Abstract：
PURPOSE:This study aimed to develop a sustained-release formulation of exenatide (EXT) for the long-term therapeutic efficacy in the treatment of type II diabetes. METHODS:In this study, we present an injectable phospholipid gel by mixing biocompatible phospholipid S100, medium chain triglyceride (MCT) with 85% (w/w) ethanol. A systemic pre-formulation study has been carried out to improve the stability of EXT during formulation fabrication. With the optimized formulation, the pharmacokinetic profiles in rats were studied and two diabetic animal models were employed to evaluate the therapeutic effect of EXT phospholipid gel via a single subcutaneous injection versus repeated injections of normal saline and EXT solution. RESULTS:With optimized formulation, sustained release of exenatide in vivo for over three consecutive weeks was observed after one single subcutaneous injection. Moreover, the pharmacodynamic study in two diabetic models justified that the gel formulation displayed a comparable hypoglycemic effect and controlled blood glucose level compared with exenatide solution treated group. CONCLUSIONS:EXT-loaded phospholipid gel represents a promising controlled release system for long-term therapy of type II diabetes.
journal_name
Pharm Resjournal_title
Pharmaceutical researchauthors
Hu M,Zhang Y,Xiang N,Zhong Y,Gong T,Zhang ZR,Fu Ydoi
10.1007/s11095-016-1873-9subject
Has Abstractpub_date
2016-06-01 00:00:00pages
1318-26issue
6eissn
0724-8741issn
1573-904Xpii
10.1007/s11095-016-1873-9journal_volume
33pub_type
杂志文章abstract：:Animal models are used commonly in various stages of drug discovery and development to aid in the prospective assessment of drug-drug interaction (DDI) potential and the understanding of the underlying mechanism for DDI of a drug candidate. In vivo assessments in an appropriate animal model can be very valuable, when ...
journal_title：Pharmaceutical research
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journal_title：Pharmaceutical research
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journal_title：Pharmaceutical research
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journal_title：Pharmaceutical research
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journal_title：Pharmaceutical research
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doi：10.1023/a:1012111008617
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更新日期：2009-12-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2018-10-18 00:00:00
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journal_title：Pharmaceutical research
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更新日期：1997-10-01 00:00:00
abstract：PURPOSE:To investigate the potential of chitosan nanoparticles as a system for improving the systemic absorption of insulin following nasal instillation. METHODS:Insulin-loaded chitosan nanoparticles were prepared by ionotropic gelation of chitosan with tripolyphosphate anions. They were characterized for their size a...
journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：1999-10-01 00:00:00
abstract：PURPOSE:We evaluated the effect of luminal bacterial metabolism on intestinal absorption of azetirelin in rats. In vitro characteristics of bacterial metabolism of azetirelin were also investigated with the goal of overcoming the low stability of the peptidic drug against luminal microorganisms. METHODS:Plasma azetire...
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pub_type： 杂志文章
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更新日期：1997-08-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
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更新日期：2014-11-01 00:00:00
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journal_title：Pharmaceutical research
pub_type： 杂志文章
doi：10.1007/s11095-009-9876-4
更新日期：2009-07-01 00:00:00
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更新日期：2016-01-01 00:00:00
