Zhang Xingwang, Zhang Yong, Zhang Tianpeng, Zhang Jianping, Wu Baojian
Division of Pharmaceutics and.
J Microencapsul. 2015;32(5):496-502. doi: 10.3109/02652048.2015.1057251. Epub 2015 Jun 16.
Niclosamide (NL) has demonstrated its great potential in fighting against leukaemia recently. However, either oral or systemic delivery of NL is challenged by its insoluble nature. Here, we developed two different NL-loaded submicron lipid emulsions (NL-SLEs) and compared their suitability in bioavailability enhancement. Conventional and PEGylated NL-SLEs (NL-CSLEs and NL-PSLEs) were prepared by melt dispersion/high pressure homogenisation technique. They were about 307.8 and 162.2 nm in particle size, respectively, and both of them possessed satisfactory stability and drug load (>9.0%). After oral administration, significantly enhanced bioavailability was achieved through NL-CSLEs and NL-PSLEs (441.11 and 463.55% relative to the reference). Apart from global size, NL-CSLEs and NL-PSLEs exhibited similar attributes in release, lipolysis, mucin binding, etc. Taken together, SLEs with or without PEG-lipid have shown to be promising for oral delivery of NL. PEG-lipid could significantly reduce the particle size of SLEs. But, macromolecular PEG-lipid was required to effectively stealth the lipid carriers.
氯硝柳胺（NL）最近已显示出其在对抗白血病方面的巨大潜力。然而，NL的口服或全身给药都因其不溶性而受到挑战。在此，我们开发了两种不同的载氯硝柳胺亚微米脂质乳剂（NL-SLEs），并比较了它们在提高生物利用度方面的适用性。通过熔融分散/高压均质技术制备了常规和聚乙二醇化的NL-SLEs（NL-CSLEs和NL-PSLEs）。它们的粒径分别约为307.8和162.2 nm，并且都具有令人满意的稳定性和载药量（>9.0%）。口服给药后，通过NL-CSLEs和NL-PSLEs实现了显著提高的生物利用度（相对于参比制剂分别为441.11%和463.55%）。除了整体尺寸外，NL-CSLEs和NL-PSLEs在释放、脂解、粘蛋白结合等方面表现出相似的特性。综上所述，含或不含聚乙二醇脂质的SLEs已显示出在NL口服给药方面具有前景。聚乙二醇脂质可显著降低SLEs的粒径。但是，需要大分子聚乙二醇脂质来有效地使脂质载体隐形。
