巻号一覧
36 巻 (2011)
- 6 号 p. 271-
- 5 号 p. 203-
- 4 号 p. 128-
- 3 号 p. 83-
- 2 号 p. 49-
- 1 号 p. 1-
36 巻, 4 号
選択された号の論文の10件中1～10を表示しています
- |<
- <
- 1
- >
- >|
巻頭言
特集：第33年回 生体膜特別公演
総説
-
金井 好克2011 年 36 巻 4 号 p. 128-138
発行日: 2011年
公開日: 2011/12/13
ジャーナル オープンアクセスTransporters are responsible for the selective permeability of organic and inorganic solutes through the bio-membrane and contribute to determine the distribution of compounds in the body in concert with metabolic/synthetic enzymes. The drugs affecting transporters are, thus, expected to alter the distribution of compounds in the body and to restore homeostasis in the disease conditions. Additionally, transporters contribute to pharmacokinetics by mediating permeation of drugs and their metabolites. Molecular biological approaches revealed molecular nature of transporters and greatly advanced the research field. Now the directions of the transporter researches have been shifted to the understanding of structural bases of the transport functions, to the revealing of functional units of membrane transport and to the understanding of in vivo function of transporter molecules. The knowledge of the functional units of membrane transport is essential to link the function of transporter molecules revealed by molecular cloning to the physiological functions of cells and homeostasis. The idea of “transportsome” would contribute to it抄録全体を表示PDF形式でダウンロード (830K)
特集：生体膜関連シンポジウム「高分子と生体膜の相互作用を利用した新たな治療戦略」
総説
-
二木 史朗2011 年 36 巻 4 号 p. 139-144
発行日: 2011年
公開日: 2011/12/13
ジャーナル オープンアクセスOne of the great obstacles in developing therapeutic agents based on biomacromolecules, including peptides, proteins, and nucleic acids, should be their low membrane permeability due to their high hydrophilicity and large molecular sizes. On the other hand, there is a growing research interest in intracellular delivery of biomacromolecules using arginine-rich cell-penetrating peptides (CPPs). Chemical conjugation of bioactive macromolecules with these CPPs allows efficient translocation of these molecules into cells. Successful intracellular delivery of various nano-particles using CPPs have also been reported. Involvement of macropinocytosis has been reported as an internalization mechanism of arginine-rich CPPs. Accumulation of arginine-rich CPPs and their conjugates on cell surfaces by the interaction of membrane associated proteoglycans and the eventual induction of macropinocytosis can be a rationale to explain the high efficacy of the intracellular delivery.抄録全体を表示PDF形式でダウンロード (699K) -
高野 幹久, 湯元 良子2011 年 36 巻 4 号 p. 145-153
発行日: 2011年
公開日: 2011/12/13
ジャーナル オープンアクセスThe lung is expected as a promising administration route for protein and peptide drugs. However, information concerning alveolar absorption mechanisms of these high molecular weight drugs is lacking. The alveolar region of the lung is lined with a continuous epithelium comprising of type I and type II epithelial cells, and squamous type I cells cover 90~95% and cuboidal type II cells cover 5~10% of the alveolar surface area. Using primary cultured alveolar type II and transdifferentiated type I cells, however, it was found that type II cells would play a significant role in albumin and insulin endocytosis from the alveolar space. Functional and siRNA studies suggest that albumin is taken up by clathrin-mediated endocytosis in type II cells, while clathrin- and caveolae-independent but dynamin-dependent pathway is involved in insulin endocytosis. The approach to enhance insulin uptake by the alveolar epithelial cells and absorption from the lung is also discussed.抄録全体を表示PDF形式でダウンロード (966K) -
米谷 芳枝2011 年 36 巻 4 号 p. 154-162
発行日: 2011年
公開日: 2011/12/13
ジャーナル オープンアクセスCurrently, lipid-based particles are mostly used for controlled release of drugs and drug targeting. The introduction of polyethylene glycol (PEG) derivative to lipids, i.e. “PEGylated” makes long-circulating liposomes in blood. Furthermore, PEGylation has emerged as a platform for incorporation of active targeting ligands, providing the drug and gene carriers with specific targeting properties through a flexible tether. This review focuses on the developments surrounding such functional PEGylation of lipid-based particles to promote tissues and cell-targeting, thereby enhancing efficacy of therapeutic strategies.抄録全体を表示PDF形式でダウンロード (1737K) -
玉井 郁巳2011 年 36 巻 4 号 p. 163-170
発行日: 2011年
公開日: 2011/12/13
ジャーナル オープンアクセスSince membrane transporters efficiently facillitate intestinal absorption of nutrients, it should be possible to utilyze those transporters to improve permeability of drugs/drug candidates. In the present study, oligopeptide transporter PEPT1, which accepts various di- and tri-peptides as substrates and transports them using proton gradient as the driving force, was examined as the tools for oral drug delivery of peptide-mimetic compounds. Since substrates of PEPT1 exhibits varible optimal pH depending on substrates, acidic polymer Eudragit L100-55 (EL) was employed to control intestinal luminal pH to be optimal for low permerble PEPT1 substrate, β-lactam antibiotic cefiximie which exhibits optimal transport by PEPT1 at pH 5 or lower, as model compound. Intestinal absorption of cefixime was studied in rats by in situ ileal closed loops and by in vivo oral administration of the drugs concomitantly with EL. EL decreased the pH in the intestinal lumen, and increased the absorption in both the in situ closed loop and in vivo oral administration studies. Furthermore, the increased absorption of cefixime caused by EL was reduced by simultaneous administration of cefadroxil, a PEPT1 substrate/inhibitor, in a dose-dependent manner. Accordingly, an improvement of intestinal absorption of peptide-mimetics via PEPT1 is possible by optimizing the transporter activity through coadministration of a proton-releasing polymer which supplies the driving force for the transporter.抄録全体を表示PDF形式でダウンロード (1157K)
