In vitro and in vivo evaluations on nanoparticle and phospholipid hybrid nanoparticles with absorption enhancers for oral insulin delivery

2020 ◽  
pp. 1-10
Author(s):  
N. Basaran Mutlu-Agardan ◽  
S. Han
Keyword(s):  
Insulin Delivery ◽  
Hybrid Nanoparticles ◽  
Oral Insulin ◽  
Absorption Enhancers

Efficient oral insulin delivery by dendronized chitosan: in vitro and in vivo studies

RSC Advances ◽  
2014 ◽  
Vol 4 (83) ◽  
pp. 43890-43902 ◽  
Author(s):  
Piyasi Mukhopadhyay ◽  
Kishor Sarkar ◽  
Sourav Bhattacharya ◽  
Roshnara Mishra ◽  
P. P. Kundu
Keyword(s):  
Insulin Delivery ◽  
In Vivo Studies ◽  
Oral Insulin

scholarly journals “Oil-soluble” Reversed Lipid Nanoparticles for Oral Insulin Delivery

2020 ◽  
Author(s):  
Tao Wang ◽  
Dongqin Quan
Keyword(s):  
Oral Absorption ◽  
Insulin Delivery ◽  
Lipid Nanoparticles ◽  
Oral Insulin ◽  
Glucose Levels ◽  
Blood Glucose Levels ◽  
Transmission Electron ◽  
Insulin Solution

Abstract Background In this study, we aimed to design a novel oral insulin delivery system, named “oil-soluble” reversed lipid nanoparticles (ORLN), in which a hydrophilic insulin molecule is encapsulated by a phospholipid (PC) shell and dissolved in oil to prevent the enzymatic degradation of insulin. ORLN was characterized by transmission electron microscopy and dynamic light scattering. Results In vitro enzymatic stability studies showed higher concentrations of insulin in cells incubated with ORLN-encapsulated insulin than in those incubated with free insulin solution in artificial intestinal fluid (pH 6.5). The protective effect of ORLN was attributed to its special release behavior and the formulation of the PC shell and oil barrier. Furthermore, an in vivo oral efficacy study confirmed that blood glucose levels were markedly decreased after ORLN administration in both healthy and diabetic mice. In vivo pharmacokinetic results showed that the bioavailability of ORLN-conjugated insulin was approximately 28.7% relative to that of the group subcutaneously administered with an aqueous solution of insulin, indicating enhanced oral absorption. Conclusions In summary, the ORLN system developed here shows promise as a nanocarrier for improving the oral absorption of insulin.

Oral insulin delivery by self-assembled chitosan nanoparticles: In vitro and in vivo studies in diabetic animal model

2013 ◽  
Vol 33 (1) ◽  
pp. 376-382 ◽  
Author(s):  
Piyasi Mukhopadhyay ◽  
Kishor Sarkar ◽  
Mousumi Chakraborty ◽  
Sourav Bhattacharya ◽  
Roshnara Mishra ◽  
...  
Keyword(s):  
Animal Model ◽  
Chitosan Nanoparticles ◽  
Insulin Delivery ◽  
Diabetic Animal ◽  
In Vivo Studies ◽  
Oral Insulin ◽  
Self Assembled

scholarly journals Oral Insulin Delivery Using Poly (Styrene Co-Maleic Acid) Micelles in a Diabetic Mouse Model

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1026
Author(s):  
Fatemah Bahman ◽  
Sebastien Taurin ◽  
Diab Altayeb ◽  
Safa Taha ◽  
Moiz Bakhiet ◽  
...  
Keyword(s):  
Mouse Model ◽  
Maleic Acid ◽  
Oral Delivery ◽  
Animal Studies ◽  
Ex Vivo ◽  
Insulin Delivery ◽  
Diabetic Mouse ◽  
Oral Insulin

The oral delivery of insulin is a convenient and safe physiological route of administration for management of diabetes mellitus. In this study, we developed a poly-(styrene-co-maleic acid) (SMA) micellar system for oral insulin delivery to overcome the rapid degradation of insulin in the stomach, improve its absorption in the intestine, and provide a physiologically-relevant method of insulin to reach portal circulation. The insulin was encapsulated into SMA micelles in a pH-dependent process. The charge and size of the nanoparticles were determined by dynamic light scattering. The insulin loading of the nanoparticles was measured by HPLC. The transport of the SMA-insulin through biological membranes was assessed in vitro using Caco-2 cells, ex vivo rat intestinal section, and in vivo in a streptozotocin-induced diabetes mouse model. SMA-insulin micelles were negatively charged and had a mean diameter of 179.7 nm. SMA-insulin efficiently stimulated glucose uptake in HepG-2 hepatic cells and was transported across the Caco-2 epithelial cells in vitro by 46% and ex vivo across intestinal epithelium by 22%. The animal studies demonstrated that orally-administered SMA-insulin can produce a hypoglycemic effect up to 3 h after administration of one dose. Overall, our results indicate that SMA micelles are capable of the oral delivery of bioactive compounds like insulin and can be effective tools in the management of diabetes.

scholarly journals Phospholipid complex based nanoemulsion system for oral insulin delivery: preparation, in vitro, and in vivo evaluations

2019 ◽  
Vol Volume 14 ◽  
pp. 3055-3067 ◽  
Author(s):  
Xiong-Bin Hu ◽  
Tian-Tian Tang ◽  
Yong-Jiang Li ◽  
Jun-Yong Wu ◽  
Jie-Min Wang ◽  
...  
Keyword(s):  
Insulin Delivery ◽  
Oral Insulin ◽  
Phospholipid Complex

scholarly journals “Oil-soluble” Reversed Lipid Nanoparticles for Oral Insulin Delivery

2020 ◽  
Author(s):  
Tao Wang ◽  
Liao Shen ◽  
Yadan Zhang ◽  
Haiyan Li ◽  
Yongan Wang ◽  
...  
Keyword(s):  
Oral Absorption ◽  
Insulin Delivery ◽  
Lipid Nanoparticles ◽  
Oral Insulin ◽  
Glucose Levels ◽  
Blood Glucose Levels ◽  
Transmission Electron ◽  
Insulin Solution

Abstract Background: In this study, we aimed to design a novel oral insulin delivery system, named “oil-soluble” reversed lipid nanoparticles (ORLN), in which a hydrophilic insulin molecule is encapsulated by a phospholipid (PC) shell and dissolved in oil to prevent the enzymatic degradation of insulin. ORLN was characterized by transmission electron microscopy and dynamic light scattering. Results: In vitro enzymatic stability studies showed higher concentrations of insulin in cells incubated with ORLN-encapsulated insulin than in those incubated with free insulin solution in artificial intestinal fluid (pH 6.5). The protective effect of ORLN was attributed to its special release behavior and the formulation of the PC shell and oil barrier. Furthermore, an in vivo oral efficacy study confirmed that blood glucose levels were markedly decreased after ORLN administration in both healthy and diabetic mice. In vivo pharmacokinetic results showed that the bioavailability of ORLN-conjugated insulin was approximately 28.7% relative to that of the group subcutaneously administered with an aqueous solution of insulin, indicating enhanced oral absorption.Conclusions: In summary, the ORLN system developed here shows promise as a nanocarrier for improving the oral absorption of insulin.

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