Penetration and enzymatic barriers to peptide and protein absorption

Lee, Vincent H.L.; Yamamoto, Akira

doi:10.1016/0169-409x(89)90018-5

Cited by 408 publications

(196 citation statements)

References 185 publications

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“…When biologically active peptides are used clinically in their natural form, their biologic effects are often rapidly lost in vivo due to rapid proteolytic degradation of the active form of the peptide [21]. There is evidence that this cleavage of short peptides may be markedly inhibited by modifications of the Nand C-terminal residues [30].…”

Section: Discussionmentioning

confidence: 99%

“…Computer analysis (Peptide Companion) showed that P60 is likely to fold into an amphipatic helix, although the amphipatic structure is not ideal. Especially, P 21 and T 23 seem to be ''misplaced'', which might be an indication that the C-terminus of P60 is not helical. Replacement of the C-terminal part of P60 (PRTE) by the sequence RPLR was predicted to yield better felicity.…”

Section: Synthetic Peptidesmentioning

confidence: 99%

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Development of novel LL-37 derived antimicrobial peptides with LPS and LTA neutralizing and antimicrobial activities for therapeutic application

et al. 2006

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Section: Discussionmentioning

confidence: 99%

Section: Synthetic Peptidesmentioning

confidence: 99%

Development of novel LL-37 derived antimicrobial peptides with LPS and LTA neutralizing and antimicrobial activities for therapeutic application

et al. 2006

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“…Drug lipophilicity is estimated by determining the drug's octanol-water partition coefficient (Smith et al, 1975;Garcia et al, 2001). Insulin has low lipophilicity with an octanol-water partition coefficient of about 0.0215 (Lee, 1988). Further, the iso-electric point of insulin is around 5 and hence insulin is negatively charged at the neutral pH of the small intestine.…”

Section: Introductionmentioning

confidence: 99%

Confocal microscopic analysis of transport mechanisms of insulin across the cell monolayer

Kavimandan

Peppas

2008

International Journal of Pharmaceutics

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Development of oral insulin formulations would significantly improve the quality of life of patients suffering from diabetes. Complexation hydrogels developed in our laboratory, are one of the most promising classes of materials for use in targeted oral delivery of proteins. Results from confocal microscopy analysis of insulin transport in Caco-2 cells indicated that the primary route of transport was the paracellular pathway and that the transcellular component of the transport was insignificant. In addition, studies with sodium caprate, a model permeation enhancer, showed that using a permeation enhancer with complexation hydrogels may cause permanent damage to the cell monolayer.

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“…However, administration of protein and peptide drug is quite challenging in terms of sustained delivery, targeting formulations and controlled manner. Unlike synthetic pharmaceutical, protein is more sensitive because of their diffusivity and low partition coefficient [1]. Due to these features, proteins may undergo chemical changes, proteolysis and denaturation during passing through the human gut [2,3].…”

Section: Introductionmentioning

confidence: 99%

Development of Alginate–Gum Arabic Beads for Targeted Delivery of Protein

Mohamed¹,

Mustafa²,

Fitrianto³

et al. 2017

J Biomol Res Ther

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Controlled release beads were prepared by using the combination of alginate and gum Arabic through ionotropic gelation method. Bovine serum albumin was used as model protein for in vitro assessments. The effect of amount of sodium alginate and gum Arabic as the factor affecting protein encapsulation efficiency and protein release were optimized and analyzed by using RSM-FCCD. It was observed that protein encapsulation efficiency was increased and protein release was decreased with the increase of both of the amount of sodium alginate and gum Arabic, used as polymer blend. The optimized beads showed high encapsulation efficiency (87.5 ± 3.65%) with suitable protein release (100% protein release after almost 4 hrs). The swelling of beads were highly influenced by pH of dissolution medium. These beads were also characterized by FT-IR spectroscopy, SEM and TA for protein-excipients interaction, beads surface morphology and beads strength, respectively. These calcium alginate/gum Arabic beads have good potential to be used as delivery vehicle for protein drugs.

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Penetration and enzymatic barriers to peptide and protein absorption

Cited by 408 publications

References 185 publications

Development of novel LL-37 derived antimicrobial peptides with LPS and LTA neutralizing and antimicrobial activities for therapeutic application

Development of novel LL-37 derived antimicrobial peptides with LPS and LTA neutralizing and antimicrobial activities for therapeutic application

Confocal microscopic analysis of transport mechanisms of insulin across the cell monolayer

Development of Alginate–Gum Arabic Beads for Targeted Delivery of Protein

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