کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
2487804 | 1114434 | 2006 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
In Vivo Evaluation of a Nasal Insulin Delivery System Based on Thiolated Chitosan
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کلمات کلیدی
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
اکتشاف دارویی
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چکیده انگلیسی
The aim of this study was the preparation and in vivo evaluation of a nasal insulin delivery system based on thiolated chitosan. 2-Iminothiolane was covalently attached to chitosan. The resulting conjugate (chitosan-TBA) exhibited 304.9â±â63.5 µmol thiol groups per gram polymer. Microparticles were prepared via a new precipitation-micronization technique. The microparticulate delivery system comprised insulin, reduced glutathione and chitosan-TBA (Chito-TBA/Ins) or unmodified chitosan (Chito/Ins) and control microparticles were composed of insulin and mannitol (Mannitol/Ins). Due to a hydration process the size of Chito-TBA/Ins and Chito/Ins microparticles increased in phosphate buffer pH 6.8 2.6- and 2.2-fold, respectively. Fluorescent-labeled insulin-loaded chitosan-TBA microparticles showed a controlled release over 4 h. Chito-TBA/Ins administered nasally to rats led to an absolute bioavailability of 6.9â±â1.5%. The blood glucose level decreased for more than 2 h and the calculated absolute pharmacological efficacy was 4.9â±â1.4%. Chito/Ins, in comparison, displayed a bioavailability of 4.2â±â1.8% and a pharmacological efficacy of 0.7â±â0.6%. Mannitol/Ins showed a bioavailability of 1.6â±â0.4% and no reduction of the blood glucose level at all. According to these findings microparticles comprising chitosan-TBA seem to have substantial higher potential for nasal insulin administration than unmodified chitosan.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical Sciences - Volume 95, Issue 11, November 2006, Pages 2463-2472
Journal: Journal of Pharmaceutical Sciences - Volume 95, Issue 11, November 2006, Pages 2463-2472
نویسندگان
Alexander H. Krauland, Verena M. Leitner, Vjera Grabovac, Andreas Bernkop-Schnürch,