Hiraku Onishi

..From these results, it is expected that GC-SP will be accumulated at inflammatory sites based on enhanced permeability and retention (EPR) effects, and release PD there effectively...

..These characteristics on particle size and in vitro release suggested that Ch-SP-MS should have good potential as a microparticulate system for the treatment of IBD...

..It was demonstrated that the patch with OA showed a good adhesion to oral mucosa and worked efficiently for rapid absorption of DZ...

..After i.v. injection in rats, NP maintained irinotecan plasma concentration longer than CPT-11 aqueous solution. The present nanoparticle formation is suggested as a possibly useful dosage form of irinotecan against solid tumor...

..Considering the mucoadhesive properties of chitosan microparticles, Ch-LF(N) are suggested to be useful for gradual supply to topical diseased sites or for effective delivery to intestinal areas with abundant LF receptors...

..2, and gradually released Ch-SP-MS at pH 6.8 and 7.4 due to dissolution of the Eudragit layer. Eudragit coating is suggested to be useful to efficiently deliver Ch-SP-MS to the intestinal disease sites...

..These delivery systems are expected to improve the utility of LF...

..45 microm (Suc-MP-MMC) were derived by the addition of EDC before emulsification. Suc-MP-MMC exhibited a higher drug content than CML-MP-MMC. CML-MP-MMC and Suc-MP-MMC exhibited 50% drug release times of 2.87h and 42.1 h, respectively...

..As the implant displayed the discrepancy between in vitro and in vivo release rates, the improvement of the in vivo release rate is required...

..Therefore, it is important to develop a system delivering LF efficiently to intestinal mucosa or gut-associated lymphoid tissue...

..It was demonstrated that Ch-SP-MS/EuL enhanced effectiveness of PD and reduced toxic side effects of PD greatly. Also, these results established the prediction by previous in vitro and in vivo studies...

..It is proposed that the semisolid dosage form CZP1-PEG-OA should be a possibly useful preparation for the antiepileptic or sedative medication...

..In this review, several micro- or nanoparticles composed of macromolecule-drug conjugates are described for their preparation, in vitro properties and/or in vivo behavior...

..Ch-SP-MS/EuL are suggested as a useful delivery system to the site of inflammatory bowel disease...

..8, though swelling and softening of the microparticles occurred at pH 6.8. It is suggested that alginate/calcium complex microparticles coated with 0.25-0.5% (w/v) chitosan solution would be useful for the intestinal delivery of LF...

..As compared with CPT solution, CPT-NP showed higher tissue accumulation and better tumor localization, which were considered essentially associated with the better efficacy of CPT-NP reported in the previous study...

..The PLA/PEG-PPG-PEG nanoparticles were considered potentially useful to enhance the efficacy of CPT, to which the high drug retention in the body and gradual drug release appeared to be importantly related...

..Thus, granules and tablet are useful as a compact dosage form of MC; though the reduced adsorption capacity must be taken into account in order to expect efficacy equivalent to that of MC alone...

..It is suggested that PLA-pyrene might be a useful probe of the nanoparticles themselves. In addition, it was demonstrated that PLA-(MeO-PEG) nanoparticles should be a useful drug carrier for passive tumor targeting...

..It was demonstrated that the present direct compression using homogeneous FS/S1670/MC powder mixture could give an excellent fast-disintegrating tablet of FS...

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..FU ODTs with improved taste, rapid disintegration and greater hardness could be prepared with YO-containing granules made by the wet granulation method using MA as a binding agent...

..Therefore, in the present study, it was attempted to develop an easily-handled dosage form, which was more physically stable and allowed rapid drug absorption from oral mucosa...

..Thus, the Witocan H tablet with Sc1-B5 is suggested as the best acetaminophen chewable tablet, exhibiting suppressed bitterness, low sweetness, improved oral feeling and good drug release...

..Furthermore, a possibility that the B-LF release could be controlled by adjusting the Ca(2+) concentration in Ca-PC was suggested...

..The present implant tablet is suggested to be useful as a drug delivery system for supplying drugs for approximately 1 week...

..Our findings suggest that the combination of PG and MEN was useful as enhancers for the transdermal absorption of PF. These results provide useful information to develop a transdermal dosage form of PF as a sedative or a hypnotic...

..In these systems, one of the most important concepts is the enhanced permeability and retention (EPR) effect. The outcomes obtained by these approaches are displayed by introducing concrete examples...

..Similar adsorption characteristics were also observed in a real drug, acetaminophen. It is suggested that the MC tablets prepared by the wet granule compression using MT as a binder should be useful as a compact dosage form of MC...

..After i.v. administration to the tumor-bearing mice, CPT-NP showed better plasma retention, and high and long tumor localization. CPT-NP are suggested to greatly improve the efficacy of CPT due to their pharmacokinetic features...

..These results suggest that DLs are applicable as an oral dosage form for peptide drugs such as insulin etc., especially in combination with protease inhibitors...

..8. These particle characteristics and in vitro behaviors demonstrated that the present Eudragit-coated Ch-SP-MS were considered potentially suitable for in vivo or practical application as a specific delivery system of PD to IBD sites...

