Abstract:
PURPOSE:To investigate the influence of nanocarrier molecular size and shape on breast duct retention in normal rats using a non-invasive optical imaging method. METHODS:Fluorescein-labeled PEG nanocarriers of different molecular weights and shapes (linear, two-arm, four-arm, and eight-arm) were intraductally administered (50 nmol) to female Sprague-Dawley rats. Whole body images were obtained non-invasively. Fluorescence intensities (i.e., amount remaining in duct) were plotted against time to estimate the nanocarrier ductal retention half-lives (t(1/2)). Plasma samples were taken and the pharmacokinetics (Tmax, Cmax) of absorbed nanocarriers was also assessed. RESULTS:The t(1/2) of linear 12, 20, 30, 40, and two-arm 60 kDa nanocarriers were 6.7 ± 0.9, 16.1 ± 4.1, 16.6 ± 3.4, 21.5 ± 2.7, and 19.5 ± 6.1 h, whereas the four-arm 20, 40, and eight-arm 20 kDa had t(1/2) of 9.0 ± 0.5, 11.5 ± 1.9, and 12.6 ± 3.0 h. The t(1/2) of unconjugated fluorescein was significantly lower (14.5 ± 1.4 min). The Tmax for 12, 40, 60 kDa nanocarriers were 1, 24, and 32 h, respectively, and only 30 min for fluorescein. CONCLUSIONS:Since normal breast ducts are highly permeable, the use of nanocarriers may be helpful in prolonging ductal retention of diagnostic and/or therapeutic agents.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Singh Y,Gao D,Gu Z,Li S,Rivera KA,Stein S,Love S,Sinko PJdoi
10.1007/s11095-012-0763-zsubject
Has Abstractpub_date
2012-09-01 00:00:00pages
2377-88issue
9eissn
0724-8741issn
1573-904Xjournal_volume
29pub_type
杂志文章abstract:PURPOSE:Deposition characteristics of MDI and DPI aerosols were compared throughout the conducting airways for the first time using a combination of in vitro experiments and a newly developed stochastic individual path (SIP) model for different inhalation profiles. METHODS:In vitro experiments were used to determine i...
journal_title:Pharmaceutical research
pub_type: 杂志文章
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abstract::Interogan variation in tissue distribution of weakly basic drugs such as quinidine, propranolol, and imipramine was investigated as a function of binding to phosphatidylserine (PhS) in tissues. Tissue distributions of these drugs were determined using 10 different tissues at a steady-state plasma concentration and wer...
journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
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abstract::Human monocytes/macrophages (MO/MAC) were isolated from peripheral blood and cultivated on hydrophobic Teflon membranes. This culture system is suitable for HIV infection of MO/MAC in vitro. After transfer into 24-well plates the mature macrophages (infected or uninfected) were used for measurements of phagocytosis. T...
journal_title:Pharmaceutical research
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doi:10.1023/a:1015852732512
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journal_title:Pharmaceutical research
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journal_title:Pharmaceutical research
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更新日期:2011-04-01 00:00:00
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journal_title:Pharmaceutical research
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更新日期:2012-09-01 00:00:00
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journal_title:Pharmaceutical research
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doi:10.1023/a:1018974409622
更新日期:1999-06-01 00:00:00
abstract::Short-lived gamma emitting radioisotopes can be incorporated into polylactide/glycolide polymeric microspheres with various specific activities for possible use in understanding the in-vivo deposition, distribution and clearance of microparticulate drug carrier systems. The incorporated radiolabel is stable with negli...
journal_title:Pharmaceutical research
pub_type: 杂志文章
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更新日期:1995-12-01 00:00:00
abstract:PURPOSE:To investigate, for the first time, the performance of a dry powder inhaler (DPI, Aerolizer(®)) in the case of a model drug (i.e. albuterol sulphate) formulated with spray dried mannitol carrier particles with homogeneous shape and solid-state form but different sizes. METHODS:Spray dried mannitol (SDM) partic...
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更新日期:2014-01-01 00:00:00
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更新日期:2005-12-01 00:00:00
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pub_type: 杂志文章
doi:10.1007/s11095-006-9568-2
更新日期:2006-03-01 00:00:00
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doi:10.1007/s11095-009-9834-1
更新日期:2009-05-01 00:00:00
abstract:PURPOSE:In this study, we developed and evaluated a novel method to produce insulin-loaded hydrophilic microspheres allowing high encapsulation efficiency and the preservation of peptide stability during particle processing. The preparation method used the diffusion of water by an excess of solvent starting from a wate...
journal_title:Pharmaceutical research
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doi:10.1023/b:pham.0000036919.94865.57
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journal_title:Pharmaceutical research
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更新日期:2009-07-01 00:00:00
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更新日期:1990-04-01 00:00:00
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更新日期:1996-01-01 00:00:00
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journal_title:Pharmaceutical research
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更新日期:1990-12-01 00:00:00
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更新日期:2000-05-01 00:00:00
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journal_title:Pharmaceutical research
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更新日期:1995-06-01 00:00:00
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更新日期:1996-10-01 00:00:00
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更新日期:1995-04-01 00:00:00
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更新日期:1995-07-01 00:00:00
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更新日期:2002-10-01 00:00:00