Abstract:
PURPOSE:The fate of inhaled salmon calcitonin (sCT) at the respiratory epithelial barrier was studied with particular emphasis on enzymatic degradation by trypsin, chymotrypsin, and neutrophil elastase. METHODS:Degradation of sCT was assessed by HPLC in cell homogenate, supernatant and intact monolayers of human respiratory epithelial cells (hBEpC, Calu-3, 16HBE14o-, A549) and Caco-2 as comparison at 37°C for 2 h. Breakdown of sCT by trypsin, chymotrypsin and neutrophil elastase was investigated. The presence of enzymes in cell supernatant and homogenate was studied by immunoblot and enzyme activity by model substrate assay. Transport studies across Calu-3 monolayers were performed. RESULTS:sCT concentration remained unchanged over 2 h, when incubated in supernatant or with cell monolayers, independent of cell type studied. When cell homogenates were used, sCT concentrations were reduced to varying extents. sCT was degraded when incubated with enzymes alone. Western blot revealed abundance of all proteinases in cell homogenates and weaker expression in supernatants. Transport studies indicated net-absorptive sCT translocation; presence of bacitracin resulted in increased amount of sCT in receiver compartments. CONCLUSIONS:Epithelial proteases play a role in the disposition of sCT after pulmonary delivery.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Baginski L,Tewes F,Buckley ST,Healy AM,Bakowsky U,Ehrhardt Cdoi
10.1007/s11095-011-0553-zsubject
Has Abstractpub_date
2012-01-01 00:00:00pages
332-41issue
1eissn
0724-8741issn
1573-904Xjournal_volume
29pub_type
杂志文章abstract:PURPOSE:SN-38, a potent chemotherapeutic drug, has not been used clinically because of its severe side effects and poor solubility. In this work, we aimed to evaluate the effect of dose and multiple injections of SN-38-loaded polymeric depots on antitumor efficacy and toxicity in vivo. METHODS:Preparation and characte...
journal_title:Pharmaceutical research
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abstract:PURPOSE:Oral bioavailability for antisense oligonucleotides has recently been reported but the mechanistic details are not known. The proposed oral delivery of nucleic acids will, therefore, require an understanding of the membrane binding interactions, cell uptake and transport of oligonucleotides across the human gas...
journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
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更新日期:2002-07-01 00:00:00
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journal_title:Pharmaceutical research
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更新日期:2007-06-01 00:00:00
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
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更新日期:1997-07-01 00:00:00
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journal_title:Pharmaceutical research
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更新日期:2020-01-28 00:00:00
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journal_title:Pharmaceutical research
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doi:10.1007/s11095-008-9674-4
更新日期:2008-11-01 00:00:00
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journal_title:Pharmaceutical research
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更新日期:1992-10-01 00:00:00
abstract:PURPOSE:This study aimed to investigate the impact of the size of X-ray iodinated contrast agent in nano-emulsions, on their toxicity and fate in vivo. METHODS:A new compound, triiodobenzoate cholecalciferol, was synthetized, formulated as nano-emulsions, and followed after i.v. administration in mice by X-ray imaging...
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更新日期:2016-03-01 00:00:00
abstract:PURPOSE:To test the hypothesis that modification of release pattern of nonsteroidal anti-inflammatory drugs (NSAIDs) formulations shifts gastrointestinal (GI) toxicity of the drugs from the upper GI region to the distal intestine. METHODS:We assessed tiaprofenic acid (TA)-induced upper and lower increased GI permeabil...
journal_title:Pharmaceutical research
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doi:10.1023/a:1018887216098
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:1995-07-01 00:00:00
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更新日期:2019-12-17 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
doi:10.1007/s11095-010-0290-8
更新日期:2011-02-01 00:00:00
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journal_title:Pharmaceutical research
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更新日期:1987-04-01 00:00:00
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更新日期:2011-05-01 00:00:00
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更新日期:2018-08-09 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2012-01-01 00:00:00
abstract::Many drugs and desirable phytochemicals are bitter, and bitter tastes are aversive. Food and pharmaceutical manufacturers share a common need for bitterness-masking strategies that allow them to deliver useful quantities of the active compounds in an acceptable form and in this review we compare and contrast the chall...
journal_title:Pharmaceutical research
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更新日期:2014-11-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:1998-08-01 00:00:00
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journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:2012-04-01 00:00:00
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pub_type: 杂志文章
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更新日期:1996-10-01 00:00:00