Study of In Vitro and In Vivo Carbamazepine Release from Coarse and Nanometric Pharmaceutical Emulsions Obtained via Ultra-High-Pressure Homogenization

In the past decade, pharmaceutical nanotechnology has proven to be a promising alternative for improving the physicochemical and biopharmaceutical features for conventional pharmaceutical drug formulations. The goal of this study was to develop, characterize, and evaluate the in vitro and in vivo re...

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Main Authors: Juan D. Echeverri, Maria J. Alhajj, Nicolle Montero, Cristhian J. Yarce, Alvaro Barrera-Ocampo, Constain H. Salamanca
Format: Article
Language:English
Published: MDPI AG 2020-03-01
Series:Pharmaceuticals
Subjects:
Online Access:https://www.mdpi.com/1424-8247/13/4/53
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author Juan D. Echeverri
Maria J. Alhajj
Nicolle Montero
Cristhian J. Yarce
Alvaro Barrera-Ocampo
Constain H. Salamanca
author_facet Juan D. Echeverri
Maria J. Alhajj
Nicolle Montero
Cristhian J. Yarce
Alvaro Barrera-Ocampo
Constain H. Salamanca
author_sort Juan D. Echeverri
collection DOAJ
description In the past decade, pharmaceutical nanotechnology has proven to be a promising alternative for improving the physicochemical and biopharmaceutical features for conventional pharmaceutical drug formulations. The goal of this study was to develop, characterize, and evaluate the in vitro and in vivo release of the model drug carbamazepine (CBZ) from two emulsified formulations with different droplet sizes (coarse and nanometric). Briefly, oil-in-water emulsions were developed using (i) Sacha inchi oil, ultrapure water, Tween<sup>TM</sup> 80, and Span<sup>TM</sup> 80 as surfactants, (ii) methyl-paraben and propyl-paraben as preservatives, and (iii) CBZ as a nonpolar model drug. The coarse and nanometric emulsions were prepared by rotor&#8722;stator dispersion and ultra-high-pressure homogenization (UHPH), respectively. The in vitro drug release studies were conducted by dialysis, whereas the in vivo drug release was evaluated in New Zealand breed rabbits. The results showed that nanoemulsions were physically more stable than coarse emulsions, and that CBZ had a very low release for in vitro determination (&lt;2%), and a release of 20% in the in vivo study. However, it was found that nanoemulsions could significantly increase drug absorption time from 12 h to 45 min.
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spelling doaj.art-bd7aace3ed8942f58cf810b412f7b4ad2022-12-21T23:52:30ZengMDPI AGPharmaceuticals1424-82472020-03-011345310.3390/ph13040053ph13040053Study of In Vitro and In Vivo Carbamazepine Release from Coarse and Nanometric Pharmaceutical Emulsions Obtained via Ultra-High-Pressure HomogenizationJuan D. Echeverri0Maria J. Alhajj1Nicolle Montero2Cristhian J. Yarce3Alvaro Barrera-Ocampo4Constain H. Salamanca5Programa de Maestría en Formulación de Productos Químicos y Derivados, Facultad de Ciencias Naturales, Universidad Icesi, Calle 18 No. 122-135, Cali 76003, ColombiaLaboratorio de Diseño y Formulación de Productos Químicos y Derivados, Facultad de Ciencias Naturales. Universidad Icesi, Calle 18 No. 122-135, Cali 76003, ColombiaLaboratorio de Diseño y Formulación de Productos Químicos y Derivados, Facultad de Ciencias Naturales. Universidad Icesi, Calle 18 No. 122-135, Cali 76003, ColombiaLaboratorio de Diseño y Formulación de Productos Químicos y Derivados, Facultad de Ciencias Naturales. Universidad Icesi, Calle 18 No. 122-135, Cali 76003, ColombiaDepartamento de Ciencias Farmacéuticas, Facultad de Ciencias Naturales, Universidad Icesi, Calle 18 No. 122-135, Cali 76003, ColombiaPrograma de Maestría en Formulación de Productos Químicos y Derivados, Facultad de Ciencias Naturales, Universidad Icesi, Calle 18 No. 122-135, Cali 76003, ColombiaIn the past decade, pharmaceutical nanotechnology has proven to be a promising alternative for improving the physicochemical and biopharmaceutical features for conventional pharmaceutical drug formulations. The goal of this study was to develop, characterize, and evaluate the in vitro and in vivo release of the model drug carbamazepine (CBZ) from two emulsified formulations with different droplet sizes (coarse and nanometric). Briefly, oil-in-water emulsions were developed using (i) Sacha inchi oil, ultrapure water, Tween<sup>TM</sup> 80, and Span<sup>TM</sup> 80 as surfactants, (ii) methyl-paraben and propyl-paraben as preservatives, and (iii) CBZ as a nonpolar model drug. The coarse and nanometric emulsions were prepared by rotor&#8722;stator dispersion and ultra-high-pressure homogenization (UHPH), respectively. The in vitro drug release studies were conducted by dialysis, whereas the in vivo drug release was evaluated in New Zealand breed rabbits. The results showed that nanoemulsions were physically more stable than coarse emulsions, and that CBZ had a very low release for in vitro determination (&lt;2%), and a release of 20% in the in vivo study. However, it was found that nanoemulsions could significantly increase drug absorption time from 12 h to 45 min.https://www.mdpi.com/1424-8247/13/4/53carbamazepinecoarse emulsionin vitro/in vivo drug releasenanoemulsionultra-high-pressure homogenization
spellingShingle Juan D. Echeverri
Maria J. Alhajj
Nicolle Montero
Cristhian J. Yarce
Alvaro Barrera-Ocampo
Constain H. Salamanca
Study of In Vitro and In Vivo Carbamazepine Release from Coarse and Nanometric Pharmaceutical Emulsions Obtained via Ultra-High-Pressure Homogenization
Pharmaceuticals
carbamazepine
coarse emulsion
in vitro/in vivo drug release
nanoemulsion
ultra-high-pressure homogenization
title Study of In Vitro and In Vivo Carbamazepine Release from Coarse and Nanometric Pharmaceutical Emulsions Obtained via Ultra-High-Pressure Homogenization
title_full Study of In Vitro and In Vivo Carbamazepine Release from Coarse and Nanometric Pharmaceutical Emulsions Obtained via Ultra-High-Pressure Homogenization
title_fullStr Study of In Vitro and In Vivo Carbamazepine Release from Coarse and Nanometric Pharmaceutical Emulsions Obtained via Ultra-High-Pressure Homogenization
title_full_unstemmed Study of In Vitro and In Vivo Carbamazepine Release from Coarse and Nanometric Pharmaceutical Emulsions Obtained via Ultra-High-Pressure Homogenization
title_short Study of In Vitro and In Vivo Carbamazepine Release from Coarse and Nanometric Pharmaceutical Emulsions Obtained via Ultra-High-Pressure Homogenization
title_sort study of in vitro and in vivo carbamazepine release from coarse and nanometric pharmaceutical emulsions obtained via ultra high pressure homogenization
topic carbamazepine
coarse emulsion
in vitro/in vivo drug release
nanoemulsion
ultra-high-pressure homogenization
url https://www.mdpi.com/1424-8247/13/4/53
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