Development and characterization of a novel drug nanocarrier for oral delivery, based on self-assembled β-casein micelles
Development and characterization of a novel drug nanocarrier for oral delivery, based on self-assembled β-casein micelles
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DOI：
10.1016/j.jconrel.2012.01.004
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发表时间：
2012-06-10
影响因子：
10.8
通讯作者：
Danino, Dganit
中科院分区：
文献类型：
--
作者：
Bachar, Michal;Mandelbaum, Amitai;Danino, Dganit
酪蛋白是一种两亲性蛋白，自组织形成明确的核-壳胶束。我们开发了这些胶束作为口服药物递送的有效纳米载体。我们的模型药物是塞来昔布，一种用于治疗类风湿关节炎和骨关节炎的抗炎疏水药物，现在也被评估为一种有效的抗癌药物。该系统的独特之处在于，它的包封负载比其他β -酪蛋白/药物配方高100倍，并且不需要像其他高负载配方那样添加添加剂。这与无需冷冻保护剂的冻干制剂的能力相结合，所得到的粉末具有长期的物理和化学稳定性，并且通过再水化可以完全可逆地重建结构。干剂型，其中>95%的药物被包封，满足日剂量。Cryo-TEM和DLS证明药物包封导致胶束膨胀，x射线衍射表明被包封的药物是无定形的。总之，我们的新剂型非常有利于口服给药。(C) 2012 Elsevier b.v.版权所有
beta-casein is an amphiphilic protein that self-organizes into well-defined core-shell micelles. We developed these micelles as efficient nanocarriers for oral drug delivery. Our model drug is celecoxib, an anti-inflammatory hydrophobic drug utilized for treatment of rheumatoid arthritis and osteoarthritis, now also evaluated as a potent anticancer drug. This system is unique as it enables encapsulation loads >100-fold higher than other beta-casein/drug formulations, and does not require additives as do other formulations that have high loadings. This is combined with the ability to lyophilize the formulation without a cryoprotectant, long-term physical and chemical stability of the resulting powder, and fully reversible reconstitution of the structures by rehydration. The dry dosage form, in which >95% of the drug is encapsulated, meets the daily dose. Cryo-TEM and DLS prove that drug encapsulation results in micelle swelling, and X-ray diffraction shows that the encapsulated drug is amorphous. Altogether, our novel dosage form is highly advantageous for oral administration. (C) 2012 Elsevier B. V. All rights reserved.