ArticleInternational journal of pharmaceutics2008
Improved oral bioavailability and brain transport of Saquinavir upon administration in novel nanoemulsion formulations.
Article in International journal of pharmaceutics, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 49 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
49 citing papers in PubMed, 261 citations in OpenAlex.
- Preparations, Applications, Patents, and Marketed Formulations of Nanoemulsions - A Comprehensive Review.Pharmaceutical nanotechnology · 2026Review
- New PPARα Agonist A190-Loaded Microemulsion for Chemotherapy-Induced Peripheral Neuropathy.Molecular pharmaceutics · 2025Article
- Nanoemulsion: An Emerging Novel Technology for Improving the Bioavailability of Drugs.Scientifica · 2023Review
- Oral drug delivery for immunoengineering.Bioengineering & translational medicine · 2022Review
- Nanomedicine based approaches for combating viral infections.Journal of controlled release : official journal of the Controlled Release Society · 2021Review
- Nanotechnology Interventions in the Management of COVID-19: Prevention, Diagnosis and Virus-Like Particle Vaccines.Vaccines · 2021Review
- Lipid Nanocarriers for Anti-HIV Therapeutics: A Focus on Physicochemical Properties and Biotechnological Advances.Pharmaceutics · 2021Review
- Nanotechnology-based antiviral therapeutics.Drug delivery and translational research · 2021Review
- Nanoemulsion Improves the Neuroprotective Effects of Curcumin in an Experimental Model of Parkinson's Disease.Neurotoxicity research · 2021Article
- Current approaches in lipid-based nanocarriers for oral drug delivery.Drug delivery and translational research · 2021Review
- Critical Review of Lipid-Based Nanoparticles as Carriers of Neuroprotective Drugs and Extracts.Nanomaterials (Basel, Switzerland) · 2021Review
- Nanomedicine for COVID-19: the role of nanotechnology in the treatment and diagnosis of COVID-19.Emergent materials · 2021Review
- Incorporation of docosahexaenoic acid (DHA) enhances nanodelivery of antiretroviral across the blood-brain barrier for treatment of HIV reservoir in brain.Journal of controlled release : official journal of the Controlled Release Society · 2020Article
- Nanosized Cubosomal Thermogelling Dispersion Loaded with Saquinavir Mesylate to Improve Its Bioavailability: Preparation, Optimization, in vitro and in vivo Evaluation.International journal of nanomedicine · 2020Article
- Nanotechnology approaches for delivery of cytochrome P450 substrates in HIV treatment.Expert opinion on drug delivery · 2019Review
- Challenging the CNS Targeting Potential of Systemically Administered Nanoemulsion Delivery Systems: a Case Study with Rapamycin-Containing Fish Oil Nanoemulsions in Mice.Pharmaceutical research · 2019Article
- Nanotechnology approaches to eradicating HIV reservoirs.European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V · 2019Review
- Nanoemulsions for "Nose-to-Brain" Drug Delivery.Pharmaceutics · 2019Review
- Enhancement of saquinavir absorption and accumulation through the formation of solid drug nanoparticles.BMC pharmacology & toxicology · 2018Article
- Nanoemulsion as a strategy for improving the oral bioavailability and anti-inflammatory activity of andrographolide.International journal of nanomedicine · 2018Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
Abstract
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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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.