Cyclodextrins — Useful excipients for oral peptide administration?

Haeberlin, Barbara; Gengenbacher, Thomas; Meinzer, Armin; Fricker, Gert

doi:10.1016/0378-5173(96)04499-7

Cited by 47 publications

(12 citation statements)

References 9 publications

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“…Inclusion of peptides in β-cyclodextrin (β-CD) and hydroxypropyl-β-cyclodextrin (HP- β-CD) cavity resulted in increased chemical and enzymatic stability of these peptides besides improving absorption. The reason for improved absorption may be due to impairment of tight junctional integrity which was observed through enhanced permeation of paracellular marker PEG-4000 (Haeberlin et al, 1996). Cyclodextrins have been shown to enhance chemical and physical stability of peptides and proteins through complexation.…”

Section: Formulation Strategies For Increasing the Oral Bioavailabmentioning

confidence: 99%

Approaches for enhancing oral bioavailability of peptides and proteins

Renukuntla

Vadlapudi

Patel

et al. 2013

International Journal of Pharmaceutics

520

320

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Oral delivery of peptide and protein drugs faces immense challenge partially due to the gastrointestinal (GI) environment. In spite of considerable efforts by industrial and academic laboratories, no major breakthrough in the effective oral delivery of polypeptides and proteins has been accomplished. Upon oral administration, gastrointestinal epithelium acts as a physical and biochemical barrier for absorption of proteins resulting in low bioavailability (typically less than 1–2%). An ideal oral drug delivery system should be capable of a) maintaining the integrity of protein molecules until it reaches the site of absorption, b) releasing the drug at the target absorption site, where the delivery system appends to that site by virtue of specific interaction, and c) retaining inside the gastrointestinal tract irrespective of its transitory constraints. Various technologies have been explored to overcome the problems associated with the oral delivery of macromolecules such as insulin, gonadotropin-releasing hormones, calcitonin, human growth factor, vaccines, enkephalins, and interferons, all of which met with limited success. This review article intends to summarize the physiological barriers to oral delivery of peptides and proteins and novel pharmaceutical approaches to circumvent these barriers and enhance oral bioavailability of these macromolecules.

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Section: Formulation Strategies For Increasing the Oral Bioavailabmentioning

confidence: 99%

Approaches for enhancing oral bioavailability of peptides and proteins

Renukuntla

Vadlapudi

Patel

et al. 2013

International Journal of Pharmaceutics

520

320

View full text Add to dashboard Cite

show abstract

“…It is used for a variety of indications such as acromegaly, gastro-intestinal disorders and psoriasis (Batershill and Clissold, 1989;Prommer, 2008). It has been stabilised against proteolytic degradation in gastrointestinal fluids (Pless et al, 1986) making oral administration feasible (Köhler et al, 1987;Fuessl et al, 1987;Drewe et al, 1993;Fricker et al, 1991;Haeberlin et al, 1996). However, due to low bioavailability (<0.3%) it is only given by intravenous or subcutaneous administration (Arts et al, 2009;Drewe et al, 1993).…”

Section: Introductionmentioning

confidence: 97%

Oral peptide delivery by tetraether lipid liposomes

Parmentier

Thewes²,

Gropp³

et al. 2011

International Journal of Pharmaceutics

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“…We did not have direct data to confirm the potential of loosening the tight junctions for cationic HP-b-CD-PEI polymers used in the present study. However, it has been reported in the previous studies that HP-b-CD significantly enhanced permeation of paracellular marker PEG4000 across the cell monolayers and an impairment of the tight junctional integrity was regarded as one reason for improved peptide absorption (Haeberlin et al, 1996). Additionally, Marttin et al (1997) confirmed the paracellular pathway as major transport route across the nasal respiratory epithelium of a dextran molecule of 3 kDa co-administrated with 2% randomly methylated-b-CD (Marttin et al, 1997).…”

Section: Discussionmentioning

confidence: 93%