Self-emulsifying drug delivery systems in oral (poly)peptide drug delivery

Leonavičiūtė, Gintarė; Bernkop‐Schnürch, Andreas

doi:10.1517/17425247.2015.1068287

Cited by 72 publications

(36 citation statements)

References 82 publications

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“…In simulated physiological fluids, SEDDS form spontaneously transparent and kinetically stable emulsions containing dissolved active pharmaceutical ingredients . Furthermore, SEDDS can protect drugs against the harsh gastrointestinal environment such as acidic pH and enzymatic degradation and improve absorption through gastrointestinal epithelium …”

Section: Introductionmentioning

confidence: 99%

Self-emulsifying drug delivery systems and cationic surfactants: do they potentiate each other in cytotoxicity?

Lam

Le‐Vinh

Phan³

et al. 2018

Journal of Pharmacy and Pharmacology

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Objectives The aim of this study was to evaluate the cytotoxicity of self‐emulsifying drug delivery systems (SEDDS) containing five different cationic surfactants. Methods Cationic surfactants were added in a concentration of 1% and 5% (m/m) to SEDDS comprising 30% Capmul MCM, 30% Captex 355, 30% Cremophor EL and 10% propylene glycol. The resulting formulations were characterized in terms of size, zeta potential, in‐vitro haemolytic activity and toxicity on Caco‐2 via MTT assay and lactate dehydrogenase release assay. Key findings The evaluated surfactants had in both concentrations a minor impact on the size of SEDDS ranging from 30.2 ± 0.6 to 55.4 ± 1.1 nm, whereas zeta potential changed significantly from −9.0 ± 0.3 to +28.8 ± 1.6 mV. The overall cytotoxicity of cationic surfactants followed the rank order: hexadecylpyridinium chloride > benzalkonium chloride > alkyltrimethylammonium bromide > octylamine > 1‐decyl‐3‐methylimidazolium. The haemolytic activity of the combination of cationic surfactants and SEDDS on human red blood cells was synergistic. Furthermore, cationic SEDDS exhibited higher cytotoxicity of Caco‐2 cells compared to SEDDS without cationic surfactants. Conclusions According to these results, SEDDS and cationic surfactants seem to bear an additive up to synergistic toxic risk.

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Section: Introductionmentioning

confidence: 99%

Self-emulsifying drug delivery systems and cationic surfactants: do they potentiate each other in cytotoxicity?

Lam

Le‐Vinh

Phan³

et al. 2018

Journal of Pharmacy and Pharmacology

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“…Oral administration is most preferred because of patient compliance and acceptability . However, the intestinal barrier restricts the absorption of most protein drugs administered orally .…”

Section: Discussionmentioning

confidence: 99%

Intact anti‐LPS IgY is found in the blood after intragastric administration in mice

et al. 2019

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Severe burn injury and cirrhosis often cause the translocation of bacterial endotoxins into blood, leading to systemic damage and even death. Our previous studies have shown that anti‐lipopolysaccharide egg yolk antibody (anti‐LPS IgY) can neutralize bacterial endotoxins in vitro and in vivo effectively, thereby reducing endotoxin damage. Whether anti‐LPS IgY can be absorbed into the blood through the intestinal barrier and neutralize endotoxins in circulation remains unclear. In this study, we used in vivo small animal imaging techniques, protein purification, molecular biology, and mass spectrometry to show that intragastrically administered anti‐LPS IgY is detected in the blood of mice as an intact molecule and has the capacity to bind to LPS. Immunohistochemical analysis confirmed that anti‐LPS IgY is associated with the intestinal mucosa of mice. However, the route of absorption of this large protein molecule was not determined. This study suggests that anti‐LPS IgY can be absorbed into the circulation, with the same molecular mass as purified anti‐LPS IgY as a macromolecular protein, suggesting a new strategy for the prevention of damage caused by endotoxins.

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“…So far, we have focused on passive absorption; however, as alluded to in Figure , there are many barriers that affect oral bioavailability of peptides . In Figure , we highlight these barriers, starting with the peptide in solution and ending with metabolism after absorption, and also identify some specific factors relevant to each barrier.…”

Section: Other Factors Affecting Absorptionmentioning

confidence: 99%

Cyclic peptide oral bioavailability: Lessons from the past

2016

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Achieving high oral bioavailability for drugs is a key design objective in drug development. It is not surprising then that with the growing expectation of peptides as future drugs, there has also been an increasing interest in developing oral peptide therapeutics. Brought to the fore are questions such as what makes peptides orally bioavailable and how this can be achieved; questions which have inspired research into the area for decades. Early research in the area focused on linear peptides with more recent literature focusing on cyclic peptides, motivated in part by cyclic peptides like cyclosporine A that have demonstrated drug-like oral bioavailability. In this review, we take a look at research on the oral bioavailability of peptides, focusing on factors that affect passive permeability. © 2016 Wiley Periodicals, Inc. Biopolymers (Pept Sci) 106: 901-909, 2016.

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Self-emulsifying drug delivery systems in oral (poly)peptide drug delivery

Cited by 72 publications

References 82 publications

Self-emulsifying drug delivery systems and cationic surfactants: do they potentiate each other in cytotoxicity?

Self-emulsifying drug delivery systems and cationic surfactants: do they potentiate each other in cytotoxicity?

Intact anti‐LPS IgY is found in the blood after intragastric administration in mice

Cyclic peptide oral bioavailability: Lessons from the past

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