ArticlePharmaceutical research2013
Improved oral bioavailability of BCS class 2 compounds by self nano-emulsifying drug delivery systems (SNEDDS): the underlying mechanisms for amiodarone and talinolol.
Article in Pharmaceutical research, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
24 citing papers in PubMed, 104 citations in OpenAlex.
- Layer-by-Layer Engineering of Black Seed Oil Based SNEDDSs (BSO-SNEDDSs): Optimizing Chemical Stability and Bioavailability in Ramipril Formulations.International journal of nanomedicine · 2025Article
- Overcoming Solubility Challenges: Self-emulsifying Systems for Enhancing the Delivery of Poorly Water-Soluble Antiviral Drugs.Pharmaceutical nanotechnology · 2025Review
- Optimization of Glibenclamide Loaded Thermoresponsive SNEDDS Using Design of Experiment Approach: Paving the Way to Enhance Pharmaceutical Applicability.Molecules (Basel, Switzerland) · 2024Article
- Article
- Development and Evaluation of Solidified Supersaturated SNEDDS Loaded with Triple Combination Therapy for Metabolic Syndrome.AAPS PharmSciTech · 2024Article
- Strategies to Enhance the Solubility and Bioavailability of Tocotrienols Using Self-Emulsifying Drug Delivery System.Pharmaceuticals (Basel, Switzerland) · 2023Review
- The Influence of the Polymer Type on the Quality of Newly Developed Oral Immediate-Release Tablets Containing Amiodarone Solid Dispersions Obtained by Hot-Melt Extrusion.Molecules (Basel, Switzerland) · 2022Article
- Lipid-Based Nanocarriers for Neurological Disorders: A Review of the State-of-the-Art and Therapeutic Success to Date.Pharmaceutics · 2022Review
- Functional Excipients and Novel Drug Delivery Scenario in Self-nanoemulsifying Drug Delivery System: A Critical Note.Pharmaceutical nanotechnology · 2022Review
- Article
- In Vitro Evaluation of a Solid Supersaturated Self Nanoemulsifying Drug Delivery System (Super-SNEDDS) of Aprepitant for Enhanced Solubility.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Amorphous Form of Carvedilol Phosphate-The Case of Divergent Properties.Molecules (Basel, Switzerland) · 2021Article
- Incorporation of natural assumption to deal with cancer.Environmental science and pollution research international · 2021Review
- Crucial Role of PLGA Nanoparticles in Mitigating the Amiodarone-Induced Pulmonary Toxicity.International journal of nanomedicine · 2021Article
- Neurotropic activity and safety of methylene-cycloalkylacetate (MCA) derivative 3-(3-allyl-2-methylenecyclohexyl) propanoic acid.ACS chemical neuroscience · 2020Article
- Supersaturated LFCS type III self-emulsifying delivery systems of sorafenib tosylate with improved biopharmaceutical performance: QbD-enabled development and evaluation.Drug delivery and translational research · 2020Article
- Recent Advances in Oral Nano-Antibiotics for Bacterial Infection Therapy.International journal of nanomedicine · 2020Review
- Evaluation of Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Poorly Water-Soluble Talinolol: Preparation,Frontiers in pharmacology · 2019Article
- Cannabinoid Delivery Systems for Pain and Inflammation Treatment.Molecules (Basel, Switzerland) · 2018Review
- Self-Emulsifying Granules and Pellets: Composition and Formation Mechanisms for Instant or Controlled Release.Pharmaceutics · 2017Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeSuperior bioavailability of BCS Class 2 compounds incorporated into SNEDDS was previously reported. This study aims to elucidate the underlying mechanisms accountable for this phenomenon.
methodsSNEDDS of amiodarone (AM) and talinolol were developed. Pharmacokinetic parameters were assessed in vivo. Effect on intestinal permeability, P-gp efflux and toxicity was evaluated in vitro (Caco-2) and ex vivo (Ussing). Solubilization was assessed in vitro (Dynamic Lipolysis Model). Effect on intraenterocyte metabolism was evaluated using CYP3A4 microsomes.
resultsOral administration of AM-SNEDDS and talinolol-SNEDDS resulted in higher and less variable AUC and Cmax. In vitro, higher talinolol-SNEDDS Papp indicated Pgp inhibition. Lipolysis of AM-SNEDDS resulted in higher AM concentration in the fraction available for absorption. Incubation of AM-SNEDDS with CYP3A4 indicated CYP inhibition. SNEDDS didn't alter mannitol Papp and TEER. SNEDDS effect was transient.
conclusionsMultiple mechanisms are accountable for improved bioavailability and reduced variability of Class-2 compounds by SNEDDS: increased solubilization, reduced intraenterocyte metabolism and reduced P-gp efflux. SNEDDS effect is reversible and doesn't cause intestinal tissue or cell damage. These comprehensive findings can be used for intelligent selection of drugs for which oral bioavailability will improve upon incorporation into SNEDDS, based on recognition of the drug's absorption barriers and the ability of SNEDDS to overcome them.
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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.