کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2083596 1545339 2014 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Montelukast-loaded nanostructured lipid carriers: Part I Oral bioavailability improvement
ترجمه فارسی عنوان
نانوکامپوزیتهای مونل لکواستر لایه نازک: قسمت 1 بهبود زیستی خوراکی
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی بیوتکنولوژی یا زیست‌فناوری
چکیده انگلیسی


• Montelukast-NLC was successfully prepared using melt-emulsification-ultrasonication.
• Particle size of 181 nm and 96% encapsulation efficiency were obtained.
• Montelukast release was sustained over a period of 24 h from MNLC.
• 9- and 60-fold improvement in Cmax and AUC0–24, respectively was achieved.
• Encapsulation in lipid matrix resulted 143-fold improvement in the bioavailability.

The purpose of the study was to formulate montelukast-loaded nanostructured lipid carrier (MNLC) to improve its systemic bioavailability, avoid hepatic metabolism and reduce hepatic cellular toxicity due to metabolites. MNLC was prepared using melt-emulsification-homogenization method. Preformulation study was carried out to evaluate drug-excipient compatibility. MNLCs were prepared using spatially different solid and liquid lipid triglycerides. CAE (DL-Pyrrolidonecarboxylic acid salt of L-cocyl arginine ethyl ester), a cationic, biodegradable, biocompatible surfactant was used to stabilize the system. MNLCs were characterized by FTIR, XRPD and DSC to evaluate physicochemical properties. MNLCs having a particle size of 181.4 ± 6.5 nm with encapsulation efficiency of 96.13 ± 0.98% were prepared. FTIR findings demonstrated no interaction between the drug and excipients of the formulation which could lead to asymmetric vibrations. DSC and XRPD study confirmed stable amorphous form of the montelukast in lipid matrix. In vitro release study revealed sustained release over a period of 24 h. In vivo single dose oral pharmacokinetic study demonstrated 143-fold improvement in bioavailability as compared to montelukast-aqueous solution. Thus, the result of this study implies that developed MNLC formulation be suitable to sustain the drug release with improvement in the bioavailability.

Figure optionsDownload high-quality image (70 K)Download as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmaceutics and Biopharmaceutics - Volume 88, Issue 1, September 2014, Pages 160–168
نویسندگان
, ,