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3 results on '"VESICLE-BASED BARRIER"'

1. Predicting Oral Absorption of fenofibrate in Lipid-Based Drug Delivery Systems by Combining In Vitro Lipolysis with the Mucus-PVPA Permeability Model

Author

Falavigna, Margherita, Klitgaard, Mette, Berthelsen, Ragna, Muellertz, Anette, Flaten, Goril Eide, Falavigna, Margherita, Klitgaard, Mette, Berthelsen, Ragna, Muellertz, Anette, and Flaten, Goril Eide

Abstract

The aim of this work was to develop a new in vitro lipolysis-permeation model to predict the in vivo absorption of fenofibrate in self-nanoemulsifying drug delivery systems (SNEDDSs). More specifically, the in vitro intestinal lipolysis model was combined with the mucus-PVPA (Phospholipid Vesicle-based Permeation Assay) in vitro permeability model. Biosimilar mucus (BM) was added to the surface of the PVPA barriers to closer simulate the intestinal mucosa. SNEDDSs for which pharmacokinetic data after oral dosing to rats was available in the literature were prepared, and the ability of the SNEDDSs to maintain fenofibrate solubilized during in vitro lipolysis was determined, followed by the assessment of drug permeation across the mucus-PVPA barriers. The amount of drug solubilized over time during in vitro lipolysis did not correlate with the AUC (area under the curve) of the plasma drug concentration curve. However, the AUC of the drug permeated after in vitro lipolysis displayed a good correlation with the in vivo AUC (R-2 > 0.9). Thus, it was concluded that the in vitro lipolysisemucus-PVPA permeation model, simulating the physiological digestion and absorption processes, was able to predict in vivo absorption data, exhibiting great potential for further prediction of in vivo performance of SNEDDSs. (C) 2020 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.

Published
2021

2. Predicting Oral Absorption of fenofibrate in Lipid-Based Drug Delivery Systems by Combining In Vitro Lipolysis with the Mucus-PVPA Permeability Model

Author

Margherita Falavigna, Mette Klitgaard, Gøril Eide Flaten, Ragna Berthelsen, and Anette Müllertz

Subjects
Drug, VIVO PERFORMANCE, Self-emulsifying, media_common.quotation_subject, Lipolysis, Pharmaceutical Science, Administration, Oral, EFFICIENT, 02 engineering and technology, Precipitation, Pharmacology, Poorly water-soluble drug, 030226 pharmacology & pharmacy, Permeability, WATER-SOLUBLE DRUGS, In vitro/in vivo (IVIVC) correlation, 03 medical and health sciences, 0302 clinical medicine, Drug Delivery Systems, Pharmacokinetics, Intestinal mucosa, Fenofibrate, Gastrointestinal tract, In vitro model, VESICLE-BASED BARRIER, medicine, Animals, FORMULATIONS, media_common, Chemistry, VDP::Medical disciplines: 700::Basic medical, dental and veterinary science disciplines: 710::Pharmacology: 728, Area under the curve, PERMEATION ASSAY, Permeation, 021001 nanoscience & nanotechnology, TRANSPORT, Rats, Mucus, Intestinal Absorption, Solubility, Drug delivery, VDP::Medisinske Fag: 700::Basale medisinske, odontologiske og veterinærmedisinske fag: 710::Farmakologi: 728, Oral drug delivery, 0210 nano-technology, medicine.drug, Lipid-based formulation
Abstract

The aim of this work was to develop a new in vitro lipolysis-permeation model to predict the in vivo absorption of fenofibrate in self-nanoemulsifying drug delivery systems (SNEDDSs). More specifically, the in vitro intestinal lipolysis model was combined with the mucus-PVPA (Phospholipid Vesicle-based Permeation Assay) in vitro permeability model. Biosimilar mucus (BM) was added to the surface of the PVPA barriers to closer simulate the intestinal mucosa. SNEDDSs for which pharmacokinetic data after oral dosing to rats was available in the literature were prepared, and the ability of the SNEDDSs to maintain fenofibrate solubilized during in vitro lipolysis was determined, followed by the assessment of drug permeation across the mucus-PVPA barriers. The amount of drug solubilized over time during in vitro lipolysis did not correlate with the AUC (area under the curve) of the plasma drug concentration curve. However, the AUC of the drug permeated after in vitro lipolysis displayed a good correlation with the in vivo AUC (R-2 > 0.9). Thus, it was concluded that the in vitro lipolysisemucus-PVPA permeation model, simulating the physiological digestion and absorption processes, was able to predict in vivo absorption data, exhibiting great potential for further prediction of in vivo performance of SNEDDSs. (C) 2020 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.

Published
2021
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3. Successful oral delivery of poorly water-soluble drugs both depends on the intraluminal behavior of drugs and of appropriate advanced drug delivery systems

Author

Ben J. Boyd, Véronique Préat, Martin Kuentz, Andreas Bernkop-Schnürch, Annette Bauer-Brandl, Anette Müllertz, Patrick Augustijns, Neha Shrestha, Zahari Vinarov, Joachim Brouwers, Christel A. S. Bergström, Martin Brandl, and Vincent Jannin

Subjects
Future studies, Bioavailability, Solid-state, Pharmaceutical Science, Administration, Oral, 02 engineering and technology, 030226 pharmacology & pharmacy, Solid state, Pharmaceutical Sciences, 0302 clinical medicine, Drug Delivery Systems, AMORPHOUS SOLID DISPERSION, Medicine, Pharmacology & Pharmacy, Pharmaceutical sciences, Farmakologi och toxikologi, 021001 nanoscience & nanotechnology, MOLECULAR-DYNAMICS SIMULATION, Pharmaceutical Preparations, Drug delivery, SOLUBILITY-PERMEABILITY INTERPLAY, 0210 nano-technology, Life Sciences & Biomedicine, Poorly water-soluble drugs, medicine.medical_specialty, Pharmacology and Toxicology, Unmet needs, POLYMERIC PRECIPITATION INHIBITORS, HUMAN GASTROINTESTINAL-TRACT, 03 medical and health sciences, VESICLE-BASED BARRIER, Animals, Humans, Intensive care medicine, Science & Technology, Pharmaceutical Preparations/administration & dosage, Lipid formulations, business.industry, HUMAN INTESTINAL FLUIDS, Water, CLASS-II DRUGS, Farmaceutiska vetenskaper, Water soluble, Formulation, Solubility, LIPID-BASED FORMULATIONS, Water/chemistry, IN-VITRO TESTS, Water chemistry, business
Abstract

Poorly water-soluble drugs continue to be a problematic, yet important class of pharmaceutical compounds for treatment of a wide range of diseases. Their prevalence in discovery is still high, and their development is usually limited by our lack of a complete understanding of how the complex chemical, physiological and biochemical processes that occur between administration and absorption individually and together impact on bioavailability. This review defines the challenge presented by these drugs, outlines contemporary strategies to solve this challenge, and consequent in silico and in vitro evaluation of the delivery technologies for poorly water-soluble drugs. The next steps and unmet needs are proposed to present a roadmap for future studies for the field to consider enabling progress in delivery of poorly water-soluble compounds. ispartof: EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES vol:137 ispartof: location:Netherlands status: published

Published
2019
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