کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
2502801 1557406 2012 6 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Thermosensitive and mucoadhesive in situ gel based on poloxamer as new carrier for rectal administration of nimesulide
موضوعات مرتبط
علوم پزشکی و سلامت داروسازی، سم شناسی و علوم دارویی علوم دارویی
پیش نمایش صفحه اول مقاله
Thermosensitive and mucoadhesive in situ gel based on poloxamer as new carrier for rectal administration of nimesulide
چکیده انگلیسی

Poloxamer 407 has excellent thermo-sensitive gelling properties. Nevertheless, these gels possess inadequate poor bioadhesiveness and high permeability to water, which limited its’ application as a thermoresponsive matrix. The main aim of the present investigation was to develop thermosensitive and mucoadhesive rectal in situ gel of nimesulide (NM) by using mucoadhesive polymers such as sodium alginate (Alg–Na) and HPMC. These gels were prepared by addition of mucoadhesive polymers (0.5%) to the formulations of thermosensitive gelling solution containing poloxamer 407 (18%) and nimesulide (2.0%). Polyethylene glycol (PEG) was used to modify gelation temperature and drug release properties. The gelation temperature and drug release rate of the prepared in situ gels were evaluated. Gelation temperature was significantly increased with incorporation of nimesulide (2.0%) in the poloxamer solution, while the addition of the mucoadhesive polymers played a reverse role on gelation temperature. The addition of PEG polymers increased the gelation temperature and the drug release rate. Among the formulations examined, the poloxamer 407/nimesulide/sodium alginate/PEG 4000 (18/2.0/0.5/1.2%) exhibited the appropriate gelation temperature, acceptable drug release rate and rectal retention at the administration site. Furthermore, the micrographic results showed that in situ gel, given at the dose of 20 mg/kg, was safe for no mucosa irritation. In addition, it resulted in significantly higher initial serum concentrations, Cmax and AUC of NM compared to the solid suppository.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Journal of Pharmaceutics - Volume 430, Issues 1–2, 1 July 2012, Pages 114–119
نویسندگان
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