کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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2504885 | 1557472 | 2009 | 9 صفحه PDF | دانلود رایگان |

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.
Journal: International Journal of Pharmaceutics - Volume 373, Issues 1–2, 21 May 2009, Pages 107–115