Folate appended chitosan nanoparticles augment the stability, bioavailability and efficacy of insulin in diabetic rats following oral administration

Agrawal, Ashish Kumar; Urimi, Dileep; Harde, Harshad; Kushwah, Varun; Jain, Sanyog

doi:10.1039/c5ra19115g

Cited by 32 publications

(16 citation statements)

References 28 publications

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“…Formulated nanoparticles demonstrated the persistent release of insulin up to 24 h. Encapsulated insulin remained stable both conformationally and chemically. Uptake studies in Caco-2 cell lines deduced remarkably higher effects, so was the bioavailability through oral administration [ 108 ]. Chitosan-EDTA coated (CEC) liposomes encapsulating insulin were synthesized by reverse-phase evaporation method and the shape obtained was either spherical or ellipsoidal.…”

Section: Introductionmentioning

confidence: 99%

Role of capping agents in the application of nanoparticles in biomedicine and environmental remediation: recent trends and future prospects

et al. 2020

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Capping agents are of utmost importance as stabilizers that inhibit the over-growth of nanoparticles and prevent their aggregation/coagulation in colloidal synthesis. The capping ligands stabilize the interface where nanoparticles interact with their medium of preparation. Specific structural features of nanoparticles are attributed to capping on their surface. These stabilizing agents play a key role in altering the biological activities and environmental perspective. Stearic effects of capping agents adsorbed on the surface of nanoparticles are responsible for such changing physico-chemical and biological characteristics. Firstly, this novel review article introduces few frequently used capping agents in the fabrication of nanoparticles. Next, recent advancements in biomedicine and environmental remediation approaches of capped nanoparticles have been elaborated. Lastly, future directions of the huge impact of capping agents on the biological environment have been summarized.

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Section: Introductionmentioning

confidence: 99%

Role of capping agents in the application of nanoparticles in biomedicine and environmental remediation: recent trends and future prospects

et al. 2020

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“…Ligands used for uptake include; vit-amin B 12 , biotin and folate [190]. Researchers have used folate coupled chitosan nanoparticles to further increase the uptake of peptides [191]. Folic acid is actively absorbed in the GI tract by a proton-coupled FA transporter.…”

Section: Nanoparticlesmentioning

confidence: 99%

“…in vitro studies showed a statistically significant improvement in insulin delivery using folate linked nanoparticles, compared to free insulin and chitosan nanoparticles. When these formulations were given to diabetic rats orally, the folate linked nanoparticles resulted in a more sustained decrease in blood glucose compared to compared to free insulin and chitosan nanoparticles [191].…”

Section: Nanoparticlesmentioning

confidence: 99%

Development of METx: A Vasopressin Agonist

Patel¹

2016

Preprint

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Vasopressin (AVP) was one of the first peptides to be extracted and produced synthetically in the early 1950s. Since then AVP and its analogues have been increasingly researched as both AVP agonists and antagonists have therapeutic uses. Although much time and effort has been used to design potent selective AVP agonists and antagonists, very few have reached the market. AVP agonist analogues have only been approved for diabetes insipidus and variceal bleeding. Current main stay treatment for diabetes insipidus is desmopressin, a synthetic analogue of AVP. Desmopressin is well tolerated by the majority of patients, however severe adverse affects, such as hyponatraemia and water intoxication require a strict fluid intake, restricting fluid intake. Our aim is to develop METx for the treatment of diabetes insipidus to help overcome some of the limitations in lifestyle. The solubility and aggregation of METx was measured using the shake flask and pyrene assay respectively. The activity of METx was determined by measuring cAMP production by MDCK cells. The activity of METx was compared to that AVP, the natural agonist of the vasopressin receptor. Formulation studies were performed using GCPQ to create a formulation that could be used subcutaneously or orally. The stability of GCPQ formulations was determined in plasma, simulated gastric fluid (SGF) and rat intestinal wash (RIW). The activity of METx was measured in vivo by monitoring the urine production of rats upon administration of METx intravenously. METx was practically insoluble in aqueous solvents such as water and PBS, with increased solubility in organic solvents. Using TEM imaging aggregation of METx of was seen, the pyrene assay determined the critical micelle concentration to be 27.4mg l-1. METx was found to be a partial agonist of the vasopressin 2 receptor naturally expressed on the MDCK cells, it exhibited a similar EC 50 to AVP. Formulating with GCPQ a ratio of 1:5 (METx:GCPQ) was found to be the most stable in plasma, SGF and RIW. In vivo studies found METx to have a dose dependent reduction in urine production in rats, with 40mg kg-1 rats not producing any urine. The experiments suggest the development of a novel partial agonist of the vasopressin 2 receptor in vitro. The addition of GCPQ results in the formation of nanoparticles, with a ratio of 1:5 (METx:GCPQ) most stable in plasma, SGF and RIW. In vivo experiments resulted in reduced urine production by rats, in a dose responsive manner.

