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Characterization of prototype self-nanoemulsifying formulations of lipophilic compounds

Nielsen, Flemming S.; Gibault, Emilie; Ljusberg, Helena LU ; Arleth, Lise; Pedersen, An Skov and Mullertz, Anette (2007) In Journal of Pharmaceutical Sciences 96(4). p.876-892
Abstract
This study describes the evaluation and characterization of a self-nanoemulsifying drug delivery system (SNEDDS) consisting of a nonionic surfactant (Cremophor RH40), a mixture of long chain mono-, di-, and triacylglycerides (Maisine 35-1 and Sesame oil) and ethanol. Compositions containing 10% (w/w) ethanol, 40%-60% (w/w) lipid content, and 30%-50% (w/w) Cremophor RH40 were identified as pharmaceutically relevant, robust, and self-nanoemulsifying when dispersed in aqueous media. The influence of adding three different lipophilic model drug compounds (danazol, halofantrine, and probucol) to the SNEDDS was evaluated. While danazol precipitated from the SNEDDS after dispersion in aqueous media, halofantrine and procubol remained solubilized.... (More)
This study describes the evaluation and characterization of a self-nanoemulsifying drug delivery system (SNEDDS) consisting of a nonionic surfactant (Cremophor RH40), a mixture of long chain mono-, di-, and triacylglycerides (Maisine 35-1 and Sesame oil) and ethanol. Compositions containing 10% (w/w) ethanol, 40%-60% (w/w) lipid content, and 30%-50% (w/w) Cremophor RH40 were identified as pharmaceutically relevant, robust, and self-nanoemulsifying when dispersed in aqueous media. The influence of adding three different lipophilic model drug compounds (danazol, halofantrine, and probucol) to the SNEDDS was evaluated. While danazol precipitated from the SNEDDS after dispersion in aqueous media, halofantrine and procubol remained solubilized. Halofantrine- and procubol-loaded SNEDDS were evaluated in both saline and in media simulating fasted and fed-state intestinal fluid (FaSSIF and FeSSIF) using dynamic light scattering and small-angle X-ray scattering (SAXS) techniques. Stable nanoemulsions with droplet sizes in the range of 20-50 nm were formed in all media and with and without drugs. The mean size of the droplets was neither affected significantly by being dispersed into the media simulating gastro intestinal fluid, nor by addition of the drug. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
self-emulsifying drug delivery system (SEDDS), scattering (dynamic), light, surfactants, emulsion/microemulsion, formulation vehicle, scattering (SAXS), small-angle X-ray
in
Journal of Pharmaceutical Sciences
volume
96
issue
4
pages
876 - 892
publisher
John Wiley & Sons
external identifiers
  • wos:000245426900014
  • scopus:34247472175
ISSN
0022-3549
DOI
10.1002/jps.20673
language
English
LU publication?
yes
id
570edce1-13d6-4e23-b2c7-ab226172cbdd (old id 668425)
date added to LUP
2007-12-14 14:52:23
date last changed
2017-11-12 03:29:06
@article{570edce1-13d6-4e23-b2c7-ab226172cbdd,
  abstract     = {This study describes the evaluation and characterization of a self-nanoemulsifying drug delivery system (SNEDDS) consisting of a nonionic surfactant (Cremophor RH40), a mixture of long chain mono-, di-, and triacylglycerides (Maisine 35-1 and Sesame oil) and ethanol. Compositions containing 10% (w/w) ethanol, 40%-60% (w/w) lipid content, and 30%-50% (w/w) Cremophor RH40 were identified as pharmaceutically relevant, robust, and self-nanoemulsifying when dispersed in aqueous media. The influence of adding three different lipophilic model drug compounds (danazol, halofantrine, and probucol) to the SNEDDS was evaluated. While danazol precipitated from the SNEDDS after dispersion in aqueous media, halofantrine and procubol remained solubilized. Halofantrine- and procubol-loaded SNEDDS were evaluated in both saline and in media simulating fasted and fed-state intestinal fluid (FaSSIF and FeSSIF) using dynamic light scattering and small-angle X-ray scattering (SAXS) techniques. Stable nanoemulsions with droplet sizes in the range of 20-50 nm were formed in all media and with and without drugs. The mean size of the droplets was neither affected significantly by being dispersed into the media simulating gastro intestinal fluid, nor by addition of the drug.},
  author       = {Nielsen, Flemming S. and Gibault, Emilie and Ljusberg, Helena and Arleth, Lise and Pedersen, An Skov and Mullertz, Anette},
  issn         = {0022-3549},
  keyword      = {self-emulsifying drug delivery system (SEDDS),scattering (dynamic),light,surfactants,emulsion/microemulsion,formulation vehicle,scattering (SAXS),small-angle X-ray},
  language     = {eng},
  number       = {4},
  pages        = {876--892},
  publisher    = {John Wiley & Sons},
  series       = {Journal of Pharmaceutical Sciences},
  title        = {Characterization of prototype self-nanoemulsifying formulations of lipophilic compounds},
  url          = {http://dx.doi.org/10.1002/jps.20673},
  volume       = {96},
  year         = {2007},
}