| Literature DB >> 20883756 |
Hilliard L Kutscher1, Piyun Chao, Manjeet Deshmukh, Sujata Sundara Rajan, Yashveer Singh, Peidi Hu, Laurie B Joseph, Stanley Stein, Debra L Laskin, Patrick J Sinko.
Abstract
The current study examines the passive pulmonary targeting efficacy and retention of 6μm polystyrene (PS) microparticles (MPs) covalently modified with different surface groups [amine (A-), carboxyl (C-) and sulfate (S-)] or single (PEG(1)-) and double (PEG(2)-) layers of α,ω-diamino poly(ethylene glycol) attached to C-MPs. The ζ-potential of A-MPs (-44.0mV), C-MPs (-54.3mV) and S-MPs (-49.6mV) in deionized water were similar; however PEGylation increased the ζ-potential for both PEG(1)-MPs (-18.3mV) and PEG(2)-MPs (11.5mV). The biodistribution and retention of intravenously administered MPs to male Sprague-Dawley rats was determined in homogenized tissue by fluorescence spectrophotometry. PEG(1)-MPs and PEG(2)-MPs demonstrated enhanced pulmonary retention in rats at 48h after injection when compared to unmodified A-MPs (59.6%, 35.9% and 17.0% of the administered dose, respectively). While unmodified MPs did not significantly differ in lung retention, PEGylation of MPs unexpectedly improved passive lung targeting and retention by modifying surface properties including charge and hydrophobicity but not size.Entities:
Mesh：
Substances：
Year: 2010 PMID： 20883756 PMCID： PMC3912554 DOI： 10.1016/j.ijpharm.2010.09.020
Source DB: PubMed Journal: Int J Pharm ISSN： 0378-5173 Impact factor: 5.875