کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2504885 1557472 2009 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Evaluation of pharmacological efficacy of ‘insulin–surfoplex’ encapsulated polymer vesicles
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی علوم دارویی
پیش نمایش صفحه اول مقاله
Evaluation of pharmacological efficacy of ‘insulin–surfoplex’ encapsulated polymer vesicles
چکیده انگلیسی

The present study has been designed to study whether formation of ion-pair complex or ‘surfoplex’ can enhance the pharmacological efficacy of protein-loaded PCL–PEG-based polymerosomes. Insulin was selected as the model protein and was complexed with sodium deoxycholate, a naturally occurring bile salt. The surfoplexes were characterized for extent and site of complexation, stability, mass and partition coefficient. The lipophilicity of insulin was enhanced 5-fold upon complexation resulting in an increase in entrapment efficiency by 10–50% for all formulations compared to free insulin. The release of insulin from the systems was also modulated with reduction in burst release by 30%. The surfoplex was found to be therapeutically active for 8 h duration (Cmax serum insulin = 64.15 ± 13.28 mIU/mL) in diabetic rat model. However, pharmacological efficacy of the complex-loaded nanoparticles (Nps) did not show significant enhancement with respect to insulin-loaded systems. The study therefore suggests that while ion-pair complexes may improve the in vitro kinetics of protein-loaded carriers, their therapeutic potential is dependent on the intensity of interactions between the peptide chains and polymer matrix.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 373, Issues 1–2, 21 May 2009, Pages 107–115
نویسندگان
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