ArticleJournal of colloid and interface science2021
Multidomain drug delivery systems of β-casein micelles for the local oral co-administration of antiretroviral combinations.
Article in Journal of colloid and interface science, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.
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Who cites it
5 citing papers in PubMed.
- Kinetic description of changes in the size of casein microparticles under simulated gastric conditions.Scientific reports · 2025Article
- Review
- Nano drug-delivery systems for management of AIDS: liposomes, dendrimers, gold and silver nanoparticles.Nanomedicine (London, England) · 2023Review
- Casein Micelles as an Emerging Delivery System for Bioactive Food Components.Foods (Basel, Switzerland) · 2021Review
- Challenges and opportunities in delivering oral peptides and proteins.Expert opinion on drug deliveryReview
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Authors and funding
5 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The antiretroviral (ARV) cocktailrevolved the treatment of the human immunodeficiency virus (HIV) infection. Drug combinations have been also tested to treat other infectious diseases, including the recentcoronavirus disease 2019 (COVID-19) outbreak. To simplify administration fixed-dose combinationshave been introduced, however, oral anti-HIV therapy still struggles with low oral bioavailability of many ARVs.This work investigated the co-encapsulation of two clinically relevant ARV combinations,tipranavir (TPV):efavirenz (EFV) anddarunavir (DRV):efavirenz (EFV):ritonavir (RTV),within the core of β-casein (bCN) micelles. Encapsulation efficiency in both systems was ~100%. Cryo-transmission electron microscopy and dynamic light scattering of the ARV-loaded colloidaldispersions indicatefull preservation of the spherical morphology, and x-ray diffraction confirm that the encapsulated drugs are amorphous. To prolong the physicochemical stabilitythe formulations were freeze-driedwithout cryo/lyoprotectant, and successfully redispersed, with minor changes in morphology.Then, theARV-loaded micelles were encapsulated within microparticles of Eudragit® L100, which prevented enzymatic degradation and minimized drug release under gastric-like pH conditionsin vitro. At intestinal pH, the coating polymer dissolved and released the nanocarriers and content. Overall, our results confirm the promise of this flexible and modular technology platform for oral delivery of fixed dose combinations.
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