Novel poloxamer-based nanoemulsions to enhance the intestinal absorption of active compounds
Abstract
On the basis of Pluronic P104 as primary emulsifier and Lauroglycol 90 as amphiphilic oil phase, two nanoemulsion systems were developed with Pluronic((R)) L62 or L81 as secondary emulsifiers. The possible nanoemulsion region of combinations of these excipients was described in ternary phase diagrams. Three formulations were selected from the nanoemulsion region and their potential impact on oral absorption was examined in the Caco-2 monolayer model of the small intestine. The apparent permeability of the BCS class III compound Atenolol was enhanced 2.5-fold, of BCS class II compound Danazol 3.2-fold and of BCS class I compound Metoprolol 1.4-fold. The three formulations were very well tolerated by the Caco-2 cells, which was confirmed by TEER measurements, a MTT test and a LDH release test.
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Common emulsifiers for nanoemulsions include lecithin, sodium deoxycholate, Tween 20/40/60/80, Span 20/40/60/80, poloxamers, sodium dodecyl sulfate, casein, polysaccharides and PEG-containing block copolymers.
“Lecithin (phosphatidylcholine) [36], sodium deoxycholate (bile salt) [37], polyoxyethlene sorbitan monolaurate (Tween 20, 40, 60, 80) [38] and sorbitan monolaurate (Span 20, 40, 60, 80) [39] are commonly employed in the preparation of NEs. Other surfactants proposed are poloxamers [40], sodium dodecyl sulfate [41], amphiphilic proteins like casein [42], polysaccharides (starch derivatives, gums) [”
From Nanoemulsions for “Nose-to-Brain” Drug Delivery (2019) · cites this paper as [40]
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Nanoemulsions: Formation, properties and applications
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Nanoemulsions for “Nose-to-Brain” Drug Delivery
Bonferoni, M. C., Rossi, S., Sandri, G., Ferrari, F., Gavini, E., Rassu, G., & Giunchedi, P. (2019) · Pharmaceutics · doi:10.3390/pharmaceutics11020084 · Cited by 269 · see citing works
- Authors
- BRUSEWITZ, C., SCHENDLER, A., FUNKE, A., WAGNER, T., & LIPP, R.
- Affiliations
- Eli Lilly (United States) (US)
- ORCID
- FUNKE, A
- Venue
- International Journal of Pharmaceutics
- Publisher
- Elsevier BV
- Published
- 2007-02-01
- Volume
- 329
- Issue
- 1-2
- Pages
- 173-181
- ISSN
- 0378-5173 (ISSN-L)
- OpenAlex
- W2090676307
- Cited by
- 86
- References
- 19
- Citations by year
- 2026: 1 · 2025: 1 · 2024: 4 · 2023: 8 · 2022: 6 · 2021: 7 · 2020: 4 · 2019: 3 · 2018: 3 · 2017: 2 · 2016: 6 · 2015: 2 · 2014: 5 · 2013: 6 · 2012: 8
- FWCI
- 1.72
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- International Journal of Pharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Life Sciences › Agricultural and Biological Sciences › Food Science › Proteins in Food Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Keywords
- oral bioavailability enhancement, intestinal absorption, Caco-2 cell monolayers, atenolol, danazol, metoprolol, ternary phase diagram, drug permeability
- MeSH terms
- Danazol, Emulsions, Estrogen Antagonists, Humans, Intestinal Mucosa, Particle Size, Caco-2 Cells, Poloxamer, Nanomedicine
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