Formulation of Boron Encapsulated Smart Nanocapsules for Targeted Drug Delivery to the Brain

Drug delivery through the Blood–Brain Barrier (BBB) represents a significant challenge. Despite the current strategies to circumvent the BBB, nanotechnology offers unprecedented opportunities for combining selective delivery, improved bioavailability, drug protection, and enhanced pharmacokinetics p...

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Autores principales:	Anis Daou, Raid G. Alany, Gianpiero Calabrese
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	drug delivery blood–brain barrier brain tumours smart composite nanodelivery systems boron neutron capture therapy delocalised lipophilic cations Technology T Engineering (General). Civil engineering (General) TA1-2040 Biology (General) QH301-705.5 Physics QC1-999 Chemistry QD1-999
Acceso en línea:	https://doaj.org/article/5448469f6a3e4267b6c42ac4b7d647e7
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spelling	oai:doaj.org-article:5448469f6a3e4267b6c42ac4b7d647e72021-11-25T16:36:58ZFormulation of Boron Encapsulated Smart Nanocapsules for Targeted Drug Delivery to the Brain10.3390/app1122107382076-3417https://doaj.org/article/5448469f6a3e4267b6c42ac4b7d647e72021-11-01T00:00:00Zhttps://www.mdpi.com/2076-3417/11/22/10738https://doaj.org/toc/2076-3417Drug delivery through the Blood–Brain Barrier (BBB) represents a significant challenge. Despite the current strategies to circumvent the BBB, nanotechnology offers unprecedented opportunities for combining selective delivery, improved bioavailability, drug protection, and enhanced pharmacokinetics profiles. Chitosan nanocarriers allow for a more efficacious strategy at the cellular and sub-cellular levels. Boron Neutron Capture Therapy (BNCT) is a targeted chemo-radiotherapeutic technique that allows the selective depletion of cancer cells by means of selective tagging of cancer cells with <sup>10</sup>B, followed by irradiation with low-energy neutrons. Consequently, the combination of a polymer-based nanodelivery system enclosing an effective BNCT pharmacophore can potentially lead to the selective delivery of the load to cancer cells beyond the BBB. In this work, synthesized novel boronated agents based on carborane-functionalized Delocalized Lipophilic Cations (DLCs) are assessed for safety and selective targeting of tumour cells. The compounds are then encapsulated in nanocarriers constituted by chitosan to promote permeability through the BBB. Additionally, chitosan was used in combination with polypyrrole to form a smart composite nanocapsule, which is expected to release its drug load with variations in pH. Results indicate the achievement of more selective boron delivery to cells via carboranyl DLCs. Finally, preliminary cell studies indicate no toxicity was detected in chitosan nanocapsules, further enhancing its viability as a potential delivery vehicle in the BNCT of brain tumours.Anis DaouRaid G. AlanyGianpiero CalabreseMDPI AGarticledrug deliveryblood–brain barrierbrain tumourssmart composite nanodelivery systemsboron neutron capture therapydelocalised lipophilic cationsTechnologyTEngineering (General). Civil engineering (General)TA1-2040Biology (General)QH301-705.5PhysicsQC1-999ChemistryQD1-999ENApplied Sciences, Vol 11, Iss 10738, p 10738 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	drug delivery blood–brain barrier brain tumours smart composite nanodelivery systems boron neutron capture therapy delocalised lipophilic cations Technology T Engineering (General). Civil engineering (General) TA1-2040 Biology (General) QH301-705.5 Physics QC1-999 Chemistry QD1-999
spellingShingle	drug delivery blood–brain barrier brain tumours smart composite nanodelivery systems boron neutron capture therapy delocalised lipophilic cations Technology T Engineering (General). Civil engineering (General) TA1-2040 Biology (General) QH301-705.5 Physics QC1-999 Chemistry QD1-999 Anis Daou Raid G. Alany Gianpiero Calabrese Formulation of Boron Encapsulated Smart Nanocapsules for Targeted Drug Delivery to the Brain
description	Drug delivery through the Blood–Brain Barrier (BBB) represents a significant challenge. Despite the current strategies to circumvent the BBB, nanotechnology offers unprecedented opportunities for combining selective delivery, improved bioavailability, drug protection, and enhanced pharmacokinetics profiles. Chitosan nanocarriers allow for a more efficacious strategy at the cellular and sub-cellular levels. Boron Neutron Capture Therapy (BNCT) is a targeted chemo-radiotherapeutic technique that allows the selective depletion of cancer cells by means of selective tagging of cancer cells with <sup>10</sup>B, followed by irradiation with low-energy neutrons. Consequently, the combination of a polymer-based nanodelivery system enclosing an effective BNCT pharmacophore can potentially lead to the selective delivery of the load to cancer cells beyond the BBB. In this work, synthesized novel boronated agents based on carborane-functionalized Delocalized Lipophilic Cations (DLCs) are assessed for safety and selective targeting of tumour cells. The compounds are then encapsulated in nanocarriers constituted by chitosan to promote permeability through the BBB. Additionally, chitosan was used in combination with polypyrrole to form a smart composite nanocapsule, which is expected to release its drug load with variations in pH. Results indicate the achievement of more selective boron delivery to cells via carboranyl DLCs. Finally, preliminary cell studies indicate no toxicity was detected in chitosan nanocapsules, further enhancing its viability as a potential delivery vehicle in the BNCT of brain tumours.
format	article
author	Anis Daou Raid G. Alany Gianpiero Calabrese
author_facet	Anis Daou Raid G. Alany Gianpiero Calabrese
author_sort	Anis Daou
title	Formulation of Boron Encapsulated Smart Nanocapsules for Targeted Drug Delivery to the Brain
title_short	Formulation of Boron Encapsulated Smart Nanocapsules for Targeted Drug Delivery to the Brain
title_full	Formulation of Boron Encapsulated Smart Nanocapsules for Targeted Drug Delivery to the Brain
title_fullStr	Formulation of Boron Encapsulated Smart Nanocapsules for Targeted Drug Delivery to the Brain
title_full_unstemmed	Formulation of Boron Encapsulated Smart Nanocapsules for Targeted Drug Delivery to the Brain
title_sort	formulation of boron encapsulated smart nanocapsules for targeted drug delivery to the brain
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/5448469f6a3e4267b6c42ac4b7d647e7
work_keys_str_mv	AT anisdaou formulationofboronencapsulatedsmartnanocapsulesfortargeteddrugdeliverytothebrain AT raidgalany formulationofboronencapsulatedsmartnanocapsulesfortargeteddrugdeliverytothebrain AT gianpierocalabrese formulationofboronencapsulatedsmartnanocapsulesfortargeteddrugdeliverytothebrain
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Formulation of Boron Encapsulated Smart Nanocapsules for Targeted Drug Delivery to the Brain

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