کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
9918892 1557561 2005 10 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Pharmacokinetics and biodistribution of RGD-targeted doxorubicin-loaded nanoparticles in tumor-bearing mice
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی علوم دارویی
پیش نمایش صفحه اول مقاله
Pharmacokinetics and biodistribution of RGD-targeted doxorubicin-loaded nanoparticles in tumor-bearing mice
چکیده انگلیسی
We report the biodistribution and pharmacokinetics (PK) of a cyclic RGD-doxorubicin-nanoparticle (NP) formulation in tumor-bearing mice. The NP core was composed of inulin multi-methacrylate with a targeting peptide, cyclic RGD, covalently attached to the NPs via PEG-400. Seventy-two percent of the doxorubicin was attached to the NP matrix via an amide bond; 28% of doxorubicin was entrapped as unconjugated drug. The PK of total, unconjugated and metabolized doxorubicin was examined for 5 days following intravenous (i.v.) administration of the NP formulation (250 μg doxorubicin equiv.), revealing a bi-exponential fix with a terminal half-life of 5.99 h. In addition, the biodistribution studies revealed decreasing drug concentrations over time in the heart, lung, kidney and plasma and accumulating drug concentrations in the liver, spleen and tumor. The drug concentration in these latter tissues peaked between 24 and 48 h with the liver, spleen and tumor containing 56, 3.5 and 1.8% of the administered dose at t = 48 h, respectively. In contrast to all of the organs studied, the tumors contained high levels of a doxorubicin metabolite.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 293, Issues 1–2, 11 April 2005, Pages 281-290
نویسندگان
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