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Pharm Res. 2012 Sep;29(9):2377-88. doi: 10.1007/s11095-012-0763-z. Epub 2012 May 9.

Influence of molecular size on the retention of polymeric nanocarrier diagnostic agents in breast ducts.

Author information

1
Department of Pharmaceutics Ernest Mario School of Pharmacy, Rutgers The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, New Jersey 08854, USA.

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.

PMID:
22569800
PMCID:
PMC3442773
DOI:
10.1007/s11095-012-0763-z
[Indexed for MEDLINE]
Free PMC Article

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