Self-nanoemulsifying drug-delivery systems for potentiated anti-inflammatory activity of diacerein

Amal Ahmed Eltobshi,1 Elham Abdelmonem Mohamed,2 Galal Mahmoud Abdelghani,2 Ahmed Talaat Nouh3 1Department of Pharmaceutical Technology, Faculty of Pharmacy, Horus University, New Damietta 34517, Egypt; 2Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt; 3...

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Autores principales:	Eltobshi AA, Mohamed EA, Abdelghani GM, Nouh AT
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2018
Materias:	diacerein Gelucire 44/14 D-α-tocopheryl polyethylene glycol 1000 succinate self-nanoemulsifying drug delivery systems anti-inflammatory activity paw edema Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/c4f3015e36344805b2b3a26260c62f23
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spelling	oai:doaj.org-article:c4f3015e36344805b2b3a26260c62f232021-12-02T09:13:04ZSelf-nanoemulsifying drug-delivery systems for potentiated anti-inflammatory activity of diacerein1178-2013https://doaj.org/article/c4f3015e36344805b2b3a26260c62f232018-10-01T00:00:00Zhttps://www.dovepress.com/self-nanoemulsifying-drug-delivery-systems-for-potentiated-anti-inflam-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Amal Ahmed Eltobshi,1 Elham Abdelmonem Mohamed,2 Galal Mahmoud Abdelghani,2 Ahmed Talaat Nouh3 1Department of Pharmaceutical Technology, Faculty of Pharmacy, Horus University, New Damietta 34517, Egypt; 2Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt; 3Department of Pharmaceutics, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa 11152, Egypt Background: Effective treatment of osteoarthritis necessitates both symptomatic relief and hindrance of joint degeneration progression. Non-steroidal anti-inflammatory drugs permit symptomatic relief only and can cause mucosal injury in the gut. Before absorption, diacerein (Dcn) is converted into rhein that counteracts cartilage degeneration without affecting prostaglandin production. Yet, low solubility and laxative action of unabsorbed rhein in the colon hindered its use. Thus, enhanced Dcn dissolution would allow absorption at the upper gut improving its bioavailability and possibly abolishing the laxative action. Methods: Therefore, self-nanoemulsifying drug delivery systems (SNEDDSs) with each of gelucire 44/14 (Glc) and d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) at different drug:carrier weight ratios of 1:1, 1:2, 1:4, 1:6, 1:8 and 1:10 were prepared by melt method and filled into hard gelatin capsules. The optimized binary systems were selected based on solid state characterization, scanning electron microscopy (SEM) and in vitro evaluation of the prepared SNEDDSs in comparison with their corresponding physical mixtures (PMs) and Dcn. The optimized systems were further examined with respect to their morphology, size distribution and ζ-potential. Moreover, the anti-inflammatory activity of the optimized systems against carrageenan-induced paw edema in rats was assessed through estimation of edema and edema inhibition percentages as well as histopathological examination and immunohistochemical localization of tumor necrosis factor-alpha (TNF-α) and caspase-3. Results: Significantly (P<0.05) enhanced in vitro drug release was recorded for SNEDDSs with either carrier when compared to Dcn and the corresponding PMs. SNEDDSs based on 1:10 Dcn:Glc and 1:8 Dcn:TPGS showed significantly (P<0.05) reduced edema and inflammation as well as expression of TNF-α and caspase-3 relative to positive control and Dcn pretreated groups. Conclusion: These SNEDDSs can be represented as potential oral drug delivery systems of Dcn for enhanced dissolution and anti-inflammatory activity against carrageenan-induced paw edema. Keywords: diacerein, gelucire 44/14, d-α-tocopheryl polyethylene glycol 1,000 succinate, self-nanoemulsifying drug-delivery systems, anti-inflammatory activity, paw edema Eltobshi AAMohamed EAAbdelghani GMNouh ATDove Medical PressarticlediacereinGelucire 44/14D-α-tocopheryl polyethylene glycol 1000 succinateself-nanoemulsifying drug delivery systemsanti-inflammatory activitypaw edemaMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 13, Pp 6585-6602 (2018)
institution	DOAJ
collection	DOAJ
language	EN
topic	diacerein Gelucire 44/14 D-α-tocopheryl polyethylene glycol 1000 succinate self-nanoemulsifying drug delivery systems anti-inflammatory activity paw edema Medicine (General) R5-920
