Beta-casein nanovehicles for oral delivery of chemotherapeutic drugs
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- 作者：Alina Shapira ; Yehuda G. Assaraf ; Yoav D. Livney
- 关键词：β ; -Casein micelles ; Cancer ; Mitoxantrone ; Nanoparticles ; Oral delivery
- 刊名：Nanomedicine: Nanotechnology, Biology and Medicine
- 出版年：2010
- 出版时间：February 2010
- 年：2010
- 卷：6
- 期：1
- 页码：119-126
- 全文大小：609 K
文摘
Bovine β-casein (β-CN) is an abundant milk protein that is highly amphiphilic and self-assembles into stable micellar structures in aqueous solutions. Here we introduce a drug-delivery system comprising a model hydrophobic anticancer drug, mitoxantrone (MX), entrapped within β-CN–based nanoparticles. This novel drug-delivery system allows hydrophobic drugs to be thermodynamically stable in aqueous solutions for oral-delivery applications aimed at treatment of various disorders. The gastric digestibility of β-CN suggests possible targeting to stomach tumors. Dimethyl sulfoxide (DMSO)-dissolved MX was entrapped in β-CN nanoparticles by stirring this solution into phosphate-buffered β-CN solution. High-affinity MX–β-CN association was found (Ka = [2.15 ± 0.30] × 106 M-1). The optimal nanovehicle formation conditions were 1 mg/mL β-CN, ≤6 % (vol/vol) DMSO in phosphate-buffer solution, 10 mM MX in DMSO, and a MX:β-CN molar-ratio of 4:1. Under these conditions, particles of 100 to 300-nm diameter were formed. β-CN nanoparticles may serve as effective oral-delivery nanovehicles for solubilization and stabilization of hydrophobic drugs.
From the Clinical Editor
Bovine β-casein (β-CN) is an abundant milk-protein that is highly amphiphilic and self-assembles into stable micellar-structures in aqueous solutions. β-CN nanoparticles may serve as effective oral-delivery nanovehicles for solubilization and stabilization of hydrophobic drugs, as demonstrated in this study utilizing methotrexate.