Kim Dong-Myung, Lee Gee-Dong, Aum Seung-Hyun, Kim Ho-Jun
Nanofood Research Society, Seoul National University, Seoul, Korea.
Biol Pharm Bull. 2008 Sep;31(9):1704-10. doi: 10.1248/bpb.31.1704.
Propolis has well-known antimicrobial activity as well as antioxidant, antitumoral, anti-inflammatory, and regenerative properties, but its effects on the immune response are not well understood. Furthermore, clinical application of this relatively efficacious agent in cancer and other diseases has been limited due to poor aqueous solubility and, consequently, minimal systemic bioavailability. Nanoparticle-based delivery approaches have the potential to render hydrophobic agents like propolis dispersible in aqueous media, thus circumventing the pitfalls of poor solubility. We have synthesized a polymeric nanoparticle-encapsulated formulation of propolis (propolis nanofood) utilizing micellar aggregates of cross-linked and random copolymers of N-isopropylacrylamide (NIPAAM) with N-vinyl-2-pyrrolidone (VP) and poly(ethyleneglycol) monoacrylate (PEG-A). Physico-chemical characterization of the polymeric nanoparticles by dynamic laser light scattering and transmission electron microscopy confirms a narrow size distribution in the 50-nm range. Propolis nanofood, unlike free propolis, is readily dispersed in aqueous media. Propolis nanofood demonstrates comparable in vitro therapeutic efficacy to free propolis against a panel of human pancreatic cancer cell lines, as assessed by cell viability and clonogenicity assays in soft agar. Future studies utilizing propolis nanofood are warranted in pre-clinical in vivo models of cancer and other diseases that might benefit from the effects of propolis.
蜂胶具有众所周知的抗菌活性以及抗氧化、抗肿瘤、抗炎和再生特性,但其对免疫反应的影响尚不清楚。此外,由于水溶性差,因此全身生物利用度极低,这种相对有效的药物在癌症和其他疾病中的临床应用受到限制。基于纳米颗粒的递送方法有可能使蜂胶等疏水性药物分散在水性介质中,从而避免溶解性差的问题。我们利用N-异丙基丙烯酰胺(NIPAAM)与N-乙烯基-2-吡咯烷酮(VP)和聚乙二醇单丙烯酸酯(PEG-A)的交联共聚物和无规共聚物的胶束聚集体,合成了一种聚合物纳米颗粒包裹的蜂胶制剂(蜂胶纳米食品)。通过动态激光散射和透射电子显微镜对聚合物纳米颗粒进行的物理化学表征证实,其粒径分布在50纳米范围内,且分布狭窄。与游离蜂胶不同,蜂胶纳米食品很容易分散在水性介质中。通过软琼脂中的细胞活力和克隆形成试验评估,蜂胶纳米食品对一组人胰腺癌细胞系的体外治疗效果与游离蜂胶相当。在癌症和其他可能受益于蜂胶作用的疾病的临床前体内模型中,有必要对蜂胶纳米食品进行进一步研究。