Drug Delivery System
Online ISSN : 1881-2732
Print ISSN : 0913-5006
ISSN-L : 0913-5006
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Volume 32, Issue 5
Species difference problem on formulation design
Displaying 1-11 of 11 articles from this issue
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[Feature articles] “:Species difference problem on formulation design” Editor:Hiroshi Kikuchi
  • [FOREWORD] Animal species difference problem on DDS formulation design
    Hiroshi Kikuchi
    2017 Volume 32 Issue 5 Pages 367
    Published: November 25, 2017
    Released on J-STAGE: February 25, 2018
    DOIhttps://doi.org/10.2745/dds.32.367
    JOURNAL FREE ACCESS
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  • [OPINION] Species Barrier: From PK to DDS
    Hideyoshi Harashima
    2017 Volume 32 Issue 5 Pages 368
    Published: November 25, 2017
    Released on J-STAGE: February 25, 2018
    DOIhttps://doi.org/10.2745/dds.32.368
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  • Species difference in bioavailability of oral drug controlled release formulation
    Hiromu Kondo
    2017 Volume 32 Issue 5 Pages 372-380
    Published: November 25, 2017
    Released on J-STAGE: February 25, 2018
    DOIhttps://doi.org/10.2745/dds.32.372
    JOURNAL FREE ACCESS
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    In this report, two case examples on species difference between human and experimental animals are introduced. They are related to drug absorption from the lower gastrointestinal tract, which were observed in studies of the oral controlled release formulation design. Both examples showed lower colonic absorption in human than that in experimental animals （dog and monkey）. Although it is difficult to determine the relationship in characteristics of the colonic absorption between human and experimental animals only based on the examples, the result will be expected to be informative to discuss the predictability of the bioavailability of oral controlled release formulations in human from the results of the bioavailability studies in experimental animals.
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  • Approaches to improving the oral bioavailabity of the low-permeability compound DX-9065, and species differences in bioavailability in preclinical and clinical studies
    Yoshimine Fujii
    2017 Volume 32 Issue 5 Pages 381-388
    Published: November 25, 2017
    Released on J-STAGE: February 25, 2018
    DOIhttps://doi.org/10.2745/dds.32.381
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    Species differences in oral bioavailability are occasionally observed in drug development phases. They are most likely due to differences in gastrointestinal physiological parameters such as gastrointestinal pH, gastric emptying rate, intestinal transit time, bile acid concentration, and hepatic and intestinal first-pass effect between species. Therefore, to correctly predict human oral bioavailability of a drug, it is still necessary to evaluate the oral absorption profiles of experimental animals and to understand their gastrointestinal physiologies. We investigated the oral absorption profiles of DX-9065, a low-permeability compound, in in vitro and in vivo studies, and we examined several unique formulations to improve its oral absorption. Here, we give examples of species differences in drug absorption by reviewing our preclinical and clinical data for DX-9065.
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  • Species differences in oral bioavailability enhancement of lipid based formulation
    Masaaki Imono, Katsuji Sugita
    2017 Volume 32 Issue 5 Pages 389-395
    Published: November 25, 2017
    Released on J-STAGE: February 25, 2018
    DOIhttps://doi.org/10.2745/dds.32.389
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    Improvement of oral absorption for poorly water-soluble compounds is a major concern to the pharmaceutical industry. Although various formulation studies have been investigated to overcome the issue of poorly water-soluble compounds, the performance difference of the formulations between animal species is still not well known. This article is designed to contribute further research on oral bioavailability (BA) enhancements by lipid based formulation among animal species. Compound A was used as a poorly water-soluble drug. The lipid based formulation of Compound A was prepared by lipid and lecithin, and administered to rats, dogs and monkeys. Oral absorption of the lipid based formulation was dramatically enhanced, but the effect of the formulation on BA was different among the animal species. The BA enhancement ratios of the lipid formulation to conventional formulation, in rats, dogs and monkeys were 2.2, 6.3 and 3.5, respectively. Pharmacokinetic analysis suggested that the difference of gastro-intestinal and hepatic first pass metabolisms affected the performance of the lipid based formulation of Compound A.
