Nanoparticles composed of anionic phospholipid of 1,2- dipalmitoyl- sn-glycero-3-phosphorylglycerol (DPPG), “anionic bicelles”, or Technol phosphatidylglycerol (Technol PG), “anionic liposomes”, and docetaxel were prepared by mixing them in water with cholic acid-based surfactants of SC through a subsequent heating/cooling/ultrasonicating process. Ultrasonic fragmentation at low temperature of 4°C prepared small-sized anionic DPPG nanoparticles (“anionic bicelles”) (particle size: 15 nm) and small-sized anionic Technol PG nanoparticles (“anionic liposomes”) (particle size: 5 nm). Through transdermal addition (in vitro) to rat skin tissue, resveratrol-anionic DPPG nanoparticles, “anionic bicelles” (size: 15 nm), infiltrated into the epidermis layer penetrating stratum corneum (intercellular space: ca. 100 nm). Docetaxel-anionic DPPG nanoparticles or docetaxel-anionic Technol PG nanoparticles showed high anti-cancer activity toward skin cancer A431 cells, SCL ? cells, and KB cells in in vitro anti-skin cancer test. Additionally, during the in vivo anti-skin cancer test (anti-skin tumor test) using mouse model of skin cancer, our study revealed that the numbers of papillomas of the mouse applied with docetaxel-anionic DPPG nanoparticles, “anionic bicelles”, or docetaxel-anionic Technol PG nanoparticles, “anionic liposomes”, to mouse skin decreased, although those of the mouse applied with docetaxel itself to mouse skin (control) increased. These findings showed that docetaxel-anionic DPPG nanoparticles or docetaxel-anionic Technol PG nanoparticles could permeate stratum corneum and be incorporated into the epidermis layer of mouse, treating skin cancer. On the other hand, glycosylation of galantamine (reminyl) and pergolide mesilate (permax) was achieved by using enzymes as biocatalysts. Galantamine (reminyl) gluco-oligosaccharides and pergolide mesilate (permax) gluco-oligosaccharides showed high neuroprotective activity with enhancement of survival of TH-positive neurons in rat primary midbrain cultures in in vitro anti-dementia test. Galantamine (reminyl) gluco-oligosaccharides and pergolide mesilate (permax) gluco-oligosaccharides showed high in vitro neuroprotective activity toward Aβ treated rat hippocampal neurons. Galantamine (reminyl) gluco-oligosaccharides and pergolide mesilate (permax) gluco-oligosaccharides, which were intraperitoneally or orally injected to a mouse, could penetrate the blood-brain barrier (BBB) of mouse brain and be incorporated into the mouse’s brain tissue (in vivo). Galantamine (reminyl) gluco-oligosaccharides enhanced spatial learning of mice in in vivo Y-maze test and in vivo novel object recognition test. Pergolide mesilate (permax) gluco-oligosaccharides, which were intraperitoneally or orally injected to 6-OHDA-induced hemi-parkinsonism mice, decreased the number of ipsilateral turns of mice (in vivo) and activated contralateral hind limb steps (in vivo), indicating that pergolide mesilate (permax) gluco-oligosaccharides could treat the Parkinson's disease (PD) improving the parkinsonian signs. In addition, maltoside of α-tocopherol showed high anti-allergic activity toward wheat-allergen, gliadin and glutenin. Maltoside of daidzein and genistein also had strong anti-allergic activity against soybean-allergen, globulin.

Download this article as