特集：境界領域シンポジウム「ナノ粒子表面物性に基づいたDDS開発」
総説
-
小暮 健太朗, 濱 進2011 年 36 巻 4 号 p. 171-176
発行日: 2011年
公開日: 2011/12/13
ジャーナル オープンアクセスFor achievement of efficient antitumor therapy, we developed novel DDS nano-carriers, which have specific surface properties suitable for in vivo delivery to tumor. In order to avoid interaction with biological components, such as serum protein and reticuloendothelial system, we focused attention on the carriers having negatively charged surface. At first, we constructed negatively charged DDS carrier by tocopheryl succinate (TS), which is known as an anti-tumor vitamin E derivative. The DDS carrier consisting of TS showed potent anti-tumor activity. However, cellular uptake was not enough because of its negatively charged surface. Then, we constructed a novel DDS nano-carrier, which can change surface charge dependent on environmental pH. The novel pH sensitive DDS nano-carrier showed pH-dependent cellular uptake and functionality. Moreover, the nano-carrier accumulated in the tumor like PEG-liposome, although the carrier has no PEG modification to maintain blood circulation time. Consequently, we developed novel DDS nano-carriers having surface functionality responsive to environment in tumor.抄録全体を表示PDF形式でダウンロード (873K) -
早川 栄治2011 年 36 巻 4 号 p. 177-182
発行日: 2011年
公開日: 2011/12/13
ジャーナル オープンアクセスSoftgel capsules consist of a gelatin based shell or vegetable origin materials such as starch and carrageenan. They can be filled with liquids or pastes. Dynamic nature of the soft capsules affected by atmospheric condition or filled liquid is considered in view of the surface interaction.抄録全体を表示PDF形式でダウンロード (877K) -
河野 健司, 弓場 英司2011 年 36 巻 4 号 p. 183-190
発行日: 2011年
公開日: 2011/12/13
ジャーナル オープンアクセスFor establishment of safe and effective therapy, carriers that achieve high-precision drug delivery are required. Liposomes are one of the most promising drug delivery systems. To increase usefulness of liposomes as drug delivery systems, we have attempted to provide various functions to liposomes via surface surface modification of liposomes with functional polymers. Functions of polymer-modified liposomes were based on their interactions. Therefore, surface-modification of liposomes with temperature-sensitive polymers can give temperature-responsive liposomes whose drug release is triggered by mild heating. Also, surface modification of liposomes with pH-sensitive polymers can generate pH-responsive liposomes whose destabilization is induced in weakly acidic environments. In addition, modification with several kinds of polymers with different functions can generate multifunctional liposomes. Here, we describe design, preparation and performance of functional liposomes based on the surface modification with functional polymers, such as temperature-sensitive, pH-sensitive, magnetic resonance-detectable polymers for the production of liposomes for high-precision site-specific delivery and/or intracellular delivery of bioactive molecules.抄録全体を表示PDF形式でダウンロード (1051K) -
澤田 晋一, 秋吉 一成2011 年 36 巻 4 号 p. 191-196
発行日: 2011年
公開日: 2011/12/13
ジャーナル オープンアクセスNanosize hydrogels (nanogels) are polymer nanoparticles with three-dimensional networks formed by chemical and/or physical cross-linking of polymer chains. We reported for the first time physically cross-linked nanogels by self-assembly of amphiphilic polysaccharides in water. Biomedical applications of nanogels have made rapid progress in the last 10 years. A current challenge is the development of strategies for the delivery of more fragile drugs such as proteins which are easily unfolded or inactivated under physiological conditions. To overcome this issue, the chaperone-like function of the polysaccharide nanogels is an important concept that can lead to breakthroughs in the effective delivery of proteins. Here, we report recent progress in polysaccharide nanogel engineering for protein delivery.抄録全体を表示PDF形式でダウンロード (2164K)
製品＆技術
-
綿部 智一, 中塚 修志2011 年 36 巻 4 号 p. 197-200
発行日: 2011年
公開日: 2011/12/13
ジャーナル オープンアクセスE mizu shower is a new energy saving system for the outdoor compressor units of air conditioners and refrigerators. By spraying misty RO permeate water onto the aluminum radiation fins, it reduces temperature on aluminum fins and electric use, due to the effect of the heat vaporization. Spraying tap water or ordinal water onto aluminum fins causes scales and corrosion of the aluminums. Scales on the fins decreases the heat exchange rate and reduces the efficiency of outdoor compressor units. Using RO permeate water which is removed ionic components (calcium, chlorine, silica) in water by an RO membrane prevents scales and corrosion of the aluminum fins by filtering ordinal water into purified water.抄録全体を表示PDF形式でダウンロード (894K)
編集後記
- |<
- <
- 1
- >
- >|