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

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          Abstract

          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 TM 80, and Span TM 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–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 (<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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          Oral drug delivery with polymeric nanoparticles: the gastrointestinal mucus barriers.

          Oral delivery is the most common method for drug administration. However, poor solubility, stability, and bioavailability of many drugs make achieving therapeutic levels via the gastrointestinal (GI) tract challenging. Drug delivery must overcome numerous hurdles, including the acidic gastric environment and the continuous secretion of mucus that protects the GI tract. Nanoparticle drug carriers that can shield drugs from degradation and deliver them to intended sites within the GI tract may enable more efficient and sustained drug delivery. However, the rapid secretion and shedding of GI tract mucus can significantly limit the effectiveness of nanoparticle drug delivery systems. Many types of nanoparticles are efficiently trapped in and rapidly removed by mucus, making controlled release in the GI tract difficult. This review addresses the protective barrier properties of mucus secretions, how mucus affects the fate of orally administered nanoparticles, and recent developments in nanoparticles engineered to penetrate the mucus barrier. Copyright © 2011 Elsevier B.V. All rights reserved.
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            On the importance and mechanisms of burst release in matrix-controlled drug delivery systems.

            Although the significance of burst release in controlled delivery systems has not been entirely ignored, no successful theories have been put forth to fully describe the phenomenon. Despite the fact that the fast release of drug in a burst stage is utilized in certain drug administration strategies, the negative effects brought about by burst can be pharmacologically dangerous and economically inefficient. Therefore a thorough understanding of the burst effect in controlled release systems is undoubtedly necessary. In this article, we review experimental observations of burst release in monolithic polymer controlled drug delivery systems, theories of the physical mechanisms causing burst, some of the unique ideas used to prevent burst, and the treatment of burst release in controlled release models.
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              Nanoemulsion: an advanced mode of drug delivery system

              An advanced mode of drug delivery system has been developed to overcome the major drawbacks associated with conventional drug delivery systems. This review gives a detailed idea about a nanoemulsion system. Nanoemulsions are nano-sized emulsions, which are manufactured for improving the delivery of active pharmaceutical ingredients. These are the thermodynamically stable isotropic system in which two immiscible liquids are mixed to form a single phase by means of an emulsifying agent, i.e., surfactant and co-surfactant. The droplet size of nanoemulsion falls typically in the range 20–200 nm. The main difference between emulsion and nanoemulsion lies in the size and shape of particles dispersed in the continuous phase. In this review, the attention is focused to give a basic idea about its formulation, method of preparation, characterization techniques, evaluation parameters, and various applications of nanoemulsion.
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                Author and article information

                Journal
                Pharmaceuticals (Basel)
                Pharmaceuticals (Basel)
                pharmaceuticals
                Pharmaceuticals
                MDPI
                1424-8247
                26 March 2020
                April 2020
                : 13
                : 4
                : 53
                Affiliations
                [1 ]Programa de Maestría en Formulación de Productos Químicos y Derivados, Facultad de Ciencias Naturales, Universidad Icesi, Calle 18 No. 122-135, Cali 76003, Colombia; juandiegoqf@ 123456hotmail.com
                [2 ]Laboratorio de Diseño y Formulación de Productos Químicos y Derivados, Facultad de Ciencias Naturales. Universidad Icesi, Calle 18 No. 122-135, Cali 76003, Colombia; mariajoalhajj@ 123456hotmail.com (M.J.A.); nicollemontero76@ 123456gmail.com (N.M.); cjyarce@ 123456icesi.edu.co (C.J.Y.)
                [3 ]Departamento de Ciencias Farmacéuticas, Facultad de Ciencias Naturales, Universidad Icesi, Calle 18 No. 122-135, Cali 76003, Colombia; aabarrera@ 123456icesi.edu.co
                Author notes
                [* ]Correspondence: chsm70@ 123456gmail.com
                Author information
                https://orcid.org/0000-0001-5390-1409
                https://orcid.org/0000-0002-9179-0997
                https://orcid.org/0000-0003-0675-7365
                https://orcid.org/0000-0003-0906-9293
                https://orcid.org/0000-0003-1587-5371
                Article
                pharmaceuticals-13-00053
                10.3390/ph13040053
                7243108
                32224877
                85d20c32-530b-4fce-a601-65daa392fbaa
                © 2020 by the authors.

                Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license ( http://creativecommons.org/licenses/by/4.0/).

                History
                : 17 February 2020
                : 23 March 2020
                Categories
                Article

                carbamazepine,coarse emulsion,in vitro/in vivo drug release,nanoemulsion,ultra-high-pressure homogenization

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