Quality by Design Approach for Preparation of Zolmitriptan/Chitosan Nanostructured Lipid Carrier Particles – Formulation and Pharmacodynamic Assessment

Quality by Design Approach for Preparation of Zolmitriptan/Chitosan Nanostructured Lipid Carrier Particles – Formulation and Pharmacodynamic Assessment

Randa Hanie Awadeen, Mariza Fouad Boughdady, Mahasen Mohamed Meshali Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, EgyptCorrespondence: Randa Hanie AwadeenDepartment of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, EgyptTel +2010020...

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Autores principales: Awadeen RH, Boughdady MF, Meshali MM
Formato: article
Lenguaje:EN
Publicado: Dove Medical Press 2020
Materias:
zolmitriptan
factorial design
nanostructured lipid carrier
in-situ gelling
pharmacodynamics
Medicine (General)
R5-920
Acceso en línea:https://doaj.org/article/693f905a883f404db4e8c187cf6eca4f
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spelling oai:doaj.org-article:693f905a883f404db4e8c187cf6eca4f2021-12-02T15:01:26ZQuality by Design Approach for Preparation of Zolmitriptan/Chitosan Nanostructured Lipid Carrier Particles – Formulation and Pharmacodynamic Assessment1178-2013https://doaj.org/article/693f905a883f404db4e8c187cf6eca4f2020-11-01T00:00:00Zhttps://www.dovepress.com/quality-by-design-approach-for-preparation-of-zolmitriptanchitosan-nan-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Randa Hanie Awadeen, Mariza Fouad Boughdady, Mahasen Mohamed Meshali Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, EgyptCorrespondence: Randa Hanie AwadeenDepartment of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, EgyptTel +201002074761Email Randahany@mans.edu.egPurpose: Zolmitriptan (ZT) is a selective serotonin agonist that is used for the treatment of migraine. It belongs to BCS class III with high solubility and low permeability. Besides, the drug is subjected to pre-systemic metabolism. Accordingly, new Zolmitriptan/chitosan nanostructured lipid carriers (ZT/CT NLCs) coated with Tween 80 (stealthy layer) have been developed to overcome such demerits.Methods: The NLCs were developed by combining ultrasonication and double emulsion (w/o/w) techniques. The lipids were Gelucire and Labrasol. Herein, the quality by design (23 full factorial design) was scrupulously followed, where critical process parameters and critical quality attributes were predefined. The optimized formulation (F8) was fully characterized with respect to entrapment efficiency (%EE), percentage yield (% yield), particle size, size distribution (PDI), zeta potential (ZP), morphological appearance (TEM). In vitro release, stability study and pharmacodynamic evaluations were also assessed. The optimized freeze dried formula was dispensed in in situ gelling hard gelatin capsule encompassing pectin and guar gum for further in vitro and pharmacodynamic evaluations.Results: The optimized spherical nanoparticles experienced high percentage EE and yield (78.14% and 60.19%, respectively), low particle size and PDI (343.87 nm and 0.209, respectively), as well as high negative ZP (− 25.5 mV). It showed good physical stability at refrigerated conditions. The NLCs dispensed in in situ gelling hard gelatin capsule comprising pectin and guar gum experienced sustained release for 30 h and significantly maintained the pharmacological effect in mice up to 8 h (p < 0.001).Conclusion: ZT, a BCS class III drug that suffers from poor permeability and pre-systemic metabolism, was successfully maneuvered as nanostructured lipid carrier particles (NLCs). The incorporation of the NLCs in in situ gelling hard gelatin capsules fulfilled a dual function in increasing permeability, as well as sustaining the pharmacodynamic effect. This result would open new vistas in improving the efficacy of other class III drugs.Keywords: zolmitriptan, factorial design, nanostructured lipid carrier, in situ gelling, pharmacodynamicsAwadeen RHBoughdady MFMeshali MMDove Medical Pressarticlezolmitriptanfactorial designnanostructured lipid carrierin-situ gellingpharmacodynamicsMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 15, Pp 8553-8568 (2020)
institution DOAJ
collection DOAJ
language EN
topic zolmitriptan
factorial design
nanostructured lipid carrier
in-situ gelling
pharmacodynamics
Medicine (General)
R5-920
spellingShingle zolmitriptan
factorial design
nanostructured lipid carrier
