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Improved oral bioavailability and brain transport of Saquinavir upon administration in novel nanoemulsion formulations
Open accessAbstract
The aim of this investigation was to develop novel oil-in-water (o/w) nanoemulsions containing Saquinavir (SQV), an anti-HIV protease inhibitor, for enhanced oral bioavailability and brain disposition. SQV was dissolved in different types of edible oils rich in essential polyunsaturated fatty acids (PUFA) to constitute the internal oil phase of the nanoemulsions. The external phase consisted of surfactants Lipoid-80 and deoxycholic acid dissolved in water. The nanoemulsions with an average oil droplet size of 100-200 nm, containing tritiated [(3)H]-SQV, were administered orally and intravenously to male Balb/c mice. The SQV bioavailability as well as distribution in different organ systems was examined. SQV concentrations in the systemic circulation administered in flax-seed oil nanoemulsions were threefold higher as compared to the control aqueous suspension. The oral bioavailability and distribution to the brain, a potential sanctuary site for HIV, were significantly enhanced with SQV delivered in nanoemulsion formulations. In comparing SQV in flax-seed oil nanoemulsion with aqueous suspension, the maximum concentration (C(max)) and the area-under-the-curve (AUC) values were found to be five- and threefold higher in the brain, respectively, suggesting enhanced rate and extent of SQV absorption following oral administration of nanoemulsions. The results of this study show that oil-in-water nanoemulsions made with PUFA-rich oils may be very promising for HIV/AIDS therapy, in particular, for reducing the viral load in important anatomical reservoir sites.
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“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 [37]
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Background
Metadata
- Authors
- Vyas, T. K., Shahiwala, A., & Amiji, M. M.
- Affiliations
- Northeastern University (US)
- Corresponding author
- Amiji, Mansoor M.
- Venue
- International Journal of Pharmaceutics
- Publisher
- Elsevier BV
- Published
- 2008-01
- Volume
- 347
- Issue
- 1-2
- Pages
- 93-101
- ISSN
- 0378-5173 (ISSN-L)
- PMC
- PMC2213794
- OpenAlex
- W2069726112
- Cited by
- 264
- References
- 25
- Citations by year
- 2026: 1 · 2025: 8 · 2024: 5 · 2023: 8 · 2022: 8 · 2021: 18 · 2020: 18 · 2019: 18 · 2018: 22 · 2017: 19 · 2016: 23 · 2015: 16 · 2014: 16 · 2013: 23 · 2012: 21
- FWCI
- 5.44
- Type
- journal article
- Language
- en
- Open access
- green
- www.ncbi.nlm.nih.gov
- Locations
- International Journal of Pharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- PubMed Central (acceptedVersion)
- Funders
- National Cancer Institute (R01CA119617)
- 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
- saquinavir, nanoemulsions, oral bioavailability, brain distribution, HIV protease inhibitors, polyunsaturated fatty acids, linseed oil, deoxycholic acid, drug absorption, HIV/AIDS treatment, drug delivery
- MeSH terms
- Sunflower Oil, Administration, Oral, Animals, Biological Availability, Brain, Deoxycholic Acid, Emulsions, Injections, Intravenous, Linseed Oil, Male, Mice, Inbred BALB C, Particle Size, Phosphatidylcholines, Plant Oils, Sonication, Surface Properties, HIV Protease Inhibitors, Saquinavir, Area Under Curve, Nanotechnology, Microscopy, Electron, Transmission, Mice, Static Electricity
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