Superiority of TPGS-loaded micelles in the brain delivery of vinpocetine via administration of thermosensitive intranasal gel

Tarek A Ahmed,1,2 Khalid M El-Say,1,2 Osama AA Ahmed,1,3 Bader M Aljaeid11Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Kingdom of Saudi Arabia; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo 11651...

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Autores principales:	Ahmed TA, El-Say KM, Ahmed OAA, Aljaeid BM
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2019
Materias:	Brain distribution Lipid based nanocarriers In situ gel Intranasal Vinpocetine. Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/1bb25681293c440a8555f1c7d8b519f1
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spelling	oai:doaj.org-article:1bb25681293c440a8555f1c7d8b519f12021-12-02T05:42:56ZSuperiority of TPGS-loaded micelles in the brain delivery of vinpocetine via administration of thermosensitive intranasal gel1178-2013https://doaj.org/article/1bb25681293c440a8555f1c7d8b519f12019-07-01T00:00:00Zhttps://www.dovepress.com/superiority-of-tpgs-loaded-micelles-in-the-brain-delivery-of-vinpoceti-peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Tarek A Ahmed,1,2 Khalid M El-Say,1,2 Osama AA Ahmed,1,3 Bader M Aljaeid11Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Kingdom of Saudi Arabia; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo 11651, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, EgyptBackground: Vinpocetine (VPN) is a synthetic derivative of the Vinca minor alkaloids. The drug is characterized by a short half-life, limited water solubility and high hepatic first-pass effect. The objective was to develop different lipid-based nanocarriers (NCs) loaded into a thermosensitive in situ gelling (ISG) system to improve VPN bioavailability and brain targeting via intranasal (IN) delivery.Methods:  Different lipid-based NCs were developed and characterized for vesicle size, zeta potential, VPN entrapment efficiency (EE) and morphological characterization using transmission electron microscope (TEM). The prepared NCs were loaded into ISG formulations and characterized for their mucoadhesive properties. Ex-vivo permeation and histological study of the nasal mucosa were conducted. Pharmacokinetic and brain tissue distribution were investigated and compared to a marketed VPN product following administration of a single dose to rats.Results: VPN-D-α-Tocopherol polyethylene glycol 1000 succinate (TPGS) micelles nano-formulation showed the smallest particle size, highest EE among the studied NCs. TEM images revealed an almost spherical shape for all the prepared NCs. Among the NCs studied, VPN-loaded TPGS micelles demonstrated the highest percent cumulative VPN ex vivo permeation. All the prepared ISG formulations revealed the presence of mucoadhesive properties and showed no signs of inflammation or necrosis upon histological examination. Rats administered IN VPN-loaded TPGS-micelles ISG showed superior VPN concentration in the brain tissue and significant high relative bioavailability when compared to that received raw VPN-loaded ISG and marketed drug oral tablets. VPN-D-α-Tocopherol polyethylene glycol 1000 succinate (TPGS) micelles nano-formulation showed the smallest particle size, highest EE among the studied NCs. TEM images revealed an almost spherical shape for all the prepared NCs. Among the NCs studied, VPN-loaded TPGS micelles demonstrated the highest percent cumulative VPN ex vivo permeation. All the prepared ISG formulations revealed the presence of mucoadhesive properties and showed no signs of inflammation or necrosis upon histological examination. Rats administered IN VPN-loaded TPGS-micelles ISG showed superior VPN concentration in the brain tissue and significant high relative bioavailability when compared to that received raw VPN-loaded ISG and marketed drug oral tablets.Conclusion: VPN-loaded TPGS-micelles ISG formulation is a successful brain drug delivery system with enhanced bioavailability for drugs with poor bioavailability and those that are frequently administered.Keywords: brain distribution, lipid based nanocarriers, in situ gel, intranasal, vinpocetineAhmed TAEl-Say KMAhmed OAAAljaeid BMDove Medical PressarticleBrain distributionLipid based nanocarriersIn situ gelIntranasalVinpocetine.Medicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 14, Pp 5555-5567 (2019)
institution	DOAJ
collection	DOAJ
language	EN
topic	Brain distribution Lipid based nanocarriers In situ gel Intranasal Vinpocetine. Medicine (General) R5-920
