Development and in vitro Evaluation of Gastro-protective Aceclofenac-loaded Self-emulsifying Drug Delivery System

Chen Jianxian,1,2 Kalsoom Saleem,3 Muhammad Ijaz,4 Masood Ur-Rehman,3 Ghulam Murtaza,4 Mulazim Hussain Asim5 1School of Economics, Capital University of Economics and Business, Beijing, People’s Republic of China; 2Chapter of traditional Chinese Medicine, China Information Industry Associa...

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Autores principales: Jianxian C, Saleem K, Ijaz M, Ur-Rehman M, Murtaza G, Asim MH
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Publicado: Dove Medical Press 2020
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spelling oai:doaj.org-article:6ac3d80fe74e49e18a3277a5e299f2982021-12-02T10:01:48ZDevelopment and in vitro Evaluation of Gastro-protective Aceclofenac-loaded Self-emulsifying Drug Delivery System1178-2013https://doaj.org/article/6ac3d80fe74e49e18a3277a5e299f2982020-07-01T00:00:00Zhttps://www.dovepress.com/development-and-in-vitro-evaluation-of-gastro-protective-aceclofenac-l-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Chen Jianxian,1,2 Kalsoom Saleem,3 Muhammad Ijaz,4 Masood Ur-Rehman,3 Ghulam Murtaza,4 Mulazim Hussain Asim5 1School of Economics, Capital University of Economics and Business, Beijing, People’s Republic of China; 2Chapter of traditional Chinese Medicine, China Information Industry Association, Beijing, China; 3Riphah Institute of Pharmaceutical Sciences, Islamabad, Pakistan; 4COMSATS University Islamabad, Lahore Campus, Lahore 54000, Pakistan; 5Institute of Pharmaceutical Technology, University of Innsbruck, Innsbruck 6020, AustriaCorrespondence: Muhammad IjazLahore Campus, COMSATS University Islamabad, Lahore 54000, PakistanTel +0092-42-99204787Email ijaz_doctor@yahoo.comMasood Ur-RehmanRiphah Institute of Pharmaceutical Sciences, Islamabad, PakistanEmail aarbimasood@gmail.comAim: Chronic use of oral nonsteroidal anti-inflammatory drugs (NSAIDs) is commonly associated with gastric irritation and gastric ulceration. Therefore, the aim of study was to develop a novel oral drug delivery system with minimum gastric effects and improved dissolution rate for aceclofenac (ACF), a model BCS class-II drug.Methods: Self-emulsifying drug delivery systems (SEDDS) were formulated to increase the solubility and ultimately the oral bioavailability of ACF. Oleic acid was used as an oil phase, Tween 80 (T80) and Kolliphor EL (KEL) were used as surfactants, whereas, polyethylene glycol 400 (PEG 400) and propylene glycol (PG) were employed as co-surfactants. Optimized formulations (F1, F2, F3 and F4) were analyzed for droplet size, poly dispersity index (PDI), cell viability studies, in vitro dissolution in both simulated gastric fluid and simulated intestinal fluid, ex vivo permeation studies and thermodynamic stability.Results: The optimized formulations showed mean droplet sizes in the range of 111.3 ± 3.2 nm and 470.9 ± 12.52 nm, PDI from 244.6 nm to 389.4 ± 6.51 and zeta-potential from − 33 ± 4.86 mV to − 38.5 ± 5.15 mV. Cell viability studies support the safety profile of all formulations for oral administration. The in vitro dissolution studies and ex vivo permeation analysis revealed significantly improved drug release ranging from 95.68 ± 0.02% to 98.15 ± 0.71% when compared with control. The thermodynamic stability studies confirmed that all formulations remain active and stable for a longer period.Conclusion: In conclusion, development of oral SEDDS might be a promising tool to improve the dissolution of BCS class-II drugs along with significantly reduced exposure to gastric mucosa.Keywords: self-emulsification, BCS class-II, solubility, gastric irritation, gastro-protective, nano-emulsionJianxian CSaleem KIjaz MUr-Rehman MMurtaza GAsim MHDove Medical Pressarticleself-emulsificationbcs class-iisolubilitygastric irritationgastro-protectivenano-emulsionMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 15, Pp 5217-5226 (2020)
institution DOAJ
collection DOAJ
language EN
topic self-emulsification
bcs class-ii
solubility
gastric irritation
gastro-protective
nano-emulsion
Medicine (General)
R5-920
spellingShingle self-emulsification
bcs class-ii
solubility
gastric irritation
gastro-protective
nano-emulsion
Medicine (General)
R5-920
Jianxian C
Saleem K
Ijaz M
Ur-Rehman M
Murtaza G
Asim MH
Development and in vitro Evaluation of Gastro-protective Aceclofenac-loaded Self-emulsifying Drug Delivery System
description Chen Jianxian,1,2 Kalsoom Saleem,3 Muhammad Ijaz,4 Masood Ur-Rehman,3 Ghulam Murtaza,4 Mulazim Hussain Asim5 1School of Economics, Capital University of Economics and Business, Beijing, People’s Republic of China; 2Chapter of traditional Chinese Medicine, China Information Industry Association, Beijing, China; 3Riphah Institute of Pharmaceutical Sciences, Islamabad, Pakistan; 4COMSATS University Islamabad, Lahore Campus, Lahore 54000, Pakistan; 5Institute of Pharmaceutical Technology, University of Innsbruck, Innsbruck 6020, AustriaCorrespondence: Muhammad IjazLahore Campus, COMSATS University Islamabad, Lahore 54000, PakistanTel +0092-42-99204787Email ijaz_doctor@yahoo.comMasood Ur-RehmanRiphah Institute of Pharmaceutical Sciences, Islamabad, PakistanEmail aarbimasood@gmail.comAim: Chronic use of oral nonsteroidal anti-inflammatory drugs (NSAIDs) is commonly associated with gastric irritation and gastric ulceration. Therefore, the aim of study was to develop a novel oral drug delivery system with minimum gastric effects and improved dissolution rate for aceclofenac (ACF), a model BCS class-II drug.Methods: Self-emulsifying drug delivery systems (SEDDS) were formulated to increase the solubility and ultimately the oral bioavailability of ACF. Oleic acid was used as an oil phase, Tween 80 (T80) and Kolliphor EL (KEL) were used as surfactants, whereas, polyethylene glycol 400 (PEG 400) and propylene glycol (PG) were employed as co-surfactants. Optimized formulations (F1, F2, F3 and F4) were analyzed for droplet size, poly dispersity index (PDI), cell viability studies, in vitro dissolution in both simulated gastric fluid and simulated intestinal fluid, ex vivo permeation studies and thermodynamic stability.Results: The optimized formulations showed mean droplet sizes in the range of 111.3 ± 3.2 nm and 470.9 ± 12.52 nm, PDI from 244.6 nm to 389.4 ± 6.51 and zeta-potential from − 33 ± 4.86 mV to − 38.5 ± 5.15 mV. Cell viability studies support the safety profile of all formulations for oral administration. The in vitro dissolution studies and ex vivo permeation analysis revealed significantly improved drug release ranging from 95.68 ± 0.02% to 98.15 ± 0.71% when compared with control. The thermodynamic stability studies confirmed that all formulations remain active and stable for a longer period.Conclusion: In conclusion, development of oral SEDDS might be a promising tool to improve the dissolution of BCS class-II drugs along with significantly reduced exposure to gastric mucosa.Keywords: self-emulsification, BCS class-II, solubility, gastric irritation, gastro-protective, nano-emulsion
format article
author Jianxian C
Saleem K
Ijaz M
Ur-Rehman M
Murtaza G
Asim MH
author_facet Jianxian C
Saleem K
Ijaz M
Ur-Rehman M
Murtaza G
Asim MH
author_sort Jianxian C
title Development and in vitro Evaluation of Gastro-protective Aceclofenac-loaded Self-emulsifying Drug Delivery System
title_short Development and in vitro Evaluation of Gastro-protective Aceclofenac-loaded Self-emulsifying Drug Delivery System
title_full Development and in vitro Evaluation of Gastro-protective Aceclofenac-loaded Self-emulsifying Drug Delivery System
title_fullStr Development and in vitro Evaluation of Gastro-protective Aceclofenac-loaded Self-emulsifying Drug Delivery System
title_full_unstemmed Development and in vitro Evaluation of Gastro-protective Aceclofenac-loaded Self-emulsifying Drug Delivery System
title_sort development and in vitro evaluation of gastro-protective aceclofenac-loaded self-emulsifying drug delivery system
publisher Dove Medical Press
publishDate 2020
url https://doaj.org/article/6ac3d80fe74e49e18a3277a5e299f298
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