ArticleACS omega2025
Physiologically Based Pharmacokinetic Modeling of Efavirenz Nanoparticles: from Animal Model to Human Extrapolation.
Article in ACS omega, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.
What it found
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The trial behind it
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Who cites it
3 citing papers in PubMed.
- Engineering Oral Nanoparticles: Navigating Biological Barriers in the Gastrointestinal Tract.Pharmaceutical research · 2026Review
- Application of New Approach Methodologies to Improve Oral Biopharmaceutic Assessments.Pharmaceutics · 2026Review
- Optimized Milling Approaches for Scalable Production of Ritonavir Nanocrystals: from Process Design to Bioperformance Evaluation.ACS omega · 2026Article
Corrections and comments
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Authors and funding
9 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The present work aims to establish a formulation-specific, physiologically based pharmacokinetic (PBPK) model for efavirenz (EFV) nanocrystals that have shown increased dissolution and were produced following a top-down approach based on wet milling and spray drying by integrating solid-state characterization, in vitro performance, and preclinical pharmacokinetics to enable translational predictions in humans. The resulting material was thoroughly characterized using diffraction-based, spectroscopic, thermal, morphological, and particle sizing techniques, along within vitro dissolution testing and an in vivo pharmacokinetic analysis in rats. Then, a fully rat PBPK model was constructed using GastroPlus and incorporating the biopharmaceutical nanoparticle properties through the product particle size distribution (P-PSD) approach. The physiologically based biopharmaceutics model (PBBM) was validated with rat in vivo data and subsequently extrapolated to simulate human physiology. Compared with unprocessed EFV, nanocrystals exhibited superior dissolution efficiency (90.4% vs 52.6%) and a more homogeneous size distribution. Furthermore, the in vivo studies confirmed an increase in EFV exposure. The rat PBPK model accurately reproduced plasma profiles of both formulations, with all predictive error metrics falling within the acceptable 2-fold range. Extrapolation to human physiology revealed that a 350 mg EFV NC dose achieved systemic exposure comparable to that of standard 600 mg immediate-release tablet, but with faster absorption. Sensitivity analyses highlighted the critical influence of particle size and bile salt solubilization capacity on EFV oral absorption. This study pioneers the application of a fully mechanistic PBPK/PBBM model tailored to nanocrystal formulations of EFV. By bridging preclinical and human data through in silico simulation, the proposed approach supports dose optimization strategies and reinforces the role of nanotechnology in advancing nonbiological complex drug development.
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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.