Self-nanoemulsifying ramipril tablets: a novel delivery system for the enhancement of drug dissolution and stability

Khalid F Alhasani,1 Mohsin Kazi,1,2 Mohamed Abbas Ibrahim,1 Ahmad A Shahba,1,2 Fars K Alanazi1,21Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Kingdom of Saudi Arabia; 2Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics,...

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Autores principales: Alhasani KF, Kazi M, Ibrahim MA, Shahba AA, Alanazi FK
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Publicado: Dove Medical Press 2019
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spelling oai:doaj.org-article:39ecfdfefa5e45c1b19c1a7f42204abe2021-12-02T09:32:15ZSelf-nanoemulsifying ramipril tablets: a novel delivery system for the enhancement of drug dissolution and stability1178-2013https://doaj.org/article/39ecfdfefa5e45c1b19c1a7f42204abe2019-07-01T00:00:00Zhttps://www.dovepress.com/self-nanoemulsifying-ramipril-tablets-a-novel-delivery-system-for-the--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Khalid F Alhasani,1 Mohsin Kazi,1,2 Mohamed Abbas Ibrahim,1 Ahmad A Shahba,1,2 Fars K Alanazi1,21Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Kingdom of Saudi Arabia; 2Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Kingdom of Saudi ArabiaBackground: Ramipril (RMP) suffers from poor aqueous solubility along with sensitivity to mechanical stress, heat, and moisture. The aim of the current study is to improve RMP solubility and stability by designing solid self-nanoemulsifying drug delivery system (S-SNEDDS) as tablet.Methods: The drug was initially incorporated in different liquid formulations (L-SNEDDS) which were evaluated by equilibrium solubility, droplet size, and zeta potential studies. The optimized formulation was solidified into S-SNEDDS powder by the adsorbent Syloid® and compressed into a self-nanoemulsifying tablet (T-SNEDDS). The optimized tablet was evaluated by drug content uniformity, hardness, friability, disintegration, and dissolution tests. Furthermore, pure RMP, optimized L-SNEDDS, and T-SNEDDS were enrolled in accelerated and long-term stability studies.Results: Among various liquid formulations, F5 L-SNEDDS [capmul MCM/transcutol/HCO-30 (25/25/50%w/w)] showed relatively high drug solubility, nano-scaled droplet size, and high negative zeta potential value. The optimized SNEDDS solidification with Syloid® at ratio (1:1) resulted in a compressible powder with an excellent flowability. The optimized tablet (T-SNEDDS) showed accepted content uniformity, hardness, friability, and disintegration time (<15 minutes). The optimized L-SNEDDS, S-SNEDDS, and T-SNEDDS showed superior enhancement of RMP dissolution compared to the pure drug. Most importantly, T-SNEDDS showed significant (P<0.05) improvement of RMP stability compared to the pure drug and L-SNEDDS in both accelerated and long-term stability studies.Conclusion: RMP-loaded T-SNEDDS offers a potential oral dosage form that provides combined improvement of RMP dissolution and chemical stability.Keywords: solid self-nanoemulsifying drug delivery systems (S-SNEDDS), self-nanoemulsifying tablets, ramipril, dissolution improvement, stability studiesAlhasani KFKazi MIbrahim MAShahba AAAlanazi FKDove Medical PressarticleSolid self-nanoemulsifying drug delivery systems (S-SNEDDS)self-nanoemulsifying tabletsramiprildissolution improvementstability studies.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 5435-5448 (2019)
institution DOAJ
collection DOAJ
language EN
topic Solid self-nanoemulsifying drug delivery systems (S-SNEDDS)
self-nanoemulsifying tablets
ramipril
dissolution improvement
stability studies.
Medicine (General)
R5-920
spellingShingle Solid self-nanoemulsifying drug delivery systems (S-SNEDDS)
self-nanoemulsifying tablets
ramipril
dissolution improvement
stability studies.
Medicine (General)
R5-920
Alhasani KF
Kazi M
Ibrahim MA
Shahba AA
Alanazi FK
Self-nanoemulsifying ramipril tablets: a novel delivery system for the enhancement of drug dissolution and stability
description Khalid F Alhasani,1 Mohsin Kazi,1,2 Mohamed Abbas Ibrahim,1 Ahmad A Shahba,1,2 Fars K Alanazi1,21Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Kingdom of Saudi Arabia; 2Kayyali Chair for Pharmaceutical Industries, Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Kingdom of Saudi ArabiaBackground: Ramipril (RMP) suffers from poor aqueous solubility along with sensitivity to mechanical stress, heat, and moisture. The aim of the current study is to improve RMP solubility and stability by designing solid self-nanoemulsifying drug delivery system (S-SNEDDS) as tablet.Methods: The drug was initially incorporated in different liquid formulations (L-SNEDDS) which were evaluated by equilibrium solubility, droplet size, and zeta potential studies. The optimized formulation was solidified into S-SNEDDS powder by the adsorbent Syloid® and compressed into a self-nanoemulsifying tablet (T-SNEDDS). The optimized tablet was evaluated by drug content uniformity, hardness, friability, disintegration, and dissolution tests. Furthermore, pure RMP, optimized L-SNEDDS, and T-SNEDDS were enrolled in accelerated and long-term stability studies.Results: Among various liquid formulations, F5 L-SNEDDS [capmul MCM/transcutol/HCO-30 (25/25/50%w/w)] showed relatively high drug solubility, nano-scaled droplet size, and high negative zeta potential value. The optimized SNEDDS solidification with Syloid® at ratio (1:1) resulted in a compressible powder with an excellent flowability. The optimized tablet (T-SNEDDS) showed accepted content uniformity, hardness, friability, and disintegration time (<15 minutes). The optimized L-SNEDDS, S-SNEDDS, and T-SNEDDS showed superior enhancement of RMP dissolution compared to the pure drug. Most importantly, T-SNEDDS showed significant (P<0.05) improvement of RMP stability compared to the pure drug and L-SNEDDS in both accelerated and long-term stability studies.Conclusion: RMP-loaded T-SNEDDS offers a potential oral dosage form that provides combined improvement of RMP dissolution and chemical stability.Keywords: solid self-nanoemulsifying drug delivery systems (S-SNEDDS), self-nanoemulsifying tablets, ramipril, dissolution improvement, stability studies
format article
author Alhasani KF
Kazi M
Ibrahim MA
Shahba AA
Alanazi FK
author_facet Alhasani KF
Kazi M
Ibrahim MA
Shahba AA
Alanazi FK
author_sort Alhasani KF
title Self-nanoemulsifying ramipril tablets: a novel delivery system for the enhancement of drug dissolution and stability
title_short Self-nanoemulsifying ramipril tablets: a novel delivery system for the enhancement of drug dissolution and stability
title_full Self-nanoemulsifying ramipril tablets: a novel delivery system for the enhancement of drug dissolution and stability
title_fullStr Self-nanoemulsifying ramipril tablets: a novel delivery system for the enhancement of drug dissolution and stability
title_full_unstemmed Self-nanoemulsifying ramipril tablets: a novel delivery system for the enhancement of drug dissolution and stability
title_sort self-nanoemulsifying ramipril tablets: a novel delivery system for the enhancement of drug dissolution and stability
publisher Dove Medical Press
publishDate 2019
url https://doaj.org/article/39ecfdfefa5e45c1b19c1a7f42204abe
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