Characteristics of repaglinide effects on insulin secretion

Takahashi, Harumi; Hidaka, Shigekazu; Seki, Chihiro; Yokoi, Norihide

doi:10.1016/j.ejphar.2018.03.025

Cited by 7 publications

(4 citation statements)

References 35 publications

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“…It has been reported that sulfonylureas, such as glinides are widely used to treat T2DM, which is mainly due to stimulation of insulin secretion. These drugs stimulate the pβC ATP-sensitive potassium (KATP) channel [Kasabri et al, 2012;Takahashi et al, 2018]. Glinides and sulfonylureas lead to closure of the KATP channel, evoking membrane depolarization and subsequent opening of the voltage-dependent calcium channel.…”

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Synthetic Small Molecules Induce Insulin Secretion and Pancreatic Beta-Cell-Specific Gene Expression

Rabiei¹,

Kalhor²,

Farhadi³

et al. 2022

Cells Tissues Organs

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Despite various efficient pharmaceuticals which are already used to manage diabetes, new drugs are needed to preserve and restore the function of pancreatic β-cells (pβCs) including cell specific gene expression and insulin production and secretion. Newly developed small molecules (SMs) with potential anti-diabetic activity need to be preliminary tested. Mice insulinoma MIN6 cells (MIN6) can be utilized as an in vitro screening model. These cells have pancreatic β-cells characteristics and can secrete insulin in response to glucose level changes. As well, β-cell-specific gene expression pattern of these cells is similar to that of mouse pancreatic islet cells. It is possible to use this cell line as a research tool to study the function of the pancreatic β-cells. To date, approximately 60 genes have been identified which, are effective in the pβCs embryonic development and insulin production and secretion during puberty, including pancreas/duodenum homeobox protein 1 (Pdx1), neuronal differentiation 1 (Neurod1), neurogenin3 (Ngn3), and insulin-1 precursor (Ins1). In this study, a family of new SMs that are structurally similar to glinides was synthesized through three different synthetic methods and categorized into three categories (C1-C3). Then, these novel SMs were characterized by testing their effects on cell viability, pβCs-specific gene expression, and insulin secretion of MIN6 in four different concentrations and three time points. According to our results, SMs of C1 (1j, 1k, and 1l) and two SMs of C3 (1f, 1I), at 200 μM concentration, were able to increase the expression levels of Pdx1, Neurod1, Ngn3, and Ins1 as well as the insulin secretion after 24 hours. However, C2 (1a, 1b, 1c and 1d) did not show significant bio-activity of MIN6 cells. These investigated molecules can provide a tool for exploring pseudo-islet functionality in MIN6 cells or provide a possible basis for future therapeutic interventions for diabetes.

show abstract

Section: Discussionmentioning

confidence: 99%

“…The supernatant was discarded and the pellet was suspended in 2 mL DMEM. Cells were counted and the desired volumes of cells to culture on 24-well plates were prepared for treatment with the selected SMs [Takahashi et al, 2018]. These study protocols were reviewed and approved by the Kharazmi University.…”

Section: Min6 Cell Line Culturingmentioning

confidence: 99%

Synthetic Small Molecules Induce Insulin Secretion and Pancreatic Beta-Cell-Specific Gene Expression

Rabiei¹,

Kalhor²,

Farhadi³

et al. 2022

Cells Tissues Organs

View full text Add to dashboard Cite

show abstract

“…Repaglinide is an important oral insulin secretagogue used to treat type 2 (non-insulin dependent) diabetes mellitus. 1 Scott described that repaglinide has low water solubility, 56% bioavailability and a short half-life but high permeability. Culy & Jarvis 2 mentioned that repaglinide does not always approve a suitable dose regimen due to low bioavailability because of the extensive hepatic metabolism.…”

Section: Introductionmentioning

confidence: 99%

“…Sci. 22 (1): 89-96, 2023 (June) DOI: https://doi.org/10.3329/dujps.v22i1.67099 bioavailability and extended drug delivery has become very essential to obtain optimized drug therapy. Research works have proved that suitable dosage forms can control pharmacokinetics, pharmacodynamics, non-specific toxicity and efficacy of drugs.…”

Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Repaglinide Loaded Liposomes by Ether Injection Method

Sagir

Hamiduzzaman

Dewan

et al. 2023

Dhaka Univ. J. Pharm. Sci

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Repaglinide is a commonly used antidiabetic drug to treat type 2 diabetes mellitus. However, it does not always support a suitable dose regimen due to its low bioavailability and half-life. The purpose of this study was to develop and analyze repaglinide loaded control release liposomes to provide suitable dosage form to treat diabetes. Repaglinide loaded liposomes were prepared by modified ether injection method. According to the USP-II paddle method, in vitro dissolution studies of liposomes were performed for 8 hours in phosphate buffer (pH 7.4). The stability study was executed according to ICH guidelines under three different environmental conditions for 14 days. Additionally, the presence and size of liposomal vesicles was confirmed by microscopic observation. The formulations containing phosphatidylcholine and cholesterol at a molar ratio of 1:0.4 revealed the highest drug entrapment efficiency of 73.1% with an optimum stirring rate of 300 RPM. The pegylated liposomes (PEG400/1500) prolonged the drug loading capacity for the formulations compared to non-pegylated liposomes. On the contrary, the addition of nigella oil caused a decrease in entrapment efficiencies of the liposomes. Most of the formulations followed zero order kinetic model and supper class II release mechanism. In vitro dissolution showed controlled release pattern of the liposomes and maximum drug release after 8 hours was 92.64%. Additionally, all the liposomal formulations were found to be more stable at refrigeration temperature (5 ± 2ºC) where pegylated liposomes were most stable over 14 days at three different environmental conditions. Visual observation under an optical microscope, the vesicular structure of liposomes was confirmed. Dhaka Univ. J. Pharm. Sci. 22(1): 89-96, 2023 (June)

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Improved Bioavailability of Repaglinide by Utilizing Hydrotropy-Solid Dispersing Techniques and Prepared Its Dropping Pills

Liu

Yang

et al. 2022

J Pharm Innov

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Characteristics of repaglinide effects on insulin secretion

Cited by 7 publications

References 35 publications

Synthetic Small Molecules Induce Insulin Secretion and Pancreatic Beta-Cell-Specific Gene Expression

Synthetic Small Molecules Induce Insulin Secretion and Pancreatic Beta-Cell-Specific Gene Expression

Preparation and Evaluation of Repaglinide Loaded Liposomes by Ether Injection Method

Improved Bioavailability of Repaglinide by Utilizing Hydrotropy-Solid Dispersing Techniques and Prepared Its Dropping Pills

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