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김민정,도희정,조원제,용철순,최한곤,이치호,김대덕 한국약제학회 2002 Journal of Pharmaceutical Investigation Vol.32 No.4
Rat skin permeation of various nonsteroidal antiinflammatory drugs (NSAIDs) was investigated in vitro using Franz diffusion cell at 37℃. The effect of various skin permeation enhancers was also observed as a preliminary study of developing transdermal delivery systems of NSAIDs. Lipophilicity of NSAIDs was determined from the partition coefficient (log P) in 1-octanol/water and 1-octanol/IPB mutual-saturated solutions. The solubility was determined in water, isotonic phosphate buffer (IPB), and propylene glycol (PG) at 37℃. The rat skin permeation rate of acetaminophen, piroxicam, and aceclofenac was almost negligible, although they were saturated in PG. Addition of 1 % permeation enhancer increased the permeation rate of ketoprofen, ketorolac, and diclofenac. However, the skin permeation rate of ibuprofen did not increase with the addition of various enhancers. Among the permeation enhancers tested, oleic acid was the most effective for various NSAIDs. Based on the daily dose, lipophilicity, and the skin permeation rate achieved in this study, ketoprofen and ketorolac seem to be the most promising drug candidates for transdermal delivery systems, especially when formulated with unsaturated fatty acids, such as oleic acid.
Characterization of Nanoparticles Prepared by poly(ethylene glycol)-block-poly(ε-caprolactone)
Kim, Tai-Hyoung,Chae, Su Young,Choi, Changyong,Chae, Hey Young,Kim, Dong-Gon,Kwon, Joong-Keun,Nah, Jea-Woon 한국공업화학회 2004 응용화학 Vol.8 No.1
Amphiphilic diblock copolymer with different poly(ε-caprolactone) (PCL) block length were synthesized by ring-opening polymerization of ε-caprolactone in the presence of monomethoxy poly(ethylene glycol) (mPEG-OH, MW 2000) as initiator, using stannous octoate catalyst. The self-aggregation behavior and microscopic characteristics of the diblock copolymer self-aggregation behavior and microscopic characteristics of the diblock copolymer self-aggregates, prepared by dialysis method, were investigated by ¹H NMR, dynamic light scattering (DLS), fluorescence spectroscopy. The PEG-PCL block copolymer formed self-aggregates in an aqueous environment by intra- and/or intermolecular association between hydrophobic PCL chains. The microscopic chacaterization of the PEGCL self-aggregates revealed that the hydrophobic/hydrophilic balance, resulting from different PCL block length, played a crueial roles fo ditermination of the physicochemical properties of them.
Pramipexole protects dopaminergic neurons through paraplegin against 6-hydroxydopamine
Kim, Mun ki,Park, Hyeon soo,Cho, Jea hyeon,Kim, Gon sup,Won, Chungkil Wolters Kluwer Health | Lippincott Williams Wilkin 2015 NEUROREPORT - Vol.26 No.2
The neurotransmitter dopamine (DA) regulates various physiological and psychological functions, such as movement, motivation, behavior, and learning. DA exerts its function through DA receptors and a series of studies have reported the role of DAergic receptors in preventing DAergic neuronal degeneration. Here, we studied the DA receptor-mediated neuroprotective effect of the D2-like receptor agonists against 6-hydroxydopamine (6-OHDA)-induced DAergic neurodegeneration. D2-like receptor agonists were administered in the substantia nigra in vivo and to primary cultured neurons. Treatment of 6-OHDA decreased tyrosine hydroxylase (TH) and paraplegin (mitochondrial regulation protein) immunoreactivity, whereas pretreatment with quinpirole (a full D2-like receptor agonist) preserved TH and paraplegin reactivity. This led us to test which DA receptors were necessary for the neuroprotective effect and whether paraplegin can be regulated by D2 or D3 receptor agonists. Pretreatment with the D2 receptor selective agonist, sumanirole, did not preserve TH and paraplegin reactivity from 6-OHDA. However, the D3 receptor agonist, pramipexole, protected TH reactivity and restored paraplegin expression to the control level in the presence of 6-OHDA. Interestingly, pretreatment with the D3 receptor antagonist GR103691 reduced TH and paraplegin expression levels. These results suggest that the D3 receptor agonist may protect DA neurons from the effect of 6-OHDA through the modulation of the mitochondrial regulation protein paraplegin.
Park, Jea-Gun,Nam, Woo-Sik,Seo, Sung-Ho,Kim, Yool-Guk,Oh, Young-Hwan,Lee, Gon-Sub,Paik, Un-Gyu American Chemical Society 2009 NANO LETTERS Vol.9 No.4
<P>Four-level nonvolatile small-molecule 4F(2) memory cells were developed with a sandwiched device structure consisting of an upper Al electrode, upper small-molecule layer (Alq(3), aluminum tris(8-hydroxyquinoline)), Ni nanocrystals surrounded by NiO tunneling barrier, lower small-molecule layer, and bottom Al electrode. In particular, an in situ O(2)-plasma oxidation process following Ni evaporation was developed to produce uniformly stable 10 nm Ni nanocrystals surrounded by a NiO tunneling barrier embedded in the small-molecule layer. They presented a memory margin (I(on)/I(off) ratio) of approximately 1 x 10(3), a retention time of more than 10(5) s, an endurance of more than 5 x 10(2) erase-and-program cycles, and multilevel cell (MLC) operation, being a terabit nonvolatile memory-cell. A vertically double-stacked 4F(2) multilevel nonvolatile memory cell was also developed, showing a memory margin of approximately 1 x 10(3) in both the top and bottom memory cells and eight-level cell operation.</P>