..This review summarizes the application of chitin and chitosan derivatives for hospital preparations and drug carriers...

..The presence of the tumor itself influenced the body weight and leukocyte number. However, toxic side effects could be evaluated from the body weight and leukocyte number to almost the same extent between tumor-bearing and normal mice...

..It is suggested that the PLA/PLA-(MeO-PEG) mixture nanoparticles with a higher PEG/PLA ratio should be useful as a carrier for the elevation of the plasma concentration of lipophilic drugs...

..MPs are suggested as a possible useful system to prolong the therapeutic effect of GLA...

..These properties were considered to result from well-mixed and fine-powdered SSE and FS...

..OVA-specific IgA was induced significantly more efficiently by ER-Chi-OVA than the others. These suggested that ER-Chi-OVA should be possibly useful to induce an intestinal mucosal immune response...

..DFUR-containing chitosan microspheres with fairly large size and good drug content could be obtained by the present preparation but remained to be improved for drug release properties...

..Only Chi-MPC suppressed the initial plasma level and maintained the plasma concentration for a long time up to 24 h, suggesting Chi-MPC would be useful for prolonged intestinal absorption of cephradine...

..Further, with intravenous administration at 3 days post-inoculation, Suc(II)-MMC exhibited a much higher survival effect at a dose of 4 mg kg(-1) for 4 days...

..It is suggested that a droplet of CZ/OA/propylene glycol (2.5:5.0:92.5, wt/wt) might be useful as an alternative to i.v. injection of CZ for the treatment of acute epileptic seizures...

..This review summarizes the utilization of Suc-Chi as a drug carrier for macromolecular conjugates of MMC and the therapeutic efficacy of the conjugates against various tumours...

..Although FD films were less effective than KE alone, they were superior as to usability such as changing the preparation...

..The tablet showed good adsorption potential for acetaminophen, though the adsorption rate and extent of the tablet were reduced to some extent as compared with powder...

..With regard to chemotherapy against sarcoma 180, both conjugates were considered to supply MMC slowly but effectively at higher doses...

..In addition, the double liposomes could retain OVA longer in PP, which might cause the enhancement of oral immunization...

..05). Therefore, it is speculated that not only the size of liposomes but also the cationic charge plays an important role in the intestinal absorption of DL. These findings suggested the utility of DL as an oral dosage form of SCT...

..It is suggested that PLA-aldehyde should be useful as a functional intermediate for derivatization of PLA, and PLA-(MeO-PEG(N)) can be used for the preparation of PEG-coated PLA nanoparticles...

..These results indicate that the combination of PF and PG was appropriate for the transdermal absorption of PF, and PF was absorbed through the rat skin to an extent sufficient to cause a continuous sedative effect...

..These findings suggested that the glass beads method developed in this study conferred a high drug loading and a high DL formation on liposomes compared with ordinary methods...

..The glass-filter method is the only method that we can get the double liposomes in a short period, and double liposomes prepared by this novel method had adequate size and good stability in vitro...

..In this section, the preparative procedure of PLA derivaties and several nanoparticles prepared with PLA derivatives are introduced. Moreover, the physicochemical and biopharmaceutical characteristics of the nanoparticles are overviewed...

..Thus, Lac-Suc was found available as a carrier exhibiting a high affinity to and long retention in the liver...

..Considering the elimination of pus, CH83-MH2-A tended to be better than CH83 film. CH83-MH2-A is suggested as a useful formulation for the treatment of severe burn wounds...

..The dosage forms best masking bitter taste showed good release of the drug, indicating little change in bioavailability by masking...

..These results suggested that enhancement of skin hydration plays an important role in the enhancing effect of switching iontophoresis on skin permeation...

..v. administration were higher than those at 8 h after i.p. administration. These suggested more localization of the conjugate in peripheral tissues and less excretion at i.p. administration, which might result in greater toxicity...

..MMC/kg). Both carriers, Suc showing systemic long-circulation and Lac-Suc with an ability of liver-specific localization, are thought to be drug carriers with potentialities for therapeutics at early stage of metastasis...

..The ratio of tumor accumulation reached a plateau at 48 h after injection, and the accumulation level, approximately 10%, was similar to those observed for other reported long-circulating macromolecules...

..The intrinsic viscosity ([eta]) obtained at the concentration of 0.1-0.3% (w/v) in saline showed a linear relationship between log[eta] and log MW, which provided the coefficients in the Mark-Houwink equation...

..Chi-MP showed a good mucoadhesion. The maximum plasma concentration of ketoprofen for Chi-MP was less than one-third of that for ketoprofen powder suspension. Chi-MP tended to show the higher and steadier plasma level than MS...

..The present chitosan microsphere system showed good adhesion to the intestinal mucosa, but scarcely facilitated absorption of insulin...

..Kinetic analysis demonstrated that formation I showed a nearly zero-order release rate in vivo consistent with that observed in vitro...

..To identify the optimal schedule for intraperitoneal (i.p.) infusion of floxuridine (FUDR) against peritoneal micrometastases from gastric cancer...

..It is believed that the chitin and chitosan derivatives discussed in this review are good candidates for a polymeric drug carrier in cancer chemotherapy...