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“…Oral administration of nanoparticles improves bioavailability and hypoglycemia in comparison with insulin solution administered subcutaneously. [6][7][8] In addition, a large proportion of drugs (about 40%) are poorly soluble. Subsequently, the enhancement of their oral bioavailability is the most important challenge in their development.…”

Section: Introductionmentioning

confidence: 99%

Protection of silver nanoparticles using <em>Eysenhardtia polystachya</em> in peroxide-induced pancreatic β-Cell damage and their antidiabetic properties in zebrafish

Campoy¹,

Gutierrez²,

Manriquez-Alvirde³

et al. 2018

IJN

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BackgroundThe aim was to explore the efficacy of extract of Eysenhardtia polystachya-loaded silver nanoparticles (EP/AgNPs) on pancreatic β cells, INS-1 cells, and zebrafish as a valuable model for the study of diabetes mellitus.Materials and methodsEP/AgNPs were synthesized using methanol/water bark extract of E. polystachya and characterized using various physicochemical techniques.ResultsImmersion of adult zebrafish in 111 mM glucose solution resulted in a sustained hyperglycemic, hyperlipidemic state, and serum insulin levels decreased. The synthesized EP/AgNPs showed an absorption peak at 413 nm on ultraviolet–visible spectroscopy, revealing the surface plasmon resonance of the nanoparticles. Transmission electron microscopy indicated that most of the particles were spherical, with a diameter of 10–12 nm, a polydispersity index of 0.197, and a zeta potential of −32.25 mV, suggesting high stability of the nanoparticles. EP/AgNPs promote pancreatic β-cell survival, insulin secretion, enhanced hyperglycemia, and hyperlipidemia in glucose-induced diabetic zebrafish. EP/AgNPs also showed protection of the pancreatic β-cell line INS-1 against hydrogen peroxide-induced oxidative injury.ConclusionThe results indicate that EP/AgNPs have good antidiabetic activity and therefore could be used to prevent the development of diabetes.

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Folate appended chitosan nanoparticles augment the stability, bioavailability and efficacy of insulin in diabetic rats following oral administration

Abstract: The present study embarks upon the folic acid (FA) functionalization of chitosan nanoparticles and its implications on stability, oral bioavailability and hypoglycemic activity following oral administration.

Cited by 32 publications

References 28 publications

Role of capping agents in the application of nanoparticles in biomedicine and environmental remediation: recent trends and future prospects

Role of capping agents in the application of nanoparticles in biomedicine and environmental remediation: recent trends and future prospects

Development of METx: A Vasopressin Agonist

Protection of silver nanoparticles using <em>Eysenhardtia polystachya</em> in peroxide-induced pancreatic β-Cell damage and their antidiabetic properties in zebrafish

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Folate appended chitosan nanoparticles augment the stability, bioavailability and efficacy of insulin in diabetic rats following oral administration

Abstract: The present study embarks upon the folic acid (FA) functionalization of chitosan nanoparticles and its implications on stability, oral bioavailability and hypoglycemic activity following oral administration.

Cited by 32 publications

References 28 publications

Role of capping agents in the application of nanoparticles in biomedicine and environmental remediation: recent trends and future prospects

Role of capping agents in the application of nanoparticles in biomedicine and environmental remediation: recent trends and future prospects

Development of METx: A Vasopressin Agonist

Protection of silver nanoparticles using <em>Eysenhardtia polystachya</em> in peroxide-induced pancreatic &beta;-Cell damage and their antidiabetic properties in zebrafish

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Product

Resources

About

Protection of silver nanoparticles using <em>Eysenhardtia polystachya</em> in peroxide-induced pancreatic β-Cell damage and their antidiabetic properties in zebrafish