Annonaceous acetogenins nanosuspensions stabilized by PCL-PEG block polymer: significantly improved antitumor efficacy

Annonaceous acetogenins (ACGs) have shown superior antitumor activity against a variety of cancer cell lines, but their clinical application has been limited by their poor solubility. In this study, ACGs-nanosuspensions (NSps) were successfully prepared by a precipitation ultrasonic method using mon...

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Bibliographic Details
Published in:International journal of nanomedicine 2016-01, Vol.11, p.3239-3253
Main Authors: Hong, Jingyi, Li, Yanhong, Li, Yijing, Xiao, Yao, Kuang, Haixue, Wang, Xiangtao
Format: Article
Language:English
Subjects:
Acetogenins - pharmacology
Animals
Antineoplastic Agents - pharmacology
Bioavailability
Breast cancer
Cancer therapies
Cell Death - drug effects
Cell Proliferation - drug effects
Drug delivery systems
Drug dosages
Drug Liberation
Drug resistance
Experiments
Female
HeLa Cells
Herbal medicine
Humans
Inhibitory Concentration 50
Laboratory animals
Liver cancer
MCF-7 Cells
Mice, Inbred BALB C
Nanoparticles
Nanoparticles - chemistry
Original Research
Particle Size
Penicillin
Polyesters - chemistry
Polyethylene Glycols - chemistry
Quantitative analysis
Suspensions
Tissue Distribution - drug effects
Treatment Outcome
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Summary:Annonaceous acetogenins (ACGs) have shown superior antitumor activity against a variety of cancer cell lines, but their clinical application has been limited by their poor solubility. In this study, ACGs-nanosuspensions (NSps) were successfully prepared by a precipitation ultrasonic method using monomethoxypoly (ethylene glycol)2000-poly (ε-caprolactone)2000 (mPEG2000-PCL2000) as a stabilizer. The resultant ACGs-NSps had a mean particle size of 123.2 nm, a zeta potential of -20.17 mV, and a high drug payload of 73.68%. ACGs-NSps were quite stable in various physiological solutions, and they exhibited sustained drug release. Compared to free drug, ACGs-NSps exhibited stronger cytotoxicity against 4T1, MCF-7, and HeLa cells. An in vivo real-time biodistribution investigation after labeling with 1,1'-dioctadecyltetramethyl indotricarbocyanine iodide, a noninvasive near-infrared fluorescence probe, demonstrated that ACGs-NSps could effectively accumulate in tumor. An in vivo antitumor activity study in 4T1 tumor-bearing mice revealed that ACGs-NSps achieved much better therapeutic efficacy than the traditional dosage form (oil solution) even at 1/10 of the dose (74.83% vs 45.53%, P
ISSN:1178-2013
1176-9114
1178-2013
DOI:10.2147/IJN.S108143