In vivo evaluation of an oral drug delivery system for peptides based on S-protected thiolated chitosan

Dünnhaupt, Sarah; Barthelmes, Jan; Iqbal, Javed; Perera, Glen; Thurner, Clemens C.; Friedl, Heike; Bernkop‐Schnürch, Andreas

doi:10.1016/j.jconrel.2012.04.020

Cited by 41 publications

(22 citation statements)

References 27 publications

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“…The screening of a large library of chemicals and chemical mixtures to identify compositions that enhance the uptake of peptides and proteins 120 led to the identification of the zwitterionic surfactant dimethyl palmitoyl ammonio propanesulphonate (PPS), which enhanced the intestinal permeation of calcitonin in mice 121 . Other methods of increasing absorption include pH-sensitive hydrogels to protect the drug from low pH in the stomach 122 , chitosans 123 and chitosan derivatives 124 to induce mucoadhesion of the drug carrier and increase intestinal permeation, and acrylate-based polymers to increase mucoadhesion 125 .…”

Section: Alternative Routes Of Drug Deliverymentioning

confidence: 99%

Overcoming the challenges in administering biopharmaceuticals: formulation and delivery strategies

Mitragotri

Burke

Langer

2014

Nat Rev Drug Discov

1,306

1,037

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The formulation and delivery of biopharmaceutical drugs, such as monoclonal antibodies and recombinant proteins, poses substantial challenges owing to their large size and susceptibility to degradation. In this Review we highlight recent advances in formulation and delivery strategies — such as the use of microsphere-based controlled-release technologies, protein modification methods that make use of polyethylene glycol and other polymers, and genetic manipulation of biopharmaceutical drugs — and discuss their advantages and limitations. We also highlight current and emerging delivery routes that provide an alternative to injection, including transdermal, oral and pulmonary delivery routes. In addition, the potential of targeted and intracellular protein delivery is discussed.

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Section: Alternative Routes Of Drug Deliverymentioning

confidence: 99%

Overcoming the challenges in administering biopharmaceuticals: formulation and delivery strategies

Mitragotri

Burke

Langer

2014

Nat Rev Drug Discov

1,306

1,037

View full text Add to dashboard Cite

show abstract

“…Among these materials, chitosan has been highly utilized in a number of oral drug delivery systems, including chitosan-based micro- and nanoparticulate drug delivery systems [89–94], chitosan-drug conjugates [95, 96], and chitosan macroscale patches [97, 98]. Chitosan is an attractive material for micro/nanofabricated platforms as it is compatible with a number of microfabrication approaches [99, 100], is stable through pH values relevant to GI physiology [101], and has been utilized in microfabricated oral drug delivery systems [58, 102].…”

Section: Strategies To Increase Micro/nanofabricated Oral Drug Delmentioning

confidence: 99%

Micro/nanofabricated platforms for oral drug delivery

Fox

Kim

et al. 2015

Journal of Controlled Release

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The oral route of drug administration is most preferred due to its ease of use, low cost, and high patient compliance. However, the oral uptake of many small molecule drugs and biotherapeutics is limited by various physiological barriers, and, as a result, drugs suffer from issues with low solubility, low permeability, and degradation following oral administration. The flexibility of micro- and nanofabrication techniques has been used to create drug delivery platforms designed to address these barriers to oral drug uptake. Specifically, micro/nanofabricated devices have been designed with planar, asymmetric geometries to promote device adhesion and unidirectional drug release toward epithelial tissue, thereby prolonging drug exposure and increasing drug permeation. Furthermore, surface functionalization, nanotopography, responsive drug release, motion-based responses, and permeation enhancers have been incorporated into such platforms to further enhance drug uptake. This review will outline the application of micro/nanotechnology to specifically address the physiological barriers to oral drug delivery and highlight technologies that may be incorporated into these oral drug delivery systems to further enhance drug uptake.

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“…In the second step, the thiol group of thiolated chitosan was protected by the formation of disulfide bonds with aromatic thiol-bearing ligands. The S-protected thiolated chitosan exhibited improved mucoadhesivity, enhanced permeation effect, inhibited efflux pump, bioavailability, and controlled release profile compared to the corresponding thiolated and unmodified polymers, 109,127,128 demonstrating that TCMs prepared using S-protected thiolated chitosan are a promising chitosan-based mucoadhesive polymer for the development of various mucosal vaccine delivery systems.…”

Section: Thiolated Cms As a Modified And Improved Form Of A Chitosanbmentioning

confidence: 98%

“…126 Recently, Bernkop-Schnurch et al performed several studies using aromatic thiol-bearing ligands for the synthesis of S-protected thiolated chitosan and evaluated their efficacy as mucosal drug delivery carriers. 109,127,128 To prepare the S-protected thiolated chitosan, the thiol-bearing ligand was covalently attached to chitosan as the first step of modification. In the second step, the thiol group of thiolated chitosan was protected by the formation of disulfide bonds with aromatic thiol-bearing ligands.…”

Section: Thiolated Cms As a Modified And Improved Form Of A Chitosanbmentioning

confidence: 99%

Design and application of chitosan microspheres as oral and nasal vaccine carriers: an updated review

Islam¹,

Firdous²,

Choi³

et al. 2012

IJN

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Chitosan, a natural biodegradable polymer, is of great interest in biomedical research due to its excellent properties including bioavailability, nontoxicity, high charge density, and mucoadhesivity, which creates immense potential for various pharmaceutical applications. It has gelling properties when it interacts with counterions such as sulfates or polyphosphates and when it crosslinks with glutaraldehyde. This characteristic facilitates its usefulness in the coating or entrapment of biochemicals, drugs, antigenic molecules as a vaccine candidate, and microorganisms. Therefore, chitosan together with the advance of nanotechnology can be effectively applied as a carrier system for vaccine delivery. In fact, chitosan microspheres have been studied as a promising carrier system for mucosal vaccination, especially via the oral and nasal route to induce enhanced immune responses. Moreover, the thiolated form of chitosan is of considerable interest due to its improved mucoadhesivity, permeability, stability, and controlled/extended release profile. This review describes the various methods used to design and synthesize chitosan microspheres and recent updates on their potential applications for oral and nasal delivery of vaccines. The potential use of thiolated chitosan microspheres as next-generation mucosal vaccine carriers is also discussed.

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In vivo evaluation of an oral drug delivery system for peptides based on S-protected thiolated chitosan

Cited by 41 publications

References 27 publications

Overcoming the challenges in administering biopharmaceuticals: formulation and delivery strategies

Overcoming the challenges in administering biopharmaceuticals: formulation and delivery strategies

Micro/nanofabricated platforms for oral drug delivery

Design and application of chitosan microspheres as oral and nasal vaccine carriers: an updated review

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