spellingShingle	Brain distribution Lipid based nanocarriers In situ gel Intranasal Vinpocetine. Medicine (General) R5-920 Ahmed TA El-Say KM Ahmed OAA Aljaeid BM Superiority of TPGS-loaded micelles in the brain delivery of vinpocetine via administration of thermosensitive intranasal gel
description	Tarek A Ahmed,1,2 Khalid M El-Say,1,2 Osama AA Ahmed,1,3 Bader M Aljaeid11Department of Pharmaceutics, Faculty of Pharmacy, King Abdulaziz University, Jeddah, Kingdom of Saudi Arabia; 2Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Al-Azhar University, Cairo 11651, Egypt; 3Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Minia University, Minia, EgyptBackground: Vinpocetine (VPN) is a synthetic derivative of the Vinca minor alkaloids. The drug is characterized by a short half-life, limited water solubility and high hepatic first-pass effect. The objective was to develop different lipid-based nanocarriers (NCs) loaded into a thermosensitive in situ gelling (ISG) system to improve VPN bioavailability and brain targeting via intranasal (IN) delivery.Methods:  Different lipid-based NCs were developed and characterized for vesicle size, zeta potential, VPN entrapment efficiency (EE) and morphological characterization using transmission electron microscope (TEM). The prepared NCs were loaded into ISG formulations and characterized for their mucoadhesive properties. Ex-vivo permeation and histological study of the nasal mucosa were conducted. Pharmacokinetic and brain tissue distribution were investigated and compared to a marketed VPN product following administration of a single dose to rats.Results: VPN-D-α-Tocopherol polyethylene glycol 1000 succinate (TPGS) micelles nano-formulation showed the smallest particle size, highest EE among the studied NCs. TEM images revealed an almost spherical shape for all the prepared NCs. Among the NCs studied, VPN-loaded TPGS micelles demonstrated the highest percent cumulative VPN ex vivo permeation. All the prepared ISG formulations revealed the presence of mucoadhesive properties and showed no signs of inflammation or necrosis upon histological examination. Rats administered IN VPN-loaded TPGS-micelles ISG showed superior VPN concentration in the brain tissue and significant high relative bioavailability when compared to that received raw VPN-loaded ISG and marketed drug oral tablets. VPN-D-α-Tocopherol polyethylene glycol 1000 succinate (TPGS) micelles nano-formulation showed the smallest particle size, highest EE among the studied NCs. TEM images revealed an almost spherical shape for all the prepared NCs. Among the NCs studied, VPN-loaded TPGS micelles demonstrated the highest percent cumulative VPN ex vivo permeation. All the prepared ISG formulations revealed the presence of mucoadhesive properties and showed no signs of inflammation or necrosis upon histological examination. Rats administered IN VPN-loaded TPGS-micelles ISG showed superior VPN concentration in the brain tissue and significant high relative bioavailability when compared to that received raw VPN-loaded ISG and marketed drug oral tablets.Conclusion: VPN-loaded TPGS-micelles ISG formulation is a successful brain drug delivery system with enhanced bioavailability for drugs with poor bioavailability and those that are frequently administered.Keywords: brain distribution, lipid based nanocarriers, in situ gel, intranasal, vinpocetine
format	article
author	Ahmed TA El-Say KM Ahmed OAA Aljaeid BM
author_facet	Ahmed TA El-Say KM Ahmed OAA Aljaeid BM
author_sort	Ahmed TA
title	Superiority of TPGS-loaded micelles in the brain delivery of vinpocetine via administration of thermosensitive intranasal gel
title_short	Superiority of TPGS-loaded micelles in the brain delivery of vinpocetine via administration of thermosensitive intranasal gel
title_full	Superiority of TPGS-loaded micelles in the brain delivery of vinpocetine via administration of thermosensitive intranasal gel
title_fullStr	Superiority of TPGS-loaded micelles in the brain delivery of vinpocetine via administration of thermosensitive intranasal gel
title_full_unstemmed	Superiority of TPGS-loaded micelles in the brain delivery of vinpocetine via administration of thermosensitive intranasal gel
title_sort	superiority of tpgs-loaded micelles in the brain delivery of vinpocetine via administration of thermosensitive intranasal gel
publisher	Dove Medical Press
publishDate	2019
url	https://doaj.org/article/1bb25681293c440a8555f1c7d8b519f1
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Superiority of TPGS-loaded micelles in the brain delivery of vinpocetine via administration of thermosensitive intranasal gel

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