β-casein–based nanovehicles for oral delivery of chemotherapeutic drugs: drug-protein interactions and mitoxantrone loading capacity

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• 作者：Alina Shapira ; Gilad Markman ; Yehuda G. Assaraf ; Yoav D. Livney
• 关键词：β ; -casein micelles ; Nanoparticles ; Oral delivery ; Cancer ; Mitoxantrone
• 刊名：Nanomedicine: Nanotechnology, Biology and Medicine
• 出版年：2010
• 出版时间：August 2010
• 年：2010
• 卷：6
• 期：4
• 页码：547-555
• 全文大小：309 K

文摘

β-casein (β-CN), a major milk protein, is amphiphilic and self-associates into micelles in aqueous solutions. We have recently introduced a novel oral drug delivery system based on β-CN nanoparticles. The current research builds on and complements this work by studying the interactions of mitoxantrone (MX) and β-CN as they co-assemble into nanoparticles, using absorption and emission spectra, static and dynamic light scattering, and fluorescent emission of both MX and tryptophan 143 (Trp143) of β-CN. The optimal loading molar ratio was 3.3 MX/β-CN at 1 mg/mL β-CN, and the association constant was (2.45 ± 1.76) × 10⁵ M^–1 based on β-CN Trp143 fluorescence; independent MX fluorescence results provided supporting values. In these conditions a bimodal particle distribution was obtained (174.4 nm, 45.9 % ; 485.1 nm, 54.1 % ). The gastric digestibility of β-CN suggests possible targeting to stomach tumors. Hence, β-CN nanoparticles have potential to serve as effective vehicles of hydrophobic drugs for oral delivery preparations.

From the Clinical Editor

Beta-casein (b-CN) is an amphiphilic milk protein that self-associates into micelles in aqueous solutions and can be utilized as a novel oral drug delivery system. This study investigates the basic properties of a mitoxantrone delivery system based on the above principles.