Nanoassemblies Based on Supramolecular Complexes of Nonionic Amphiphilic Cyclodextrin and Sorafenib as Effective Weapons to Kill Human HCC Cells
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- 作者：Maria Luisa Bond矛 ; Angela Scala ; Giuseppe Sortino ; Erika Amore ; Chiara Botto ; Antonina Azzolina ; Daniele Balasus ; Melchiorre Cervello ; Antonino Mazzaglia
- 刊名：Biomacromolecules
- 出版年：2015
- 出版时间：December 14, 2015
- 年：2015
- 卷：16
- 期：12
- 页码：3784-3791
- 全文大小：516K
- ISSN：1526-4602
文摘
Sorafenib (Sor), an effective chemiotherapeutic drug utilized against hepatocellular carcinoma (HCC), robustly interacts with nonionic amphiphilic cyclodextrin (aCD, SC6OH), forming, in aqueous solution, supramolecular complexes that behave as building blocks of highly water-dispersible colloidal nanoassemblies. SC6OH/Sor complex has been characterized by complementary spectroscopic techniques, such as UV鈥搗is, steady-state fluorescence and anisotropy, resonance light scattering and 1H NMR. The spectroscopic evidences and experiments carried out in the presence of an adamantane derivative, which competes with drug for CD cavity, agree with the entrapment of Sor in aCD, pointing out the role of the aCD cavity in the interaction between drug and amphiphile. Nanoassemblies based on SC6OH/Sor display size of 鈭?00 nm, negative zeta-potential (味 = 鈭?1 mV), and both maximum loading capacity (LC 鈭?17%) and entrapment efficiency (EE 鈭?100%). Kinetic release profiles show a slower release of Sor from nanoassemblies with respect to the free drug. SC6OH/Sor nanoassemblies have very low hemolytic activity and high efficiency in vitro in decreasing cell growth and viability of HCC cell lines, such as HepG2, Hep3B, and PLC/PRF/5, opening promising chances to their in vivo applications.