ArticleActa pharmacologica Sinica2015
Enhancement of cellular uptake, transport and oral absorption of protease inhibitor saquinavir by nanocrystal formulation.
Article in Acta pharmacologica Sinica, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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17 citing papers in PubMed, 39 citations in OpenAlex.
- Fabrication of Second-Generation Acalabrutinib Nanocrystals by Employing the Nano-Edge Method for Improving the Physico-Chemical Properties and Forecasting their In-Silico Pharmacokinetic Behaviour.AAPS PharmSciTech · 2026Article
- A Dual-Drug Nanosuspension of Bufalin and Quercetin Exhibits Potent Anti-Hepatocellular Carcinoma ActivityCurrent drug delivery · 2026Article
- Review
- Strategies to Enhance Nanocrystal Formulations for Overcoming Physiological Barriers Across Diverse Routes of Administration.International journal of nanomedicine · 2025Review
- Drug Nanocrystals: A Delivery Channel for Antiviral Therapies.AAPS PharmSciTech · 2024Review
- Taste Masking of Promethazine Hydrochloride Using l-Arginine Polyamide-Based Nanocapsules.Molecules (Basel, Switzerland) · 2023Article
- Antiviral role of nanomaterials: a material scientist's perspective.RSC advances · 2022Review
- The Study of Cyclosporin A Nanocrystals Uptake and Transport across an Intestinal Epithelial Cell Model.Polymers · 2022Article
- Nanocrystals for Improving Oral Bioavailability of Drugs: Intestinal Transport Mechanisms and Influencing Factors.AAPS PharmSciTech · 2021Review
- Intracellular uptake of nanocrystals: Probing with aggregation-induced emission of fluorescence and kinetic modeling.Acta pharmaceutica Sinica. B · 2021Article
- Preparation of oridonin nanocrystals and study of their endocytosis and transcytosis behaviours on MDCK polarized epithelial cells.Pharmaceutical biology · 2020Article
- Article
- Nanotechnology approaches for delivery of cytochrome P450 substrates in HIV treatment.Expert opinion on drug delivery · 2019Review
- Nanocrystals: A perspective on translational research and clinical studies.Bioengineering & translational medicine · 2019Review
- Enhancement of saquinavir absorption and accumulation through the formation of solid drug nanoparticles.BMC pharmacology & toxicology · 2018Article
- Co-delivery of docetaxel and silibinin using pH-sensitive micelles improves therapy of metastatic breast cancer.Acta pharmacologica Sinica · 2017Article
- The role of particle size of glyburide crystals in improving its oral absorption.Drug delivery and translational research · 2017Article
Corrections and comments
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Authors and funding
6 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimSaquinavir (SQV) is the first protease inhibitor for the treatment of HIV infection, but with poor solubility. The aim of this study was to prepare a colloidal nanocrystal suspension for improving the oral absorption of SQV.
methodsSQV nanocrystals were prepared using anti-solvent precipitation-high pressure homogenization method. The nanocrystals were characterized by a Zetasizer and transmission electron microscopy (TEM). Their dissolution, cellular uptake and transport across the human colorectal adenocarcinoma cell line (Caco-2) monolayer were investigated. Bioimaging of ex vivo intestinal sections of rats was conducted with confocal laser scanning microscopy. Pharmacokinetic analysis was performed in rats administered nanocrystal SQV suspension (50 mg/kg, ig), and the plasma SQV concentrations were measured with HPLC.
resultsThe SQV nanocrystals were approximately 200 nm in diameter, with a uniform size distribution. The nanocrystals had a rod-like shape under TEM. The dissolution, cellular uptake, and transport across a Caco-2 monolayer of the nanocrystal formulation were significantly improved compared to those of the coarse crystals. The ex vivo intestinal section study revealed that the fluorescently labeled nanocrystals were located in the lamina propria and the epithelium of the duodenum and jejunum. Pharmacokinetic study showed that the maximal plasma concentration (Cmax) was 2.16-fold of that for coarse crystalline SQV suspension, whereas the area under the curve (AUC) of nanocrystal SQV suspension was 1.95-fold of that for coarse crystalline SQV suspension.
conclusionThe nanocrystal drug delivery system significantly improves the oral absorption of saquinavir.
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