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Preparation method of PEG-PLA/PLA composite drug loaded nanometer microballoon

A PEG-PLA, drug-loaded nanotechnology, applied in the field of drug release carrier preparation, can solve the problems of large particle size, uneven particle size, cumbersome process, etc., and achieve simple preparation method, short reaction time, and improved solubility Effect

Active Publication Date: 2014-04-02
WANNAN MEDICAL COLLEGE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these preparation methods have disadvantages such as long time-consuming, complicated operation, cumbersome process, large particle size, non-uniform particle size, and low encapsulation efficiency of the prepared microspheres.

Method used

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  • Preparation method of PEG-PLA/PLA composite drug loaded nanometer microballoon
  • Preparation method of PEG-PLA/PLA composite drug loaded nanometer microballoon
  • Preparation method of PEG-PLA/PLA composite drug loaded nanometer microballoon

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Weigh 200mg PEG-PLA (weight average molecular weight 8500), 100mg PLA (weight average molecular weight 30000), 30mg paclitaxel, add 2mL dichloromethane, 100w ultrasound for 1min to completely dissolve the carrier material and drug, then add 20mL deionized water to it , continue ultrasonication at 200w for 3min in an ice-water bath, then rise to room temperature, stir mechanically at 300rpm for 8h to completely volatilize the organic solvent, and finally freeze and centrifuge the drug-loaded microsphere emulsion at 15000rpm at 4°C for 15min at high speed, and freeze-dry the obtained solid to remove water and place it in Store in a sealed container at 4°C. The prepared paclitaxel-loaded PEG-PLA / PLA composite nanospheres showed a regular "core-shell" structure under TEM, with an average particle size of 300nm and an encapsulation efficiency of 80%.

Embodiment 2

[0028] Weigh 200mg PEG-PLA (weight average molecular weight 9800), 100mg PLA (weight average molecular weight 30000), 20mg paclitaxel, add 2mL dichloromethane, 300w ultrasonic 2min to completely dissolve the carrier material and drug, then add 10mL deionized water to it , continue ultrasonication at 200w for 10min in an ice-water bath, then rise to room temperature, ultrasonication at 200w for 1h to completely volatilize the organic solvent, and finally refrigerate and centrifuge the drug-loaded microsphere emulsion at 15000rpm at 4°C for 10min at high speed, and freeze-dry the obtained solid to remove water and place it in 4 ℃ sealed storage. The prepared paclitaxel-loaded PEG-PLA / PLA composite nanospheres showed a regular "core-shell" structure under TEM, with an average particle size of 250nm and an encapsulation efficiency of 75%.

Embodiment 3

[0030] Weigh 300mg PEG-PLA (weight average molecular weight 9800), 100mg PLA (weight average molecular weight 30000), 30mg paclitaxel, add 2mL dichloromethane, 500w ultrasound for 1min to completely dissolve the carrier material and drug, then add 30mL deionized water to it , continue ultrasonication at 300w for 15min in an ice-water bath, then rise to room temperature, mechanically stir at 900rpm for 20h to completely volatilize the organic solvent, and finally freeze and centrifuge the drug-loaded microsphere emulsion at 18000rpm at 4°C for 10min at high speed, and freeze-dry the obtained solid to remove water and place it in Store in a sealed container at 4°C. The prepared paclitaxel-loaded PEG-PLA / PLA composite nanospheres showed a regular "core-shell" structure under TEM, with an average particle size of 200nm and an encapsulation efficiency of 85%.

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Abstract

The invention relates to a preparation method of PEG-PLA / PLA composite drug loaded nanometer microballoon. The preparation process comprises the following steps: firstly, adding PEG-PLA, PLA and hydrophobic medicament into a volatile organic solvent and mixing by ultrasound; adding water and emulsifying into a primary emulsion; completely volatilizing the organic solvent and preparing a drug loaded microballoon suspension; refrigerating the suspension at a high speed and depriving moisture by centrifugation, and carrying out freeze drying; obtaining the PEG-PLA / PLA composite drug loaded nanometer microballoon. The invention has the advantages of simple preparation method, simple operation, low cost, time saving and high efficiency and easy large scale production, simultaneously the prepared drug loaded microballoon has a core-casing structure with small particle size, high drug loading and long-acting slow release.

Description

technical field [0001] The invention belongs to the technical field of preparation of drug release carriers, and in particular relates to a preparation method of PEG-PLA / PLA composite drug-loaded nano microspheres. Background technique [0002] Drug carrier is an important part of drug sustained-release system, and also the main factor affecting drug efficacy. The preparation of drug carriers with stable structure, small particle size, long circulation time in vivo, good safety and high targeting has become the goal pursued by the domestic and foreign medical circles. [0003] Polylactic acid (PLA) is a non-toxic and non-irritating polymer material obtained by polymerizing D,L-lactic acid as a monomer. It has good biocompatibility and biodegradability. It is the second polyglycolic acid (PGA) The second type of degradable polymer materials approved by the FDA for use in the human body. However, the structure of PLA contains a large number of hydrophobic ester bonds, which ...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/34B82Y40/00
Inventor 孙玉汤琳陈云艳
Owner WANNAN MEDICAL COLLEGE
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