spellingShingle	diacerein Gelucire 44/14 D-α-tocopheryl polyethylene glycol 1000 succinate self-nanoemulsifying drug delivery systems anti-inflammatory activity paw edema Medicine (General) R5-920 Eltobshi AA Mohamed EA Abdelghani GM Nouh AT Self-nanoemulsifying drug-delivery systems for potentiated anti-inflammatory activity of diacerein
description	Amal Ahmed Eltobshi,1 Elham Abdelmonem Mohamed,2 Galal Mahmoud Abdelghani,2 Ahmed Talaat Nouh3 1Department of Pharmaceutical Technology, Faculty of Pharmacy, Horus University, New Damietta 34517, Egypt; 2Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt; 3Department of Pharmaceutics, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa 11152, Egypt Background: Effective treatment of osteoarthritis necessitates both symptomatic relief and hindrance of joint degeneration progression. Non-steroidal anti-inflammatory drugs permit symptomatic relief only and can cause mucosal injury in the gut. Before absorption, diacerein (Dcn) is converted into rhein that counteracts cartilage degeneration without affecting prostaglandin production. Yet, low solubility and laxative action of unabsorbed rhein in the colon hindered its use. Thus, enhanced Dcn dissolution would allow absorption at the upper gut improving its bioavailability and possibly abolishing the laxative action. Methods: Therefore, self-nanoemulsifying drug delivery systems (SNEDDSs) with each of gelucire 44/14 (Glc) and d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS) at different drug:carrier weight ratios of 1:1, 1:2, 1:4, 1:6, 1:8 and 1:10 were prepared by melt method and filled into hard gelatin capsules. The optimized binary systems were selected based on solid state characterization, scanning electron microscopy (SEM) and in vitro evaluation of the prepared SNEDDSs in comparison with their corresponding physical mixtures (PMs) and Dcn. The optimized systems were further examined with respect to their morphology, size distribution and ζ-potential. Moreover, the anti-inflammatory activity of the optimized systems against carrageenan-induced paw edema in rats was assessed through estimation of edema and edema inhibition percentages as well as histopathological examination and immunohistochemical localization of tumor necrosis factor-alpha (TNF-α) and caspase-3. Results: Significantly (P<0.05) enhanced in vitro drug release was recorded for SNEDDSs with either carrier when compared to Dcn and the corresponding PMs. SNEDDSs based on 1:10 Dcn:Glc and 1:8 Dcn:TPGS showed significantly (P<0.05) reduced edema and inflammation as well as expression of TNF-α and caspase-3 relative to positive control and Dcn pretreated groups. Conclusion: These SNEDDSs can be represented as potential oral drug delivery systems of Dcn for enhanced dissolution and anti-inflammatory activity against carrageenan-induced paw edema. Keywords: diacerein, gelucire 44/14, d-α-tocopheryl polyethylene glycol 1,000 succinate, self-nanoemulsifying drug-delivery systems, anti-inflammatory activity, paw edema
format	article
author	Eltobshi AA Mohamed EA Abdelghani GM Nouh AT
author_facet	Eltobshi AA Mohamed EA Abdelghani GM Nouh AT
author_sort	Eltobshi AA
title	Self-nanoemulsifying drug-delivery systems for potentiated anti-inflammatory activity of diacerein
title_short	Self-nanoemulsifying drug-delivery systems for potentiated anti-inflammatory activity of diacerein
title_full	Self-nanoemulsifying drug-delivery systems for potentiated anti-inflammatory activity of diacerein
title_fullStr	Self-nanoemulsifying drug-delivery systems for potentiated anti-inflammatory activity of diacerein
title_full_unstemmed	Self-nanoemulsifying drug-delivery systems for potentiated anti-inflammatory activity of diacerein
title_sort	self-nanoemulsifying drug-delivery systems for potentiated anti-inflammatory activity of diacerein
publisher	Dove Medical Press
publishDate	2018
url	https://doaj.org/article/c4f3015e36344805b2b3a26260c62f23
work_keys_str_mv	AT eltobshiaa selfnanoemulsifyingdrugdeliverysystemsforpotentiatedantiinflammatoryactivityofdiacerein AT mohamedea selfnanoemulsifyingdrugdeliverysystemsforpotentiatedantiinflammatoryactivityofdiacerein AT abdelghanigm selfnanoemulsifyingdrugdeliverysystemsforpotentiatedantiinflammatoryactivityofdiacerein AT nouhat selfnanoemulsifyingdrugdeliverysystemsforpotentiatedantiinflammatoryactivityofdiacerein
_version_	1718398210015232000

Self-nanoemulsifying drug-delivery systems for potentiated anti-inflammatory activity of diacerein

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