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Nanosuspension of annonaceous acetogenin drugs and preparation method of nanosuspension

A nano-suspension and custard apple technology, which is applied in drug combination, drug delivery, and pharmaceutical formulation, can solve the problems of difficulty in maximizing the curative effect, low bioavailability, and limited in vivo research, and achieve broad industrialization Prospect, economic safety of excipients, effect of high tumor cell inhibition rate

Active Publication Date: 2017-02-22
INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] ACGs have poor water solubility, less than 1ug / mL, and are difficult to administer, resulting in greatly limited in vivo research
Existing in vivo studies mostly adopt suspension gavage, or disperse in vegetable oil for oral administration, and its curative effect is difficult to maximize due to low bioavailability
Moreover, ACGs have large toxic and side effects, narrow therapeutic window, and have certain toxicity to the liver and kidney of rats.

Method used

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  • Nanosuspension of annonaceous acetogenin drugs and preparation method of nanosuspension
  • Nanosuspension of annonaceous acetogenin drugs and preparation method of nanosuspension
  • Nanosuspension of annonaceous acetogenin drugs and preparation method of nanosuspension

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Effect test

Embodiment 1

[0034] Weigh 9 mg of annonacein lactone, dissolve 3 mg of mPEG2000-PCL2000 in 0.5 mL of acetone, and slowly drip the above acetone solution into 4 mL of deionized water at room temperature under ultrasonic conditions of 250 Hz. After continuing to sonicate for 15 minutes, the acetone was removed by rotary evaporation to obtain the ACGs nanosuspension. The average particle size is 123.2nm ( figure 1 ), the polydispersity index (PDI) was 0.134, and the potential value was -20.17mV.

Embodiment 2

[0036]Weigh 9 mg of annonacein lactone, dissolve 3 mg of mPEG2000-PCL1140 in 0.5 mL of acetone, and slowly drip the above acetone solution into 4 mL of deionized water at room temperature under ultrasonic conditions of 250 Hz. After continuing to sonicate for 15 minutes, the acetone was removed by rotary evaporation to obtain the ACGs nanosuspension. The average particle diameter was 136.4 nm, the polydispersity index (PDI) was 0.06, and the potential value was -19.9 mV.

Embodiment 3

[0038] Weigh 9 mg of annonacein lactone, dissolve 3 mg of mPEG5000-PCL1000 in 0.5 mL of acetone, and slowly drip the above acetone solution into 4 mL of deionized water at room temperature under ultrasonic conditions of 250 Hz. After continuing to sonicate for 15 minutes, the acetone was removed by rotary evaporation to obtain the ACGs nanosuspension. The average particle diameter is 163.7nm, the polydispersity index (PDI) is 0.09, and the potential value is -17mV.

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Abstract

The invention belongs to the technical field of medicines, and in particular relates to a nanosuspension of annonaceous acetogenin drugs prepared from such amphiphilic stabilizers as mPEG PCL, mPEG PLA, mPEG PLGA, mPEG DSPE, mPEG Chol, SPC, Tween80, BSA, TPGS and the like, as well as a preparation method and an application of the nanosuspension. The annonaceous acetogenin total lactone nanosuspension is prepared by virtue of a solvent precipitation-ultrasonic injection method, and according to a prescription, the proportioning ratio of the annonaceous acetogenin drugs to the stabilizer is at 1 to (0.02-10) (in percentage by weight). The prepared annonaceous acetogenin nanosuspension can reach a load-loading capacity to 90% to the greatest extent and can reach a minimum grain size to 123.2nm, and the nanosuspension is good in polydispersity. The nanosuspension is stable in both gastrointestinal fluid and plasma, and the nanosuspension is applicable to oral administration and injection administration; the nanosuspension has a good in-vitro sustained-release effect and is free from burst release; the nanoparticle, in comparison with a crude drug solution, is more obvious in tumor cell inhibitory rate in vitro; the nanosuspension, in in-vivo tissue distribution, shows tumor passive targeting; therefore, the nanosuspension is beneficial for enhancing efficacy and reducing toxic and side effects. Meanwhile, an in-vivo efficacy experiment shows that the nanosuspension is outstanding in antineoplastic efficacy, and the nanosuspension has a broad development prospect.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an anemone prepared from amphiphilic stabilizers such as mPEG-PCL, mPEG-PLA, mPEG-PLGA, mPEG-DSPE, mPEG-Chol, SPC, Tween80, BSA, and TPGS Nano-suspension of similar drugs, and its preparation method and application. Background technique [0002] Annonacein includes annonacein lactones (ACGs for short) and its monomers bullatacin, squamostatin, annosquacin, etc. Annonacein is a series of long-chain fatty acids with 35 or 37 carbons extracted from the seeds of Annonaceae plants, and contains 0 to 3 tetrahydrofuran (THF) ring-like structures. Most of the total lactones and monomers of custard apple showed strong anti-tumor activity, and the most active monomer bullatacin was effective against lung cancer A549 cells, human liver cancer HepG2 cells, human cervical cancer HeLa cells, and human breast cancer MCF-7 cells. , human colon cancer Lovo cells, sarcoma S180 cells, e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/19A61K36/185A61K47/34A61K47/24A61K47/26A61K47/28A61K47/22A61K47/42A61P35/00
CPCA61K9/0019A61K9/10A61K9/19A61K36/185A61K47/22A61K47/24A61K47/26A61K47/28A61K47/34A61K47/42
Inventor 王向涛洪靖怡李艳红李怡静
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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