کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2474753 1113161 2015 10 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
In vitro and in vivo evaluation of cubosomes containing 5-fluorouracil for liver targeting
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی اکتشاف دارویی
پیش نمایش صفحه اول مقاله
In vitro and in vivo evaluation of cubosomes containing 5-fluorouracil for liver targeting
چکیده انگلیسی

The objective of this study was to prepare cubosomal nanoparticles containing a hydrophilic anticancer drug 5-fluorouracil (5-FU) for liver targeting. Cubosomal dispersions were prepared by disrupting a cubic gel phase of monoolein and water in the presence of Poloxamer 407 as a stabilizer. Cubosomes loaded with 5-FU were characterized in vitro and in vivo. In vitro, 5-FU-loaded cubosomes entrapped 31.21% drug and revealed nanometer-sized particles with a narrow particle size distribution. In vitro 5-FU release from cubosomes exhibited a phase of rapid release of about half of the entrapped drug during the first hour, followed by a relatively slower drug release as compared to 5-FU solution. In vivo biodistribution experiments indicated that the cubosomal formulation significantly (P<0.05) increased 5-FU liver concentration, a value approximately 5-fold greater than that observed with a 5-FU solution. However, serum serological results and histopathological findings revealed greater hepatocellular damage in rats treated with cubosomal formulation. These results demonstrate the successful development of cubosomal nanoparticles containing 5-FU for liver targeting. However, further studies are required to evaluate hepatotoxicity and in vivo antitumor activity of lower doses of 5-FU cubosomal formulation in treatment of liver cancer.

5-Fluorouracil (5-FU) was successfully incorporated into cubosomal nanoparticles. Cubosomes loaded with 5-FU exhibited reasonable in vitro characteristics. Moreover, in vivo biodistribution of 5-FU in rat׳s liver indicated that the cubosomal formulation increased 5-FU liver concentration (nearly 5-fold) compared to 5-FU solution. In conclusion, cubosomes containing 5-FU has significant liver targeting properties.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Acta Pharmaceutica Sinica B - Volume 5, Issue 1, January 2015, Pages 79–88
نویسندگان
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