Lectin-mediated bioadhesion: Proteolytic stability and binding-characteristics of wheat germ agglutinin and Solanum tuberosum lectin on Caco-2, HT-29 and human colonocytes

Gabor, Franz; Wirth, Michael; Jurkovich, Barbara; Haberl, Ines; Theyer, Gerhard; Walcher, Gerhard; Hamilton, Gerhard

doi:10.1016/s0168-3659(97)00057-6

Cited by 48 publications

(19 citation statements)

References 20 publications

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“…Previous studies have shown that Caco-2 cells bind WGA and WGA-conjugates. 19,[21][22][23][24] This experiment was done to look at adhesion of functionalized microparticles in an in vitro setting.…”

Section: Resultsmentioning

confidence: 99%

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Wheat Germ Agglutinin Functionalized Complexation Hydrogels for Oral Insulin Delivery

2008

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Insulin was loaded into hydrogel microparticles after two hours with loading efficiencies greater than 70% for both poly(methacrylic acid-grafted-ethylene glycol) (P(MAA-g-EG)) and poly(methacrylic acid-grafted-ethylene glycol) functionalized with wheat germ agglutinin (P(MAA-g-EG) WGA). The pH-responsive release results demonstrated that the pH shift from the stomach to the small intestine can be used as a physiologic trigger to release insulin from P(MAA-g-EG) and P(MAA-g-EG) WGA microparticles, thus limiting release of insulin into the acidic environment of the stomach. Microplates were successfully treated with PGM to create a surface that allowed for specific binding between mucins and lectins. The 1% PGM treatment followed by a 2 h BSA blocking step gave the most consistent results when incubated with F-WGA. In addition, the PGM-treated microplates were shown to create specific interactions between F-WGA and the PGM by use of a competitive carbohydrate. The 1% PGM treated microplates were also used to show that adhesion was improved in the P(MAA-g-EG) WGA microparticles over the P(MAA-g-EG) microparticles. The interaction between the PGM-treated microplate and P(MAA-g-EG) WGA was again shown to be specific by adding a competitive carbohydrate, while the interaction between P(MAA-g-EG) and the PGM-treated microplate was nonspecific. Cellular monolayers were used as another method for demonstrating that the functionalized microparticles increase adhesion over the nonfunctionalized microparticles. This work has focused on improving the mucoadhesive nature of P(MAA-g-EG) by functionalizing these hydrogel carriers with wheat germ agglutinin (WGA) to create a specific mucosal interaction and then evaluating the potential of these carriers as oral insulin delivery systems by in vitro methods. From these studies, it is concluded that the addition of the WGA on the microparticles produces a specific adhesion to carbohydrate-containing surfaces and that P(MAA-g-EG) WGA shows great promise as an oral insulin delivery system.

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Section: Resultsmentioning

confidence: 99%

“…19 Each well of a 96-well plate, pretreated with 0.1, 1, and 10% PGM and blocked with BSA, was incubated with 50 µL of a 40 µg/mL solution of F-WGA in PBS for 1 h at 37°C. After 1 h, 50 µL of a serial dilution of N,N′,N′′-triacetyl-chitotriose (1.0-0.0625 mg/ml) was added to each well and incubated for 1 h at 37°C.…”

Section: Methodsmentioning

confidence: 99%

Wheat Germ Agglutinin Functionalized Complexation Hydrogels for Oral Insulin Delivery

2008

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“…25) Polystyrene microparticules coated with tomato lectin were shown to be specifically adhesive to enterocytes. 26) Tomato lectin is a potential targeting moiety due to its low toxicity and high specificity, but its inactivation due to cross-reactivity with mucus limits its usefulness. The potential of tamato lectin can, however, be tapped by exploiting its cellular uptake for drug delivery.…”

Section: Specific Site Directed Bioadhesives-the Next Generationmentioning

confidence: 99%

Mucoadhesive Microspheres for Controlled Drug Delivery

Chowdary

Rao

2004

Biological & Pharmaceutical Bulletin

155

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Mucoadhesion is a topic of current interest in the design of drug delivery systems. Mucoadhesive microspheres exhibit a prolonged residence time at the site of application or absorption and facilitate an intimate contact with the underlying absorption surface and thus contribute to improved and/or better therapeutic performance of drugs. In recent years such mucoadhesive microspheres have been developed for oral, buccal, nasal, ocular, rectal and vaginal routes for either systemic or local effects. The objective of this article is review the principles underlying the development and evaluation of mucoadhesive microspheres and the research work carried out on these systems.

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“…Lectins are proteins that bind sugar reversibly and are involved in many cell recognition and adhesion processes. They have been extensively adopted to target both absorptive enterocytes and M cells [27]. Wheat germ agglutinin binds (WGA) specifically to cell membranes and is taken up into cells by receptor-mediated endocytosis [28].…”

Section: Solid Lipid Nanoparticles (Sln)mentioning

confidence: 99%

Oral Delivery of Insulin: Novel Approaches

Elsayed¹

2012

Recent Advances in Novel Drug Carrier Systems

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Lectin-mediated bioadhesion: Proteolytic stability and binding-characteristics of wheat germ agglutinin and Solanum tuberosum lectin on Caco-2, HT-29 and human colonocytes

Cited by 48 publications

References 20 publications

Wheat Germ Agglutinin Functionalized Complexation Hydrogels for Oral Insulin Delivery

Wheat Germ Agglutinin Functionalized Complexation Hydrogels for Oral Insulin Delivery

Mucoadhesive Microspheres for Controlled Drug Delivery

Oral Delivery of Insulin: Novel Approaches

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