and curing and forming microspheres; and performing centrifugal separation on the cured drug-loading microspheres to obtain the uniformly dispersed taxol-loading polylactic acid-hydroxyacetic acid (PLGA) microspheres. The taxol-loading targeted therapeutic PLGA microspheres prepared by the preparation method have an ideal drug loading ratio and encapsulation efficiency while guaranteeing the drug stability of taxol, can reach an effect of slow release, maintain the optimum drug concentration in vivo, prolong the action time of the drug and reduce the side effects brought by burst release of the drug, and have important theoretical value and actual application prospect.

Description

technical field [0001] The invention belongs to the field of preparation of microspheres of targeted therapeutic drugs in sustained-release dosage form, and in particular relates to a preparation method of paclitaxel-loaded polylactic-glycolic acid (PLGA) microspheres. Background technique [0002] Paclitaxel is a new type of effective anti-tumor drug isolated from the bark of the Pacific yew tree. The molecular formula of paclitaxel is C 47 h 51 0 14 N, molecular weight 853.9 (structural formula shown below), highly lipophilic, insoluble in water, plasma protein binding rate 89%-98%, half-life 5.3-17.4h, mainly metabolized by liver, only 5% cleared by kidney. [0003] [0004] The study found that paclitaxel can be used as a specific stabilizer of cell microtubules, which can promote the assembly of microtubules and maintain the stability of microtubules. When the cells are in contact with paclitaxel, a large number of microtubules will accumulate in the cells, and th...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K47/34A61K31/337A61P35/00
Inventor 王欣宇张宗瑞
Owner WUHAN UNIV OF TECH
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap