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Development and Evaluation of Liquid and Solid Self-Emulsifying Drug Delivery Systems for Atorvastatin

The objective of this work was to design and characterize liquid and solid self-emulsifying drug delivery systems (SEDDS) for poorly soluble atorvastatin. To optimize the composition of liquid atorvastatin-SEDDS, solubility tests, pseudoternary phase diagrams, emulsification studies and other in vit...

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Autores principales: Czajkowska-Kośnik, Anna, Szekalska, Marta, Amelian, Aleksandra, Szymańska, Emilia, Winnicka, Katarzyna
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6332319/
https://www.ncbi.nlm.nih.gov/pubmed/26610464
http://dx.doi.org/10.3390/molecules201219745
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author Czajkowska-Kośnik, Anna
Szekalska, Marta
Amelian, Aleksandra
Szymańska, Emilia
Winnicka, Katarzyna
author_facet Czajkowska-Kośnik, Anna
Szekalska, Marta
Amelian, Aleksandra
Szymańska, Emilia
Winnicka, Katarzyna
author_sort Czajkowska-Kośnik, Anna
collection PubMed
description The objective of this work was to design and characterize liquid and solid self-emulsifying drug delivery systems (SEDDS) for poorly soluble atorvastatin. To optimize the composition of liquid atorvastatin-SEDDS, solubility tests, pseudoternary phase diagrams, emulsification studies and other in vitro examinations (thermodynamic stability, droplet size and zeta potential analysis) were performed. Due to the disadvantages of liquid SEDDS (few choices for dosage forms, low stability and portability during the manufacturing process), attempts were also made to obtain solid SEDDS. Solid SEDDS were successfully obtained using the spray drying technique from two optimized liquid formulations, CF3 and OF2. Despite liquid SEDDS formulation, CF3 was characterized by lower turbidity, higher percentage transmittance and better self-emulsifying properties, and based on the in vitro dissolution study it can be concluded that better solubilization properties were exhibited by solid formulation OF2. Overall, the studies demonstrated the possibility of formulating liquid and solid SEEDS as promising carriers of atorvastatin. SEDDS, with their unique solubilization properties, provide the opportunity to deliver lipophilic drugs to the gastrointestinal tract in a solubilized state, avoiding dissolution—a restricting factor in absorption rate of BCS Class 2 drugs, including atorvastatin.
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spelling pubmed-63323192019-01-24 Development and Evaluation of Liquid and Solid Self-Emulsifying Drug Delivery Systems for Atorvastatin Czajkowska-Kośnik, Anna Szekalska, Marta Amelian, Aleksandra Szymańska, Emilia Winnicka, Katarzyna Molecules Article The objective of this work was to design and characterize liquid and solid self-emulsifying drug delivery systems (SEDDS) for poorly soluble atorvastatin. To optimize the composition of liquid atorvastatin-SEDDS, solubility tests, pseudoternary phase diagrams, emulsification studies and other in vitro examinations (thermodynamic stability, droplet size and zeta potential analysis) were performed. Due to the disadvantages of liquid SEDDS (few choices for dosage forms, low stability and portability during the manufacturing process), attempts were also made to obtain solid SEDDS. Solid SEDDS were successfully obtained using the spray drying technique from two optimized liquid formulations, CF3 and OF2. Despite liquid SEDDS formulation, CF3 was characterized by lower turbidity, higher percentage transmittance and better self-emulsifying properties, and based on the in vitro dissolution study it can be concluded that better solubilization properties were exhibited by solid formulation OF2. Overall, the studies demonstrated the possibility of formulating liquid and solid SEEDS as promising carriers of atorvastatin. SEDDS, with their unique solubilization properties, provide the opportunity to deliver lipophilic drugs to the gastrointestinal tract in a solubilized state, avoiding dissolution—a restricting factor in absorption rate of BCS Class 2 drugs, including atorvastatin. MDPI 2015-11-25 /pmc/articles/PMC6332319/ /pubmed/26610464 http://dx.doi.org/10.3390/molecules201219745 Text en © 2015 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons by Attribution (CC-BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Czajkowska-Kośnik, Anna
Szekalska, Marta
Amelian, Aleksandra
Szymańska, Emilia
Winnicka, Katarzyna
Development and Evaluation of Liquid and Solid Self-Emulsifying Drug Delivery Systems for Atorvastatin
title Development and Evaluation of Liquid and Solid Self-Emulsifying Drug Delivery Systems for Atorvastatin
title_full Development and Evaluation of Liquid and Solid Self-Emulsifying Drug Delivery Systems for Atorvastatin
title_fullStr Development and Evaluation of Liquid and Solid Self-Emulsifying Drug Delivery Systems for Atorvastatin
title_full_unstemmed Development and Evaluation of Liquid and Solid Self-Emulsifying Drug Delivery Systems for Atorvastatin
title_short Development and Evaluation of Liquid and Solid Self-Emulsifying Drug Delivery Systems for Atorvastatin
title_sort development and evaluation of liquid and solid self-emulsifying drug delivery systems for atorvastatin
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6332319/
https://www.ncbi.nlm.nih.gov/pubmed/26610464
http://dx.doi.org/10.3390/molecules201219745
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