Ge Ruiliang, Ji Yuexin, Ding Yanfei, Huang Chang, He Hua, Yu Deng-Guang
Department of Outpatient, The Third Affiliated Hospital, Naval Medical University, Shanghai, China.
School of Materials and Chemistry, University of Shanghai for Science and Technology, Shanghai, China.
Front Bioeng Biotechnol. 2023 Jan 19;11:1112338. doi: 10.3389/fbioe.2023.1112338. eCollection 2023.
The poor solubility of numerous drugs pose a long-existing challenge to the researchers in the fields of pharmaceutics, bioengineering and biotechnology. Many "top-down" and "bottom-up" nano fabrication methods have been exploited to provide solutions for this issue. In this study, a combination strategy of top-down process (electrospinning) and bottom-up (self-emulsifying) was demonstrated to be useful for enhancing the dissolution of a typical poorly water-soluble anticancer model drug (paclitaxel, PTX). With polyvinylpyrrolidone (PVP K90) as the filament-forming matrix and drug carrier, polyoxyethylene castor oil (PCO) as emulsifier, and triglyceride (TG) as oil phase, Both a single-fluid blending process and a coaxial process were utilized to prepare medicated nanofibers. Scanning electron microscope and transmission electron microscope (TEM) results clearly demonstrated the morphology and inner structures of the nanofibers. The lipid nanoparticles of emulsions after self-emulsification were also assessed through TEM. The encapsulation efficiency (EE) and dissolution tests demonstrated that the cores-shell nanofibers could provide a better self-emulsifying process int terms of a higher EE and a better drug sustained release profile. Meanwhile, an increase of sheath fluid rate could benefit an even better results, suggesting a clear process-property-performance relationship. The protocols reported here pave anew way for effective oral delivery of poorly water-soluble drug.
许多药物的低溶解度长期以来一直给制药、生物工程和生物技术领域的研究人员带来挑战。人们已经采用了许多“自上而下”和“自下而上”的纳米制造方法来解决这个问题。在本研究中,一种将自上而下的方法(静电纺丝)和自下而上的方法(自乳化)相结合的策略被证明有助于提高一种典型的难溶性抗癌模型药物(紫杉醇,PTX)的溶出度。以聚乙烯吡咯烷酮(PVP K90)作为成丝基质和药物载体,聚氧乙烯蓖麻油(PCO)作为乳化剂,甘油三酯(TG)作为油相,采用单流体共混工艺和同轴工艺制备含药纳米纤维。扫描电子显微镜和透射电子显微镜(TEM)结果清楚地显示了纳米纤维的形态和内部结构。自乳化后乳液的脂质纳米颗粒也通过TEM进行了评估。包封率(EE)和溶出度测试表明,核壳纳米纤维在更高的EE和更好的药物缓释曲线方面可以提供更好的自乳化过程。同时,鞘液流速的增加有利于获得更好的结果,表明存在明确的工艺-性质-性能关系。本文报道的方案为难溶性药物的有效口服给药开辟了一条新途径。