New biomimetic barrier Permeapad™ for efficient investigation of passive permeability of drugs

被引:110
作者
di Cagno, Massimiliano [1 ]
Bibi, Hanady A. [2 ]
Bauer-Brandl, Annette [2 ]
机构
[1] Arctic Univ Norway, Dept Pharm, Drug Transport & Delivery Res Grp, Tromso, Norway
[2] Univ Southern Denmark, Dept Phys Chem & Pharm, Odense, Denmark
关键词
Permeapad (TM); Permeability testing; Biomimetic barrier; Apparent permeability coefficient; Franz cell diffusion system; MEMBRANE PERMEATION ASSAY; VESICLE-BASED BARRIER; CACO-2; ABSORPTION; PREDICTION; MODEL;
D O I
10.1016/j.ejps.2015.03.019
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In this work the suitability of a newly invented physical patch comprising a biomimetic barrier (named Permeapad (TM)) for drug permeability tests has been investigated. Exemplars of Permeapad (TM) were adapted to Franz diffusion cells and apparent permeability (P-app) of a series of drugs were measured and compared with calculated partition coefficients (logP(cal)) of the investigated drugs as well as literature reference values obtained from Parallel Artificial Membrane Permeation Assay (PAMPA) and the cellular based method Caco-2. Moreover, tightness of the barrier to hydrophilic marker's permeation, resistance of these barriers to proton permeation (pH changes) and shelf-life functionality were also investigated. Comparison with the published data indicated a good correlation between the permeability values measured and partition coefficients (logP(cal)). Moreover, a good correlation between the permeabilities measured with the new barrier and well-established in vitro permeability methods (PAMPA and Caco-2 respectively) was found for both highly absorbed and poorly permeable compounds. Permeapad (TM) also proved to maintain high integrity over time and in different pH environments. In conclusion, Permeapad (TM) as an innovative barrier appears to be a promising tool for fast, cost effective and reliable screening of drugs and chemical entities' passive permeability. (C) 2015 Elsevier B.V. All rights reserved.
引用
收藏
页码:29 / 34
页数:6
相关论文
共 25 条
  • [1] [Anonymous], ASSAY DRUG PERMEABIL
  • [2] [Anonymous], HIT LEAD PROFILING
  • [3] CORRELATION BETWEEN ORAL-DRUG ABSORPTION IN HUMANS AND APPARENT DRUG PERMEABILITY COEFFICIENTS IN HUMAN INTESTINAL EPITHELIAL (CACO-2) CELLS
    ARTURSSON, P
    KARLSSON, J
    [J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1991, 175 (03) : 880 - 885
  • [4] Avdeef Alex, 2005, Expert Opin Drug Metab Toxicol, V1, P325, DOI 10.1517/17425255.1.2.325
  • [5] Brandl M., 2009, WILEY ENCY CHEM BIOL, V3, P541
  • [6] Development and evaluation of an in vitro method for prediction of human drug absorption - I. Assessment of artificial membrane composition
    Corti, G
    Maestrelli, F
    Cirri, M
    Furlanetto, S
    Mura, P
    [J]. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2006, 27 (04) : 346 - 353
  • [7] Drug "supersaturation" states induced by polymeric micelles and liposomes: A mechanistic investigation into permeability enhancements
    di Cagno, Massimiliano
    Luppi, Barbara
    [J]. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2013, 48 (4-5) : 775 - 780
  • [8] Comparison of Blood-Brain Barrier Permeability Assays: In Situ Brain Perfusion, MDR1-MDCKII and PAMPA-BBB
    Di, Li
    Kerns, Edward H.
    Bezar, Ian F.
    Petusky, Susan L.
    Huang, Youping
    [J]. JOURNAL OF PHARMACEUTICAL SCIENCES, 2009, 98 (06) : 1980 - 1991
  • [9] In-vitro permeability of poorly water soluble drugs in the phospholipid vesicle-based permeation assay: the influence of nonionic surfactants
    Fischer, Sarah Maud
    Flaten, Goril Eide
    Hagesaether, Ellen
    Fricker, Gert
    Brandl, Martin
    [J]. JOURNAL OF PHARMACY AND PHARMACOLOGY, 2011, 63 (08) : 1022 - 1030
  • [10] Drug permeability across a phospholipid vesicle based barrier: A novel approach for studying passive diffusion
    Flaten, GE
    Dhanikula, AB
    Luthman, K
    Brandl, M
    [J]. EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES, 2006, 27 (01) : 80 - 90