کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
5809720 1556165 2016 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Optimization of the process variables of tilianin-loaded composite phospholipid liposomes based on response surface-central composite design and pharmacokinetic study
ترجمه فارسی عنوان
بهینه سازی متغیرهای فرآیند لیپوزوم های فسفولیپید کامپوزیتی لجن بر اساس طرح پاسخ کامپوزیت مرکزی پاسخ و مطالعه فارماکوکینتیک
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی اکتشاف دارویی
چکیده انگلیسی

Tilianin is attracting considerable attention because of its antihypertensive, anti-atherogenic and anticonvulsive efficacy. However, tilianin has poor oral bioavailability. Thus, to improve the oral bioavailability of tilianin, composite phospholipid liposomes were adopted in this work as a novel nanoformulation. The aim was to develop and formulate tilianin composite phospholipid liposomes (TCPLs) through ethanol injection and to apply the response surface-central composite design to optimize the tilianin composite phospholipid liposome formulation. The independent variables were the amount of phospholipids (X1), amount of cholesterol (X2) and weight ratio of phospholipid to drug (X3); the depended variables were particle size (Y1) and encapsulation efficiency (EE) (Y2) of TCPLs. Results indicated that the optimum preparation conditions were as follows: phospholipid amount, 500 mg, cholesterol amount, 50 mg and phospholipid/drug ratio, 25. These variables were also the major contributing variables for particle size (101.4 ± 6.1 nm), higher EE (90.28% ± 1.36%), zeta potential (− 18.3 ± 2.6 mV) and PDI (0.122 ± 0.027). Subsequently, differential scanning calorimetry techniques were used to investigate the molecular interaction in TCPLs, and the in vitro drug release of tilianin and TCPLs was investigated by the second method of dissolution in the Chinese Pharmacopoeia (Edition 2015). Furthermore, pharmacokinetics in Sprague Dawley rats was evaluated using a rat jugular vein intubation tube. Results demonstrated that the Cmax of TCPLs became 5.7 times higher than that of tilianin solution and that the area under the curve of TCPLs became about 4.6-fold higher than that of tilianin solution. Overall, our results suggested that the prepared tilianin composite phospholipid liposome formulations could be used to improve the bioavailability of tilianin after oral administration.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmaceutical Sciences - Volume 85, 31 March 2016, Pages 123-131
نویسندگان
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