کد مقاله کد نشریه سال انتشار مقاله انگلیسی ترجمه فارسی نسخه تمام متن
8513441 1556496 2018 42 صفحه PDF سفارش دهید دانلود رایگان
عنوان انگلیسی مقاله ISI
Fabrication and Use of Poly(d,l-lactide-co-glycolide)-Based Formulations Designed for Modified Release of 5-Fluorouracil
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موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی اکتشاف دارویی
پیش نمایش صفحه اول مقاله
Fabrication and Use of Poly(d,l-lactide-co-glycolide)-Based Formulations Designed for Modified Release of 5-Fluorouracil
چکیده انگلیسی
5-fluorouracil (5-FU) is a chemotherapeutic agent that has been used for the treatment of a variety of malignancies since its initial introduction to the clinic in 1957. Owing to its short biological half-life, multiple dosings are generally required to maintain effective 5-FU plasma concentrations throughout the therapeutic period. Clinical studies have shown that continuous 5-FU administration is generally superior to bolus injection as exhibited by lower toxicities and increased therapeutic efficacy. Optimal therapeutic efficacy, however, is often compromised by the limiting therapeutic index. Whilst oral formulations are also used, these suffer from the drawbacks of variable bioavailability and first-pass metabolism. As a result, sustained release formulations of 5-FU have been investigated in an effort to mimic the kinetics of continuous infusion particularly for situations where local delivery is considered appropriate. The biocompatible, biodegradable, and highly tunable synthetic polymer, poly(d,l-lactide-co-glycolide) (PLGA), is widely used as a vector for sustained drug delivery, however, issues such as insufficient loading and inappropriate burst release kinetics have dogged progress into the clinic for small hydrophilic drugs such as 5-FU. This review provides introductory information about the mechanism of action, pharmacokinetic and physicochemical properties, and clinical use of 5-FU that have contributed to the development of PLGA-based 5-FU release platforms. In addition, this review provides information on fabrication methods used for a range of 5-FU-loaded PLGA formulations and discusses factors affecting the release kinetics of 5-FU as well as the in vitro and in vivo antitumor or antiproliferative efficacy of these platforms.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 107, Issue 2, February 2018, Pages 513-528
نویسندگان
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