Folic acid-modified celastrol nanoparticles: synthesis, characterization, anticancer activity in 2D and 3D breast cancer models

Celastrol is used in traditional Chinese medicine for treating cancers. However, its low water solubility and poor tumour selection represent major pitfalls for clinical application. In the present study, gold nanoparticle (AuNP) firstly was conjugated with PVP-co-2-dimethylaminoethyl methacrylate (...

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Bibliographic Details
Published in:Artificial cells, nanomedicine, and biotechnology nanomedicine, and biotechnology, 2020-01, Vol.48 (1), p.542-559
Main Authors: Law, Siukan, Leung, Albert Wingnang, Xu, Chuanshan
Format: Article
Language:English
Subjects:
Anticancer properties
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - metabolism
Antineoplastic Agents - pharmacology
Antitumor activity
Apoptosis
Apoptosis - drug effects
Breast cancer
Breast Neoplasms - drug therapy
Breast Neoplasms - pathology
Capsules
Celastrol
Cell Survival - drug effects
Drug Stability
Encapsulation
folate receptor-targeted celastrol AuNP (FCA)
Folate Receptors, GPI-Anchored - metabolism
Folic acid
Folic Acid - chemistry
Folic Acid - metabolism
Folic Acid - pharmacology
Fourier transforms
Gold - chemistry
Gold - pharmacology
gold nanoparticles (AuNP)
Humans
Inductively coupled plasma mass spectrometry
Infrared reflection
Infrared spectroscopy
Mass spectrometry
Mass spectroscopy
MCF-7 Cells
Metal Nanoparticles - chemistry
Metal Nanoparticles - toxicity
Molecular Structure
Nanoparticles
Particle Size
Physical properties
Polymers
Polymers - chemistry
Polymers - pharmacology
PVP-co-2-dimethylaminoethyl methacrylate
Scientific imaging
Solubility
Spheroids, Cellular - drug effects
Three dimensional models
Traditional Chinese medicine
Triterpenes - chemistry
Triterpenes - pharmacology
Tumors
Two dimensional models
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Summary:Celastrol is used in traditional Chinese medicine for treating cancers. However, its low water solubility and poor tumour selection represent major pitfalls for clinical application. In the present study, gold nanoparticle (AuNP) firstly was conjugated with PVP-co-2-dimethylaminoethyl methacrylate (Polymer) and celastrol then modified by folic acid. The as-prepared folate receptor-targeted celastrol AuNP (FCA) was characterized using attenuated total reflection Fourier transform infrared spectroscopy, UV-Vis spectrometry, transmission electron microscope, and inductively coupled plasma mass spectrometry. The physical properties of FCA were also determined in solubility, drug encapsulation and in vitro drug release. Its anticancer activities were assessed in the 2D and 3D breast cancer models. The results showed that FCA was synthesized successfully with good solubility, high encapsulation efficiency and loading content. FCA showed the optimal cumulative release at pH 5.0 and high cellular uptake and exhibited significant inhibition on breast cancer cells. FCA also induced more significant apoptosis either in 2D and 3D breast cancer model than the celastrol AuNP and celastrol alone. These findings demonstrate that FCA improves water solubility of celastrol and enhances its anticancer activities against breast cancer. FCA might be a potential candidate of anticancer drug for breast cancer in the future if further development.
ISSN:2169-1401
2169-141X
DOI:10.1080/21691401.2020.1725025