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天然黑色素:一种潜在的 pH 响应型药物释放装置。

Natural melanin: a potential pH-responsive drug release device.

机构信息

REQUIMTE, Departamento de Química, Faculdade de Ciências e Tecnologia, FCT, Universidade Nova de Lisboa, 2829-516 Caparica, Portugal.

CICS-UBI - Centro de Investigação em Ciências da Saúde, Universidade da Beira Interior, Avenida Infante Dom Henrique, 6200-506 Covilhã, Portugal.

出版信息

Int J Pharm. 2014 Jul 20;469(1):140-5. doi: 10.1016/j.ijpharm.2014.04.051. Epub 2014 Apr 23.

Abstract

This work proposes melanin as a new nanocarrier for pH-responsive drug release. Melanin is an abundant natural polymer that can be easily extracted from cuttlefish as nanoparticles with a suitable size range for drug delivery. However, despite its high potentiality, the application of this biopolymer in the pharmaceutical and biomedical fields is yet to be explored. Herein, melanin nanoparticles were impregnated with metronidazole, chosen as model antibiotic drug, using supercritical carbon dioxide. The drug release profile was investigated at acidic and physiologic pH, and the dominant mechanism was found to follow a non-Fickian transport. Drug release from melanin shows a strong pH dependency, which allied to its biocompatibility and lack of cytotoxicity envisages its potential application as nanocarrier in formulations for colon and intestine targeted drug delivery.

摘要

这项工作提出了黑色素作为一种新的纳米载体用于 pH 响应药物释放。黑色素是一种丰富的天然聚合物,可从乌贼中轻松提取出具有适合药物输送的合适粒径范围的纳米颗粒。然而,尽管其潜力巨大,但这种生物聚合物在制药和生物医学领域的应用尚未得到探索。在此,使用超临界二氧化碳将米诺环素(选择为模型抗生素药物)浸渍到黑色素纳米颗粒中。在酸性和生理 pH 下研究了药物释放曲线,发现主要的释放机制遵循非菲克扩散。黑色素的药物释放具有很强的 pH 依赖性,再加上其生物相容性和无细胞毒性,预计其可作为纳米载体应用于结肠和肠道靶向药物输送的制剂中。

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