Tags

Type your tag names separated by a space and hit enter

Organogel Nanoparticles as a New Way to Improve Oral Bioavailability of Poorly Soluble Compounds.
Pharm Res. 2020 May 11; 37(6):92.PR

Abstract

PURPOSE

The aim of the study was to evaluate organogel nanoparticles as a lipophilic vehicle to increase the oral bioavailability of poorly soluble compounds. Efavirenz (EFV), a Biopharmaceutical Classification System (BCS) Class II, was used as drug model.

METHODS

Organogel nanoparticles loaded with EFV were formulated with sunflower oil, 12-hydroxystearic acid (HSA) and polyvinyl alcohol (PVA). Various parameters have been investigated in the current study such as (i) the release profile of organogel assessed by USP 4 cell flow dialysis, (ii) the impact of organogel on intestinal absorption, using Caco-2 cells as in vitro model and jejunum segments as ex vivo assay and (iii) the bioavailability of organogel following oral pharmacokinetic study.

RESULTS

250-300 nm spherical particles with a final concentration of 4.75 mg/mL drug loading were obtained, corresponding to a thousand fold increase in EFV solubility, combined to a very high encapsulation efficiency (>99.8%). Due to rapid diffusion, drug was immediately released from the nanoparticles. The biopharmaceutical evaluation on ex vivo jejunum segments demonstrated an increased absorption of EFV from organogel nanoparticles compare to a native EFV suspension. In vitro assays combining Caco-2 cell cultures with TEM and confocal microscopy demonstrated passive diffusion, while paracellular integrity and endocytosis activity remain expelled. Oral pharmacokinetics of EFV organogel nanoparticles improve oral bioavailability (Fr: 249%) and quick absorption compared to EFV suspension.

CONCLUSION

Organogel nanoparticles increase the bioavailability of BCS Class II drugs. The main phenomena is simply oil transfer from the gelled particles through the cell membrane.

Authors+Show Affiliations

Université de Toulouse, UPS/CNRS, IMRCP, Toulouse, France.Université Clermont Auvergne, INRAE, MEDIS, F-63000, Clermont-Ferrand, France.Université Clermont Auvergne, INRAE, MEDIS, F-63000, Clermont-Ferrand, France. eric.beyssac@uca.fr.Centre de Microscopie Electronique Appliquée à la Biologie, Faculté de Médecine Rangueil, 113 route de Narbonne, 31062, Toulouse Cedex, France.Université de Toulouse, UPS/CNRS, IMRCP, Toulouse, France.Université de Toulouse, UPS/CNRS, IMRCP, Toulouse, France.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32394200

Citation

Martin, Baptiste, et al. "Organogel Nanoparticles as a New Way to Improve Oral Bioavailability of Poorly Soluble Compounds." Pharmaceutical Research, vol. 37, no. 6, 2020, p. 92.
Martin B, Garrait G, Beyssac E, et al. Organogel Nanoparticles as a New Way to Improve Oral Bioavailability of Poorly Soluble Compounds. Pharm Res. 2020;37(6):92.
Martin, B., Garrait, G., Beyssac, E., Goudouneche, D., Perez, E., & Franceschi, S. (2020). Organogel Nanoparticles as a New Way to Improve Oral Bioavailability of Poorly Soluble Compounds. Pharmaceutical Research, 37(6), 92. https://doi.org/10.1007/s11095-020-02808-w
Martin B, et al. Organogel Nanoparticles as a New Way to Improve Oral Bioavailability of Poorly Soluble Compounds. Pharm Res. 2020 May 11;37(6):92. PubMed PMID: 32394200.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Organogel Nanoparticles as a New Way to Improve Oral Bioavailability of Poorly Soluble Compounds. AU - Martin,Baptiste, AU - Garrait,Ghislain, AU - Beyssac,Eric, AU - Goudouneche,Dominique, AU - Perez,Emile, AU - Franceschi,Sophie, Y1 - 2020/05/11/ PY - 2020/01/05/received PY - 2020/03/24/accepted PY - 2020/5/13/entrez KW - Caco-2 KW - Efavirenz KW - drug delivery KW - organogel nanoparticles KW - passive diffusion SP - 92 EP - 92 JF - Pharmaceutical research JO - Pharm. Res. VL - 37 IS - 6 N2 - PURPOSE: The aim of the study was to evaluate organogel nanoparticles as a lipophilic vehicle to increase the oral bioavailability of poorly soluble compounds. Efavirenz (EFV), a Biopharmaceutical Classification System (BCS) Class II, was used as drug model. METHODS: Organogel nanoparticles loaded with EFV were formulated with sunflower oil, 12-hydroxystearic acid (HSA) and polyvinyl alcohol (PVA). Various parameters have been investigated in the current study such as (i) the release profile of organogel assessed by USP 4 cell flow dialysis, (ii) the impact of organogel on intestinal absorption, using Caco-2 cells as in vitro model and jejunum segments as ex vivo assay and (iii) the bioavailability of organogel following oral pharmacokinetic study. RESULTS: 250-300 nm spherical particles with a final concentration of 4.75 mg/mL drug loading were obtained, corresponding to a thousand fold increase in EFV solubility, combined to a very high encapsulation efficiency (>99.8%). Due to rapid diffusion, drug was immediately released from the nanoparticles. The biopharmaceutical evaluation on ex vivo jejunum segments demonstrated an increased absorption of EFV from organogel nanoparticles compare to a native EFV suspension. In vitro assays combining Caco-2 cell cultures with TEM and confocal microscopy demonstrated passive diffusion, while paracellular integrity and endocytosis activity remain expelled. Oral pharmacokinetics of EFV organogel nanoparticles improve oral bioavailability (Fr: 249%) and quick absorption compared to EFV suspension. CONCLUSION: Organogel nanoparticles increase the bioavailability of BCS Class II drugs. The main phenomena is simply oil transfer from the gelled particles through the cell membrane. SN - 1573-904X UR - https://www.unboundmedicine.com/medline/citation/32394200/Organogel_Nanoparticles_as_a_New_Way_to_Improve_Oral_Bioavailability_of_Poorly_Soluble_Compounds L2 - https://doi.org/10.1007/s11095-020-02808-w DB - PRIME DP - Unbound Medicine ER -
Try the Free App:
Prime PubMed app for iOS iPhone iPad
Prime PubMed app for Android
Prime PubMed is provided
free to individuals by:
Unbound Medicine.