Biomedical Engineering, The Ohio State University, Columbus, OH 43210, USA.
William G. Lowrie Department of Chemical and Biomolecular Engineering, The Ohio State University, Columbus, OH 43210, USA.
Int J Nanomedicine. 2020 Oct 23;15:8217-8230. doi: 10.2147/IJN.S259202. eCollection 2020.
Black raspberries (BRBs) and their anthocyanin-rich hydrophilic fractions (BRB-H) have exhibited significant chemopreventative activity across aerodigestive cancers. Lutein, the primary component of the BRB lipophilic fraction (BRB-L), also demonstrates bioactivity potential, but is less well characterized, in part because of its poor, innate bioavailability. For these lipophilic compounds to be accurately evaluated for anticancer efficacy, it is necessary to increase their functional bioavailability using delivery vehicles. Lutein has been delivered in commercial settings in emulsion form. However, emulsions are unstable, particularly in the gastrointestinal tract, which limit their use as an oral nutraceutical. Here, we evaluated lutein encapsulation and cellular uptake for nanoparticle (NP) delivery vehicles composed of three different materials synthesized via two different approaches.
Specifically, NPs were synthesized via smaller scale batch interfacial instability (II) sonication and semi-continuous high throughput electrohydrodynamic-mediated mixing nanoprecipitation (EM-NP) methods using polystyrene-polyethylene oxide (PSPEO) or polycaprolactone-polyethylene glycol (PCLPEG) block copolymers and PHOSPHOLIPON 90G (P90G, Lipoid GmbH) lipids. Size distribution, lutein encapsulation efficiency (EE), and cellular uptake and delivery were evaluated for each NP formulation.
NPs produced via high throughput EM-NP had higher EEs than NPs produced via batch II sonication, and P90G had the greatest EE (55%) and elicited faster cellular uptake in premalignant oral epithelial cells (SCC83) compared to other delivery systems.
These qualities suggest P90G could be a beneficial candidate for future lutein in vitro delivery research and clinical translation for oral cancer prevention.
黑覆盆子（BRB）及其富含花色苷的亲水性部分（BRB-H）在呼吸道和消化道癌症中表现出显著的化学预防活性。叶黄素是 BRB 亲脂部分（BRB-L）的主要成分，也具有生物活性潜力，但由于其先天生物利用度较差，其特征描述较少。为了准确评估这些亲脂化合物在抗癌功效方面的效果，有必要使用输送载体来增加其功能性生物利用度。叶黄素已在商业环境中以乳液形式提供。然而，乳液在胃肠道中不稳定，特别是在胃肠道中，这限制了它们作为口服营养保健品的使用。在这里，我们评估了三种不同材料的纳米粒子（NP）输送载体的叶黄素包封和细胞摄取，这些材料是通过两种不同方法合成的。
具体来说，使用聚苯乙烯-聚环氧乙烷（PSPEO）或聚己内酯-聚乙二醇（PCLPEG）嵌段共聚物和 PHOSPHOLIPON 90G（Lipoid GmbH）脂质，通过较小规模的批量界面不稳定性（II）超声和半连续高通量电动力介导混合纳米沉淀（EM-NP）方法合成 NPs。评估了每种 NP 制剂的粒径分布、叶黄素包封效率（EE）以及细胞摄取和递送。
通过高通量 EM-NP 生产的 NPs 的 EE 高于通过批量 II 超声生产的 NPs，并且 P90G 的 EE 最高（55%），并与其他输送系统相比，更快地在癌前口腔上皮细胞（SCC83）中摄取和递送到细胞内。
这些特性表明 P90G 可能是未来叶黄素体外输送研究和用于口腔癌预防的临床转化的有益候选物。
