Molecular Electrostatic Potentials in the Design of Dendrimers for the Delivery of Glitazones

2006 ◽  
Vol 6 (9) ◽  
pp. 3277-3282 ◽  
Author(s):  
Prasad V. Bharatam ◽  
Sandeep Sundriyal
Keyword(s):  
Type 2 Diabetes ◽  
Drug Delivery ◽  
Hydrogen Bonds ◽  
Ab Initio ◽  
Electrostatic Potential ◽  
Molecular Electrostatic Potentials ◽  
Mo Calculations ◽  
Binding Strength ◽  
Insulin Sensitizers

Glitazones are PPARγ agonistic insulin sensitizers used clinically for the treatment of type-2 diabetes. The delivery of these compounds with the help of dendrimers is possible. Ab initio MO calculations and MESP analysis indicate that the dendrimers with complementary electrostatic potential to glitazones can be designed. The estimated binding strength between one arm of dendrimer and thiazolidinedione is about 15–20 kcal/mol. This binding strength originates from three hydrogen bonds between the dendrimer and each molecule of glitazone. This binding strength is quite suitable for drug encapsulation on the dendrimer based nanoparticles and can be employed for drug delivery.

Efficacy and cardiovascular safety of Thiazolidinediones

2020 ◽  
Vol 15 ◽  
Author(s):  
Raveendran Arkiath Veettil ◽  
Cornelius James Fernandez ◽  
Koshy Jacob
Keyword(s):  
Insulin Resistance ◽  
Type 2 Diabetes ◽  
Cardiovascular Disease ◽  
Glucose Transporter ◽  
Cell Function ◽  
Cardiovascular Safety ◽  
Cardiovascular Outcome Trials ◽  
Glucose Transporter 2 ◽  
Insulin Sensitizers

: Type 2 diabetes mellitus (T2DM) is characterized by a progressive beta cell dysfunction in the setting of peripheral insulin resistance. Insulin resistance in subjects with type 2 diabetes and metabolic syndrome is primarily caused by an ectopic fat accumulation in liver and skeletal muscle. Insulin sensitizers are particularly important in the management of T2DM. Though, thiazolidinediones (TZDs) are principally insulin sensitizers, they possess an ability to preserve pancreatic β-cell function and thereby exhibit durable glycemic control. Cardiovascular outcome trials (CVOTs) have shown that Glucagon-like-peptide 1 receptor agonists (GLP-1 RAs) and sodium glucose transporter-2 inhibitors (SGLT2i) have proven cardiovascular safety. In this era of CVOTs, drugs with proven cardiovascular (CV) safety are often preferred in patients with preexisting cardiovascular disease or at risk of cardiovascular disease. In this review, we will describe the three available drugs belonging to the TZD family, with special emphasis on their efficacy and CV safety.

scholarly journals A Study of Dapagliflozin in Patients With Type 2 Diabetes Receiving High Doses of Insulin Plus Insulin Sensitizers: Applicability of a novel insulin-independent treatment

Diabetes Care ◽  
2009 ◽  
Vol 32 (9) ◽  
pp. 1656-1662 ◽  
Author(s):  
J. P.H. Wilding ◽  
P. Norwood ◽  
C. T'joen ◽  
A. Bastien ◽  
J. F. List ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Insulin Sensitizers ◽  
High Doses

Recent development and advances on the fabrication and biomedical applications of nanoparticles-based drug delivery systems for metformin

2021 ◽  
Author(s):  
Xiaowei Yang ◽  
Qi Lai ◽  
Xinmin Yang ◽  
Banglin Xie ◽  
Bin Zhang ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Drug Delivery ◽  
Biomedical Applications ◽  
Drug Delivery Systems ◽  
Delivery Systems ◽  
Hypoglycemic Agents ◽  
Important Class ◽  
Oral Hypoglycemic Agents

Metformin is an important class of oral hypoglycemic agents for type 2 diabetes via inhibiting gluconeogenesis in liver and increasing the sensitivity of receptor to insulin. It also displayed a...

scholarly journals Synthesis of N-(6-(4-(Piperazin-1-yl)phenoxy)pyridin-3-yl)benzenesulfonamide Derivatives for the Treatment of Metabolic Syndrome

2013 ◽  
Vol 2013 ◽  
pp. 1-10
Author(s):  
Nabajyoti Deka ◽  
Swapnil Bajare ◽  
Jessy Anthony ◽  
Amrutha Nair ◽  
Anagha Damre ◽  
...  
Keyword(s):  
Diabetes Mellitus ◽  
Insulin Resistance ◽  
Type 2 Diabetes ◽  
Cardiovascular Disease ◽  
Metabolic Syndrome ◽  
Type 2 Diabetes Mellitus ◽  
High Plasma ◽  
Insulin Sensitizers ◽  
Increased Risk

Metabolic syndrome is a widely prevalent multifactorial disorder associated with an increased risk of cardiovascular disease and type 2 diabetes mellitus. High plasma levels of insulin and glucose due to insulin resistance are a major component of the metabolic disorder. Thiazolidinediones (TZDs) are potent PPARγ ligand and used as insulin sensitizers in the treatment of type 2 diabetes mellitus. They are potent insulin-sensitizing agents but due to adverse effects like hepatotoxicity, a safer alternative of TZDs is highly demanded. Here we report synthesis of N-(6-(4-(piperazin-1-yl)phenoxy)pyridin-3-yl)benzenesulfonamide derivatives as an alternate remedy for insulin resistance.

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