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Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment

Azithromycin (AZM) is a macrolide antibiotic used for the treatment of various bacterial infections. The drug is known to have low oral bioavailability (37%) which may be attributed to its relatively high molecular weight, low solubility, dissolution rate, and incomplete intestinal absorption. To ov...

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Autores principales: Abou Assi, Reem, M. Abdulbaqi, Ibrahim, Seok Ming, Toh, Siok Yee, Chan, A. Wahab, Habibah, Asif, Shaik Mohammed, Darwis, Yusrida
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7693798/
https://www.ncbi.nlm.nih.gov/pubmed/33158058
http://dx.doi.org/10.3390/pharmaceutics12111052
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author Abou Assi, Reem
M. Abdulbaqi, Ibrahim
Seok Ming, Toh
Siok Yee, Chan
A. Wahab, Habibah
Asif, Shaik Mohammed
Darwis, Yusrida
author_facet Abou Assi, Reem
M. Abdulbaqi, Ibrahim
Seok Ming, Toh
Siok Yee, Chan
A. Wahab, Habibah
Asif, Shaik Mohammed
Darwis, Yusrida
author_sort Abou Assi, Reem
collection PubMed
description Azithromycin (AZM) is a macrolide antibiotic used for the treatment of various bacterial infections. The drug is known to have low oral bioavailability (37%) which may be attributed to its relatively high molecular weight, low solubility, dissolution rate, and incomplete intestinal absorption. To overcome these drawbacks, liquid (L) and solid (S) self-emulsifying drug delivery systems (SEDDs) of AZM were developed and optimized. Eight different pseudo-ternary diagrams were constructed based on the drug solubility and the emulsification studies in various SEDDs excipients at different surfactant to co-surfactant (Smix) ratios. Droplet size (DS) < 150 nm, dispersity (Đ) ≤ 0.7, and transmittance (T)% > 85 in three diluents of distilled water (DW), 0.1 mM HCl, and simulated intestinal fluids (SIF) were considered as the selection criteria. The final formulations of L-SEDDs (L-F1((H))), and S-SEDDs (S-F1((H))) were able to meet the selection requirements. Both formulations were proven to be cytocompatible and able to open up the cellular epithelial tight junctions (TJ). The drug dissolution studies showed that after 5 min > 90% and 52.22% of the AZM was released from liquid and solid SEDDs formulations in DW, respectively, compared to 11.27% of the pure AZM, suggesting the developed SEDDs may enhance the oral delivery of the drug. The formulations were stable at refrigerator storage conditions.
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spelling pubmed-76937982020-11-28 Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment Abou Assi, Reem M. Abdulbaqi, Ibrahim Seok Ming, Toh Siok Yee, Chan A. Wahab, Habibah Asif, Shaik Mohammed Darwis, Yusrida Pharmaceutics Article Azithromycin (AZM) is a macrolide antibiotic used for the treatment of various bacterial infections. The drug is known to have low oral bioavailability (37%) which may be attributed to its relatively high molecular weight, low solubility, dissolution rate, and incomplete intestinal absorption. To overcome these drawbacks, liquid (L) and solid (S) self-emulsifying drug delivery systems (SEDDs) of AZM were developed and optimized. Eight different pseudo-ternary diagrams were constructed based on the drug solubility and the emulsification studies in various SEDDs excipients at different surfactant to co-surfactant (Smix) ratios. Droplet size (DS) < 150 nm, dispersity (Đ) ≤ 0.7, and transmittance (T)% > 85 in three diluents of distilled water (DW), 0.1 mM HCl, and simulated intestinal fluids (SIF) were considered as the selection criteria. The final formulations of L-SEDDs (L-F1((H))), and S-SEDDs (S-F1((H))) were able to meet the selection requirements. Both formulations were proven to be cytocompatible and able to open up the cellular epithelial tight junctions (TJ). The drug dissolution studies showed that after 5 min > 90% and 52.22% of the AZM was released from liquid and solid SEDDs formulations in DW, respectively, compared to 11.27% of the pure AZM, suggesting the developed SEDDs may enhance the oral delivery of the drug. The formulations were stable at refrigerator storage conditions. MDPI 2020-11-04 /pmc/articles/PMC7693798/ /pubmed/33158058 http://dx.doi.org/10.3390/pharmaceutics12111052 Text en © 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/).
spellingShingle Article
Abou Assi, Reem
M. Abdulbaqi, Ibrahim
Seok Ming, Toh
Siok Yee, Chan
A. Wahab, Habibah
Asif, Shaik Mohammed
Darwis, Yusrida
Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment
title Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment
title_full Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment
title_fullStr Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment
title_full_unstemmed Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment
title_short Liquid and Solid Self-Emulsifying Drug Delivery Systems (SEDDs) as Carriers for the Oral Delivery of Azithromycin: Optimization, In Vitro Characterization and Stability Assessment
title_sort liquid and solid self-emulsifying drug delivery systems (sedds) as carriers for the oral delivery of azithromycin: optimization, in vitro characterization and stability assessment
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7693798/
https://www.ncbi.nlm.nih.gov/pubmed/33158058
http://dx.doi.org/10.3390/pharmaceutics12111052
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