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  • Animal species difference in the ABC phenomenon
    Taro Shimizu, Yu Ishima, Tatsuhiro Ishida
    2017 Volume 32 Issue 5 Pages 396-401
    Published: November 25, 2017
    Released on J-STAGE: February 25, 2018
    DOIhttps://doi.org/10.2745/dds.32.396
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    PEG has been believed a bio-inert polymer which increases bioavailability of therapeutic protein or nanocarrier and decreases immunogenicity of them. PEGylation is still a golden standard in developing protein therapeutic or nanocarrier system. However, we and other groups have reported that PEGylated liposomes or PEGylated proteins induce immune responses against PEG and subsequently produce anti-PEG antibodies, resulting in rapid clearance of second dose PEGylated materials via complement activation. Such immunological responses against PEG should be dependent on animal species to which PEGylated materials are injected. Adverse effects, which might occur during the ABC phenomenon, also should be dependent on animal species. Although there are a few publications regarding effect of animal species on the ABC phenomenon, we try to introduce this issue with our speculation and consideration.
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  • Pitfall of tumor-bearing mouse models
    Kenji Hyodo, Makoto Asano, Eiichi Yamamoto, Hiroshi Kikuchi
    2017 Volume 32 Issue 5 Pages 402-410
    Published: November 25, 2017
    Released on J-STAGE: February 25, 2018
    DOIhttps://doi.org/10.2745/dds.32.402
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    The major issue of cancer chemotherapy is the adverse effect, which is elicited by the systemic exposure of the anticancer agents. The application of DDS technology into anticancer agents is able to inhibit non-selective distribution and to increase accumulation into tumor tissue, thus it can decrease systemic adverse effects and improve therapeutic effect of the anticancer agents. To design the formulation of drugs, it must be considered that the drug products can produce the best performance on clinical settings rather than on animal experiments. However, the translation of the knowledge obtained from animal experiment into the development of the best formulation for clinical usage is quite difficult because there are some discrepancies between human clinical cancer treatments and the tumor-bearing animal experiments. Herein, we will introduce the factors to care on the development of DDS products, especially liposomal formulations, for the treatment of cancer.
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  • Transdermal Permeation of Drugs in Various Animal Species
    Hiroaki Todo
    2017 Volume 32 Issue 5 Pages 411-417
    Published: November 25, 2017
    Released on J-STAGE: February 25, 2018
    DOIhttps://doi.org/10.2745/dds.32.411
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    Excised human skin is utilized for in vitro permeation experiments to evaluate the safety and effect of topically-applied drugs by measuring its skin permeation and concentration. However, ethical considerations are the major problem for using human skin to evaluate percutaneous absorption. Moreover, large variations have been found among human skin specimens as a result of differences in age, race, and anatomical donor site. Animal skins are used to predict the in vivo human penetration/permeation of topically-applied chemicals. In the present review, skin characteristics, such as thickness of skin, lipid content, hair follicle density, and enzyme activity in each model are compared to human skin. In addition, intra- and inter-individual variation in animal models, permeation parameter correlation between animal models and human skin, and utilization of cultured human skin models are also descried. Pig, guinea pig, and hairless rat are generally selected for this purpose. Each animal model has advantages and weaknesses for utilization in in vitro skin permeation experiments. Understanding of skin permeation characteristics such as permeability coefficient(P), diffusivity(D), and partition coefficient(K) for each skin model would be necessary to obtain better correlations for animal models to human skin permeation.
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  • Species-dependent difference in the circadian rhythms of drug pharmacokinetics
    Satoru Koyanagi, Shigehiro Ohdo
    2017 Volume 32 Issue 5 Pages 418-423
    Published: November 25, 2017
    Released on J-STAGE: February 25, 2018
    DOIhttps://doi.org/10.2745/dds.32.418
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    In mammals, a variety of biological processes are subject to daily oscillations, and some of these are controlled by self-sustained oscillation mechanism called circadian clock. The rhythmic oscillations are driven by transcriptional-translational feedback loop consisting of negative and positive regulators encoded from circadian clock genes. This molecular oscillator regulates 24-hour rhythms in output physiology through the periodic activation/repression of clock-controlled genes. Accumulating evidences have revealed that daily oscillation in the physiological functions also affect drug dispositions in laboratory rodents. However, it is difficult to predict the circadian change in the drug pharmacokinetics in a diurnal active human by using the data collected from nocturnal active rodents. This review presents an overview of regulation mechanism for circadian rhythms in the expression of drug metabolism enzymes and xenobiotic transporters, and also describes the importance of evaluation of the difference in the circadian machinery between diurnal and nocturnal animals to choose the most appropriate times of day for drug administration.
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[Serial] Reviews on useful reagents for DDS research and development
“Young square”(mini review)
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