Efficacy of a new sustained-release microsphere formulation of exenatide, DA-3091, in Zucker diabetic fatty (ZDF) rats

Kwak, Hyun-Hee; Shim, Won‐Sik; Son, Mi-Kyung; Kim, Inah; Kim, Tae‐Hyoung; Youn, Hyun-Jun; Kang, Soo-Hyoung; Shim, Chang‐Koo

doi:10.1016/j.ejps.2010.03.006

Cited by 14 publications

(20 citation statements)

References 22 publications

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“…Berberine is an isoquinoline derivative alkaloid isolated from Rhizoma Coptidis that has exhibited anti‐diabetic properties in recent research. ZDF rats, derived from inbreeding hyperglycemic Zucker obese rats, exhibit marked hyperglycemia along with insulin resistance, hyperlipidemia and obesity, potentially making them useful as a model of human T2DM (Kwak et al , ). In this present study, reduction of insulin and increased levels of HbA1c, TC, and TG in sera were observed in the model rats induced by high fat and sugar feed.…”

Section: Discussionmentioning

confidence: 99%

Metabolomics Study of Type 2 Diabetes Mellitus and the AntiDiabetic Effect of Berberine in Zucker Diabetic Fatty Rats Using Uplc‐ESI‐Hdms

Dong

Chen

Yang

et al. 2016

Phytotherapy Research

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The present study aimed to evaluate the pathogenesis of type 2 diabetes mellitus (T2DM) and the anti-diabetic effect of berberine in Zucker diabetic fatty (ZDF) rats. A urinary metabolomics analysis was performed with ultra-performance liquid chromatography/electrospray ionization synapt high-definition mass spectrometry. Pattern recognition approaches were integrated to discover differentiating metabolites. We identified 29 ions (13 in negative mode and 16 in positive mode) as 'differentiating metabolites' with this metabolomic approach. A functional pathway analysis revealed that the alterations were mainly associated with glyoxylate and dicarboxylate metabolism, pentose and glucuronate interconversions and sphingolipid metabolism. These results indicated that the dysfunctions of glycometabolism and lipometabolism are involved in the pathological process of T2DM. Berberine could decrease the serum levels of glycosylated hemoglobin, total cholesterol and triglyceride and increase the secretion of insulin. The urinary metabolomics analysis showed that berberine could reduce the concentrations of citric acid, tetrahydrocortisol, ribothymidine and sphinganine to a near-normal state. These results suggested that the anti-diabetic effect of berberine occurred mainly via its regulation of glycometabolism and lipometabolism and activation of adenosine 5'-monophosphate-activated protein kinase. Our work not only provides a better understanding of the anti-diabetic effect of berberine in ZDF rats but also supplies a useful database for further study in humans and for investigating the pharmacological actions of drugs. Copyright © 2016 John Wiley & Sons, Ltd.

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Section: Discussionmentioning

confidence: 99%

Metabolomics Study of Type 2 Diabetes Mellitus and the AntiDiabetic Effect of Berberine in Zucker Diabetic Fatty Rats Using Uplc‐ESI‐Hdms

Dong

Chen

Yang

et al. 2016

Phytotherapy Research

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“…Exenatide loaded microspheres were suspended in sterile PBS (the dose of peptide was 2 mg/kg) [11] and administered by subcutaneous injection. Blood samples were collected by retro-orbital bleeding into EDTA anticoagulated tubes at different time intervals for 20 days, transferred into 1.5 ml centrifuge tubes, and centrifuged at 15,000 rpm for 5 min.…”

Section: In Vivo Release Studymentioning

confidence: 99%

Exenatide-loaded PLGA microspheres with improved glycemic control: In vitro bioactivity and in vivo pharmacokinetic profiles after subcutaneous administration to SD rats

et al. 2013

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“…Thus, lactide:glycolide ratios of 85 : 15, 65 : 35, 50 : 50, and so forth are fairly common and frequently reported in the literature [18][19][20][21][22]. Altering the copolymer composition (lactide : glycolide ratio) is a primary means to tailor drug levels in vivo for varying duration, from weeks to several months [23][24][25], leading to an improvement in patient compliance due to reduced dosing frequency [19,[26][27][28].…”

Section: Introductionmentioning

confidence: 99%

Effect of Hydration on Physicochemical Properties of End-Capped PLGA

D’Souza

Dorati

DeLuca

2014

Advances in Biomaterials

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The objective of this study was to assess the physicochemical effects of hydrating a hydrophobic end-capped poly(lactide-coglycolide) (PLGA) polymer in the liquid and vapor state. PLGA RG503 polymer was incubated at 37 ∘ C in 0.5% polyvinyl alcohol (PVA) solution and at 90% RH. Samples were withdrawn at predetermined intervals and changes to polymer properties like glass transition temperature (T g ), moisture uptake, molecular weight change, and % acid number were determined using differential scanning calorimetry, Karl Fisher titrimetry, gel permeation chromatography, and acid base titrimetry, respectively. Study results showed that T g was depressed instantaneously upon hydration, indicating that bulk water acted as a plasticizer of hydrophobic end-capped PLGA. T g values decreased to levels below the incubation temperature when hydrated in 0.5% PVA solution but not in 90% RH. The drop in T g exhibited a linear relationship ( 2 > 0.99) to the amount of water uptake by the polymer; higher moisture uptake was noted with liquid water. Removal of moisture from the polymer matrix resulted in recovery of T g , only up to a period of 14 days. Presence of water in liquid or vapor form caused a reduction in molecular weight of the polymer and a corresponding increase in % acid number over the duration of the study.

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Efficacy of a new sustained-release microsphere formulation of exenatide, DA-3091, in Zucker diabetic fatty (ZDF) rats

Cited by 14 publications

References 22 publications

Metabolomics Study of Type 2 Diabetes Mellitus and the AntiDiabetic Effect of Berberine in Zucker Diabetic Fatty Rats Using Uplc‐ESI‐Hdms

Metabolomics Study of Type 2 Diabetes Mellitus and the AntiDiabetic Effect of Berberine in Zucker Diabetic Fatty Rats Using Uplc‐ESI‐Hdms

Exenatide-loaded PLGA microspheres with improved glycemic control: In vitro bioactivity and in vivo pharmacokinetic profiles after subcutaneous administration to SD rats

Effect of Hydration on Physicochemical Properties of End-Capped PLGA

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