Oral delivery of an anti-diabetic peptide drug via conjugation and complexation with low molecular weight chitosan

Ahn, Sukyung; Lee, In-Hyun; Lee, Eun‐Hye; Kim, Hyungjun; Kim, Yong-Chul; Jon, Sangyong

doi:10.1016/j.jconrel.2013.05.031

Cited by 55 publications

(27 citation statements)

References 35 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

1,336

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

1,336

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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“…Significant difference from negative physiological saline control (*p50.05; **p50.01) (Xiong et al, 2013). tract is necessary, especially when mucoadhesive systems were used to prolong the residence time (Wong, 2010). Furthermore, potential insulin alternatives, such as psyllium polysaccharides (Singh & Chauhan, 2009), chalcone (Hsieh et al, 2012), glucagon-like peptide-1 (Ahn et al, 2013), can be added to the oral dosage form in order to avoid the risk of insulin overdose. A successful oral insulin delivery system should be biocompatible and biodegradable, keeping the stability of insulin during the absorption, and ultimately improving the bioavailability of insulin.…”

Section: Conclusion and Future Perspectivesmentioning

confidence: 99%

A review of biodegradable polymeric systems for oral insulin delivery

Luo

Xiong

Tian³

et al. 2015

Drug Delivery

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Currently, repeated routine subcutaneous injections of insulin are the standard treatment for insulin-dependent diabetic patients. However, patients' poor compliance for injections often fails to achieve the stable concentration of blood glucose. As a protein drug, the oral bioavailability of insulin is low due to many physiological reasons. Several carriers, such as macromolecules and liposomes have been used to deliver drugs in vivo. In this review article, the gastrointestinal barriers of oral insulin administration are described. Strategies for increasing the bioavailability of oral insulin, such absorption enhancers, enzyme inhibitors, enteric coatings are also introduced. The potential absorption mechanisms of insulin-loaded nanoparticles across the intestinal epithelium, including intestinal lymphatic route, transcellular route and paracellular route are discussed in this review. Natural polymers, such as chitosan and its derivates, alginate derivatives, g-PGA-based materials and starch-based nanoparticles have been exploited for oral insulin delivery; synthetic polymers, such as PLGA, PLA, PCL and PEA have also been developed for oral administration of insulin. This review focuses on recent advances in using biodegradable natural and synthetic polymers for oral insulin delivery along with their future prospects.

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Oral delivery of an anti-diabetic peptide drug via conjugation and complexation with low molecular weight chitosan

Cited by 55 publications

References 35 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

A review of biodegradable polymeric systems for oral insulin delivery

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