Chitosan and Chitosan Derivatives as Absorption Enhancers for Peptide Drugs Across Mucosal Epithelia

1999 ◽  
pp. 341-386 ◽  
Author(s):  
A Kotzé ◽  
Henrik Luessen ◽  
M Thanou ◽  
J Verhoef ◽  
A de Boer ◽  
...  
Keyword(s):  
Peptide Drugs ◽  
Absorption Enhancers ◽  
Chitosan Derivatives

The potential of cyclodextrins as absorption enhancers in nasal delivery of peptide drugs

1994 ◽  
Vol 29 (3) ◽  
pp. 351-360 ◽  
Author(s):  
J.Coos Verhoef ◽  
Nicolaas G.M. Schipper ◽  
Stefan G. Romeijn ◽  
Frans W.H.M. Merkus
Keyword(s):  
Nasal Delivery ◽  
Peptide Drugs ◽  
Absorption Enhancers

scholarly journals NMR-Guided Repositioning of Non-Steroidal Anti-Inflammatory Drugs into Tight Junction Modulators

2021 ◽  
Vol 22 (5) ◽  
pp. 2583
Author(s):  
Takeshi Tenno ◽  
Kohki Kataoka ◽  
Natsuko Goda ◽  
Hidekazu Hiroaki
Keyword(s):  
Tight Junction ◽  
Pdz Domain ◽  
Cell Monolayer ◽  
Fluorescein Isothiocyanate ◽  
Flufenamic Acid ◽  
Peptide Drugs ◽  
Absorption Enhancers ◽  
Epithelial Barrier Function ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

Bioavailability is a major bottleneck in the clinical application of medium molecular weight therapeutics, including protein and peptide drugs. Paracellular transport of these molecules is hampered by intercellular tight junction (TJ) complexes. Therefore, safe chemical regulators for TJ loosening are desired. Here, we showed a potential application of select non-steroidal anti-inflammatory drugs (NSAIDs) as TJ modulators. Based on our previous observation that diclofenac and flufenamic acid directly bound various PDZ domains with a broad specificity, we applied solution nuclear magnetic resonance techniques to examine the interaction of other NSAIDs and the first PDZ domain (PDZ1) of zonula occludens (ZO)-1, ZO-1(PDZ1). Inhibition of ZO-1(PDZ1) is expected to provide loosening of the epithelial barrier function because the domain plays a crucial role in maintaining TJ integrity. Accordingly, diclofenac and indomethacin were found to decrease the subcellular localization of claudin (CLD)-2 but not occludin and ZO-1 at the apicolateral intercellular compartment of Madin–Darby canine kidney (MDCK) II cells. These NSAIDs exhibited 125–155% improved paracellular efflux of fluorescein isothiocyanate insulin for the Caco-2 cell monolayer. We propose that these NSAIDs can be repurposed as drug absorption enhancers for peptide drugs.

Conformationally Constrained Peptide Drugs Targeted at the Blood-Brain Barrier

1995 ◽  
Author(s):  
Thomas P. Davis ◽  
Thomas J. Abbruscato ◽  
Elizabeth Brownson ◽  
Victor J. Hruby
Keyword(s):  
Blood Brain Barrier ◽  
Brain Barrier ◽  
Peptide Drugs ◽  
Conformationally Constrained ◽  
Blood Brain

THE BACTERICIDAL PROPERTIES OF CHITOSAN DERIVATIVES TO PROTECT IMPLANTS

2019 ◽  
Vol 0 (2) ◽  
pp. 21-25
Author(s):  
M.A. Guseinova ◽  
◽  
E.V. Salomatina ◽  
L.A. Smirnova ◽  
O.N. Smirnova ◽  
...  
Keyword(s):  
Chitosan Derivatives ◽  
Bactericidal Properties

Role of Nanotechnology in Delivery of Protein and Peptide Drugs

2015 ◽  
Vol 21 (29) ◽  
pp. 4155-4173 ◽  
Author(s):  
Sushilkumar Patil ◽  
Imran Vhora ◽  
Jitendra Amrutiya ◽  
Rohan Lalani ◽  
Ambikanandan Misra
Keyword(s):  
Peptide Drugs

Gastrointestinal Region Specific Insulin Permeation Enhancement by Aloe vera Gel

2020 ◽  
Vol 10 (2) ◽  
pp. 117-122
Author(s):  
Elizca Pretorius ◽  
Clarissa Willers ◽  
Josias H. Hamman ◽  
Johan D. Steyn
Keyword(s):  
Gastrointestinal Tract ◽  
Ex Vivo ◽  
Aloe Vera ◽  
Diffusion Chamber ◽  
Proximal Jejunum ◽  
Absorption Enhancers ◽  
Permeation Enhancement ◽  
Insulin Transport ◽  
Aloe Vera Gel ◽  
Specific Insulin

Background: The oral administration route is still the most preferred by patients for drug treatment, but is unfortunately not suitable for all drug compounds. For example, protein and peptide drugs (e.g. insulin) are typically administered via injection seeing as they are unstable in the gastrointestinal luminal environment and have poor membrane permeation properties. To overcome this problem, functional excipients such as drug absorption enhancers can be co-administered. Although Aloe vera gel has the ability to improve the permeation of drugs across the intestinal epithelium, its drug permeation enhancing effect has not been investigated in the different regions of the gastrointestinal tract yet. Objective: The aim of this study was to investigate the insulin permeation enhancing effects of A. vera gel material across excised pig intestinal tissues from different regions of the gastrointestinal tract and to identify the gastrointestinal region where the highest insulin permeation enhancement was achieved. : Insulin transport across excised pig intestinal tissues from the duodenum, proximal jejunum, medial jejunum, distal jejunum, ileum and colon was measured in the absence and presence of A. vera gel (0.5% w/v) using both the Sweetana-Grass diffusion chamber and everted sac techniques. Results: The insulin permeation results obtained from both ex vivo techniques showed varied permeation enhancing effects of A. vera gel as a function of the different regions of the gastrointestinal tract. The colon was identified as the gastrointestinal region where A. vera gel was the most effective in terms of insulin permeation enhancement in the Sweetana-Grass diffusion chamber technique with a Papp value of 5.50 x 10-7 cm.s-1, whereas the ileum was the region where the highest permeation enhancement occurred in the everted sac technique with a Papp value of 5.45 x 10-7 cm.s-1. Conclusion: The gastrointestinal permeation enhancing effects of A. vera gel on insulin is region specific with the highest effect observed in the ileum and colon.

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