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Double-layered hyaluronic acid/stearic acid-modified polyethyleneimine nanoparticles encapsulating (-)-gossypol: a nanocarrier for chiral anticancer drugs
Liu, Hao Li, Ke Lan, Lan Ma, Jingwen Zeng, Yun Xu, Liang Daocheng, Wu
Liu, Hao
Li, Ke
Lan, Lan
Ma, Jingwen
Zeng, Yun
Xu, Liang
Daocheng, Wu
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Abstract
This study aimed to enhance the water solubility and antitumor efficacy of (-)-gossypol. Polyethyleneimine conjugated with stearic acid (PgS) was used for loading and protecting (-)-gossypol through hydrogen bonding. Double-layered hyaluronic acid (HA)-modified PgS nanoparticles encapsulating (-)-gossypol [(-)-G-PgSHAs] were prepared through a two-step fabrication process. The nanoparticles possessed a uniform spherical shape with a dynamic size of 110.9 ± 2.4 nm, which was determined through transmission electron microscopy and dynamic light scattering analysis. The encapsulation efficiency and drug-loading capacity of (-)-G-PgSHAs were 72.6% ± 3.1% and 9.1% ± 0.42%, respectively. The IR spectra of the samples confirmed the protection effect of hydrogen bonding on the optical activity of the encapsulated (-)-gossypol. (-)-G-PgSHAs exhibited a controlled and tumor-specific release because of the high expression of HAase in the tumor region. The tumor-targeting feature of PgSHAs due to HA-receptor mediation was confirmed by in vitro cell uptake and in vivo near infrared fluorescence imaging. The in vitro test showed that the (-)-G-PgSHAs had similar cytotoxicity to free (-)-gossypol and was smaller than that of the encapsulated (±)-gossypol [(±)-G-PgSHAs]. The in vivo study of the anti-cancer effect of (-)-G-PgSHAs revealed that (-)-G-PgSHAs had a more enhanced tumor-suppression effect and reduced systemic toxicity compared with free (-)-gossypol and (±)-G-PgSHAs (P < 0.05). Therefore, PgSHA was a useful (-)-gossypol nanocarrier that exhibits high biocompatibility, tunable release of drug, and tumor-targeting characteristics for cancer treatment. In addition, this double-layered nanocarrier provided novel strategies for the encapsulation of other chiral drugs.
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2014-08-28
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Royal Society of Chemistry
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Liu, Hao, Ke Li, Lan Lan, Jingwen Ma, Yun Zeng, Liang Xu, and Daocheng Wu. "Double-layered Hyaluronic Acid/stearic Acid-modified Polyethyleneimine Nanoparticles Encapsulating (-)-gossypol: A Nanocarrier for Chiral Anticancer Drugs." Journal of Materials Chemistry B 2.32 (2014): 5238.