کد مقاله کد نشریه سال انتشار مقاله انگلیسی ترجمه فارسی نسخه تمام متن
5521655 1545314 2016 8 صفحه PDF سفارش دهید دانلود کنید
عنوان انگلیسی مقاله ISI
Research paperPreactivated thiomers for intranasal delivery of apomorphine: In vitro and in vivo evaluation
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی بیوتکنولوژی یا زیست‌فناوری
پیش نمایش صفحه اول مقاله
Research paperPreactivated thiomers for intranasal delivery of apomorphine: In vitro and in vivo evaluation
چکیده انگلیسی

The purpose of this study was to synthesize preactivated thiomers with different degrees of preactivation and to evaluate their potential as novel excipient for nasal apomorphine administration. The thiomer (PAA-cys) was synthesized by addition of thiol groups on poly(acrylic acid) with various molecular mass including 100, 250 and 450 kDa followed by immobilization of 2-mercaptonicotinic acid (2MNA) to thiol groups by disulfide bond formation resulting in PAA-cys-2MNA. These thiomers (PAA100-cys, PAA250-cys and PAA450-cys) were in the next step preactivated by 56.3, 59.5 and 46.5% (medium degree), and 80.1, 81.6 and 87% (high degree), respectively. Apomorphine permeation across porcine nasal mucosa in the presence of PAA100-cys-2MNA, PAA250-cys-2MNA and PAA450-cys-2MNA with high degree of preactivation was 3.1-, 4.4- and 4.1-fold, while 2.7-, 3.4- and 3.0-fold higher than control for medium degree of preactivation, respectively. Administration of apomorphine in the presence of PAA250-cys-2MNA showed in rats 9 and ∼2-fold improvement of relative bioavailability compared with oral and intranasal administration of apomorphine solution, respectively. Because of the pronounced improvement among other polymers, PAA250-cys-2MNA with high degree of preactivation could be considered as promising excipient for nasal delivery of apomorphine.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmaceutics and Biopharmaceutics - Volume 109, December 2016, Pages 35-42
نویسندگان
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