2007
DOI: 10.1248/bpb.30.1007
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Kinetic Model to Predict the Absorption of Nasally Applied Drugs from in Vitro Transcellular Permeability of Drugs

Abstract: In the last few decades, nasal administration has received a great deal of attention as a rationale for the systemic delivery of many drugs.1) The range of compounds investigated for possible nasal application varies greatly from very lipophilic drugs to polar, hydrophilic molecules including peptides and proteins.2) The relatively high permeability of the nasal epithelium, its high vascularization and the avoidance of hepatic first-pass metabolism makes nasal application a promising alternative, especially fo… Show more

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Cited by 21 publications
(19 citation statements)
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“…As listed in Table 1, the rank order of the TEER in the studied cell systems is MDCK (2120 ± 45 Ω•cm 2 ) >> Caco-2 (771 ± 8 Ω•cm 2 ) > MucilAir (560 ± 34 Ω•cm 2 ) > Calu-3 (484 ± 9 Ω•cm 2 ) > EpiAirway (391 ± 50 Ω•cm 2 ). [11,12]. *b: cited from the previous report [15].…”
Section: In Vitro Transepithelial Transport Studymentioning
confidence: 99%
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“…As listed in Table 1, the rank order of the TEER in the studied cell systems is MDCK (2120 ± 45 Ω•cm 2 ) >> Caco-2 (771 ± 8 Ω•cm 2 ) > MucilAir (560 ± 34 Ω•cm 2 ) > Calu-3 (484 ± 9 Ω•cm 2 ) > EpiAirway (391 ± 50 Ω•cm 2 ). [11,12]. *b: cited from the previous report [15].…”
Section: In Vitro Transepithelial Transport Studymentioning
confidence: 99%
“…of 3-4 experiments. *a: cited from our previous report [11,12]. *b: cited from the previous report [15].…”
Section: In Vitro Transepithelial Transport Studymentioning
confidence: 99%
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“…The cell line differentiates slowly to various monolayers with a differentiated phenotype with various functions of the epithelium of small intestinal villus.Caco-2 is one of the valuable cell lines to assess the drug absorption and permeability across the intestinal epithelia. [85][86][87] In vitro Excised Models: Nasal mucosae are excised from various animals and are important tools to study nasal metabolism and transport. 88 While conducting the experiments the viability of excised nasal mucosae should be maintained.…”
Section: Fig 3: Various Models For Intra Nasal Drug Transport and Abmentioning
confidence: 99%
“…It has been reported that the increase in viscosity achieved by PEGylation depends on the MW and the modification number of PEG to be modified [ 12 ]. In the present study, we synthesized PEG-PLO having a different MW ratio of PEG and PLO from that previously reported [ 11 ] and evaluated the in vitro retentivity- and the hydrophilic macromolecules permeation-enhancing ability of PEG-PLO using Caco-2 cell sheet, which is known to have a good correlation between permeability across the sheet and the nasal absorbability in rats [ 13 ], and used this for evaluation of the permeation-enhancing effects and mechanisms of HPBAAs [ 7 , 14 ]. Moreover, the improvement in retentivity in the nasal cavity by PEGylation was estimated pharmacokinetically using an “in vivo intranasal retentivity evaluation system” [ 15 ].…”
Section: Introductionmentioning
confidence: 99%