in-situ gelling
pharmacodynamics
Medicine (General)
R5-920
Awadeen RH
Boughdady MF
Meshali MM
Quality by Design Approach for Preparation of Zolmitriptan/Chitosan Nanostructured Lipid Carrier Particles – Formulation and Pharmacodynamic Assessment
description Randa Hanie Awadeen, Mariza Fouad Boughdady, Mahasen Mohamed Meshali Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, EgyptCorrespondence: Randa Hanie AwadeenDepartment of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura 35516, EgyptTel +201002074761Email Randahany@mans.edu.egPurpose: Zolmitriptan (ZT) is a selective serotonin agonist that is used for the treatment of migraine. It belongs to BCS class III with high solubility and low permeability. Besides, the drug is subjected to pre-systemic metabolism. Accordingly, new Zolmitriptan/chitosan nanostructured lipid carriers (ZT/CT NLCs) coated with Tween 80 (stealthy layer) have been developed to overcome such demerits.Methods: The NLCs were developed by combining ultrasonication and double emulsion (w/o/w) techniques. The lipids were Gelucire and Labrasol. Herein, the quality by design (23 full factorial design) was scrupulously followed, where critical process parameters and critical quality attributes were predefined. The optimized formulation (F8) was fully characterized with respect to entrapment efficiency (%EE), percentage yield (% yield), particle size, size distribution (PDI), zeta potential (ZP), morphological appearance (TEM). In vitro release, stability study and pharmacodynamic evaluations were also assessed. The optimized freeze dried formula was dispensed in in situ gelling hard gelatin capsule encompassing pectin and guar gum for further in vitro and pharmacodynamic evaluations.Results: The optimized spherical nanoparticles experienced high percentage EE and yield (78.14% and 60.19%, respectively), low particle size and PDI (343.87 nm and 0.209, respectively), as well as high negative ZP (− 25.5 mV). It showed good physical stability at refrigerated conditions. The NLCs dispensed in in situ gelling hard gelatin capsule comprising pectin and guar gum experienced sustained release for 30 h and significantly maintained the pharmacological effect in mice up to 8 h (p < 0.001).Conclusion: ZT, a BCS class III drug that suffers from poor permeability and pre-systemic metabolism, was successfully maneuvered as nanostructured lipid carrier particles (NLCs). The incorporation of the NLCs in in situ gelling hard gelatin capsules fulfilled a dual function in increasing permeability, as well as sustaining the pharmacodynamic effect. This result would open new vistas in improving the efficacy of other class III drugs.Keywords: zolmitriptan, factorial design, nanostructured lipid carrier, in situ gelling, pharmacodynamics
format article
author Awadeen RH
Boughdady MF
Meshali MM
author_facet Awadeen RH
Boughdady MF
Meshali MM
author_sort Awadeen RH
title Quality by Design Approach for Preparation of Zolmitriptan/Chitosan Nanostructured Lipid Carrier Particles – Formulation and Pharmacodynamic Assessment
title_short Quality by Design Approach for Preparation of Zolmitriptan/Chitosan Nanostructured Lipid Carrier Particles – Formulation and Pharmacodynamic Assessment
title_full Quality by Design Approach for Preparation of Zolmitriptan/Chitosan Nanostructured Lipid Carrier Particles – Formulation and Pharmacodynamic Assessment
title_fullStr Quality by Design Approach for Preparation of Zolmitriptan/Chitosan Nanostructured Lipid Carrier Particles – Formulation and Pharmacodynamic Assessment
title_full_unstemmed Quality by Design Approach for Preparation of Zolmitriptan/Chitosan Nanostructured Lipid Carrier Particles – Formulation and Pharmacodynamic Assessment
title_sort quality by design approach for preparation of zolmitriptan/chitosan nanostructured lipid carrier particles – formulation and pharmacodynamic assessment
publisher Dove Medical Press
publishDate 2020
url https://doaj.org/article/693f905a883f404db4e8c187cf6eca4f
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AT boughdadymf qualitybydesignapproachforpreparationofzolmitriptanchitosannanostructuredlipidcarrierparticlesndashformulationandpharmacodynamicassessment
AT meshalimm qualitybydesignapproachforpreparationofzolmitriptanchitosannanostructuredlipidcarrierparticlesndashformulationandpharmacodynamicassessment
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