Hu Jiangbo, Sun Lili, Zhao Dezhang, Zhang Liangke, Ye Mengliang, Tan Qunyou, Fang Chunshu, Wang Hong, Zhang Jingqing
Medicine Engineering Research Center, Chongqing Key Laboratory of Biochemical & Molecular Pharmacology, Chongqing Medical University, Chongqing, People's Republic of China.
Department of Health Statistics, College of Public Health, Chongqing Medical University, Chongqing, People's Republic of China.
Eur J Pharm Biopharm. 2014 Oct;88(2):556-64. doi: 10.1016/j.ejpb.2014.06.007. Epub 2014 Jun 22.
The purpose of this study was to develop and evaluate the supermolecular evodiamine (EVO) loaded water-in-oil nanoemulsions containing brucea javanica oil (NESEB) with enhanced physicochemical and biological characteristics. NESEB was fabricated by applying supermolecular phytosome nanotechnology and nanoemulsification technology together, in addition to using synergistic plant essential oil as a basic composition. Preferred physicochemical and biological characteristics of NESEB were investigated and compared with free EVO and other nanoemulsive EVO carriers. The possible explanations for improved absorption and bioavailability were put forward here. NESEB had high absorption and bioavailability, for example: the absorption rate constants and permeabilities of NESEB in different intestinal segments were 3.65-6.76 times that of free EVO; the relative bioavailability of NESEB to free EVO was 846.97%. NESEB markedly improved the oral bioavailability of EVO, which was most likely due to the increased gastrointestinal absorption. The development of nanoemulsion-based supermolecular EVO nanocarriers provides valuable tactics in insoluble natural antitumor drug delivering.
本研究的目的是开发并评估负载超分子吴茱萸碱(EVO)的含鸦胆子油的油包水纳米乳剂(NESEB),其具有增强的理化特性和生物学特性。NESEB是通过将超分子植物脂质体纳米技术和纳米乳化技术相结合制备而成的,此外还使用了协同增效的植物精油作为基本成分。对NESEB的优选理化特性和生物学特性进行了研究,并与游离EVO和其他纳米乳化EVO载体进行了比较。在此提出了吸收和生物利用度提高的可能解释。NESEB具有高吸收性和生物利用度,例如:NESEB在不同肠段的吸收速率常数和渗透率是游离EVO的3.65 - 6.76倍;NESEB相对于游离EVO的相对生物利用度为846.97%。NESEB显著提高了EVO的口服生物利用度,这很可能是由于胃肠道吸收增加所致。基于纳米乳剂的超分子EVO纳米载体的开发为难溶性天然抗肿瘤药物递送提供了有价值的策略。