Optimized Rivastigmine Nanoparticles Coated with Eudragit for Intranasal Application to Brain Delivery: Evaluation and Nasal Ciliotoxicity Studies

Rivastigmine, a reversible cholinesterase inhibitor, is frequently indicated in the management of demented conditions associated with Alzheimer disease. The major hurdle of delivering this drug through the oral route is its poor bioavailability, which prompted the development of novel delivery appro...

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Autores principales:	Mansi Bhanderi, Jigar Shah, Bapi Gorain, Anroop B. Nair, Shery Jacob, Syed Mohammed Basheeruddin Asdaq, Santosh Fattepur, Abdulhakeem S. Alamri, Walaa F. Alsanie, Majid Alhomrani, Sreeharsha Nagaraja, Md. Khalid Anwer
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	nanoparticles rivastigmine intranasal application optimization quality by design Technology T Electrical engineering. Electronics. Nuclear engineering TK1-9971 Engineering (General). Civil engineering (General) TA1-2040 Microscopy QH201-278.5 Descriptive and experimental mechanics QC120-168.85
Acceso en línea:	https://doaj.org/article/a9a7af170d3740dbb93f81d5536f7331
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spelling	oai:doaj.org-article:a9a7af170d3740dbb93f81d5536f73312021-11-11T17:51:55ZOptimized Rivastigmine Nanoparticles Coated with Eudragit for Intranasal Application to Brain Delivery: Evaluation and Nasal Ciliotoxicity Studies10.3390/ma142162911996-1944https://doaj.org/article/a9a7af170d3740dbb93f81d5536f73312021-10-01T00:00:00Zhttps://www.mdpi.com/1996-1944/14/21/6291https://doaj.org/toc/1996-1944Rivastigmine, a reversible cholinesterase inhibitor, is frequently indicated in the management of demented conditions associated with Alzheimer disease. The major hurdle of delivering this drug through the oral route is its poor bioavailability, which prompted the development of novel delivery approaches for improved efficacy. Due to numerous beneficial properties associated with nanocarriers in the drug delivery system, rivastigmine nanoparticles were fabricated to be administer through the intranasal route. During the development of the nanoparticles, preliminary optimization of processing and formulation parameters was done by the design of an experimental approach. The drug–polymer ratio, stirrer speed, and crosslinking time were fixed as independent variables, to analyze the effect on the entrapment efficiency (% EE) and in vitro drug release of the drug. The formulation (D8) obtained from 2<sup>3</sup> full factorial designs was further coated using Eudragit EPO to extend the release pattern of the entrapped drug. Furthermore, the 1:1 ratio of core to polymer depicted spherical particle size of ~175 nm, % EE of 64.83%, 97.59% cumulative drug release, and higher flux (40.39 ± 3.52 µg.h/cm<sup>2</sup>). Finally, the intranasal ciliotoxicity study on sheep nasal mucosa revealed that the exposure of developed nanoparticles was similar to the negative control group, while destruction of normal architecture was noticed in the positive control test group. Overall, from the in vitro results it could be summarized that the optimization of nanoparticles’ formulation of rivastigmine for intranasal application would be retained at the application site for a prolonged duration to release the entrapped drug without producing any local toxicity at the mucosal region.Mansi BhanderiJigar ShahBapi GorainAnroop B. NairShery JacobSyed Mohammed Basheeruddin AsdaqSantosh FattepurAbdulhakeem S. AlamriWalaa F. AlsanieMajid AlhomraniSreeharsha NagarajaMd. Khalid AnwerMDPI AGarticlenanoparticlesrivastigmineintranasal applicationoptimizationquality by designTechnologyTElectrical engineering. Electronics. Nuclear engineeringTK1-9971Engineering (General). Civil engineering (General)TA1-2040MicroscopyQH201-278.5Descriptive and experimental mechanicsQC120-168.85ENMaterials, Vol 14, Iss 6291, p 6291 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	nanoparticles rivastigmine intranasal application optimization quality by design Technology T Electrical engineering. Electronics. Nuclear engineering TK1-9971 Engineering (General). Civil engineering (General) TA1-2040 Microscopy QH201-278.5 Descriptive and experimental mechanics QC120-168.85
spellingShingle	nanoparticles rivastigmine intranasal application optimization quality by design Technology T Electrical engineering. Electronics. Nuclear engineering TK1-9971 Engineering (General). Civil engineering (General) TA1-2040 Microscopy QH201-278.5 Descriptive and experimental mechanics QC120-168.85 Mansi Bhanderi Jigar Shah Bapi Gorain Anroop B. Nair Shery Jacob Syed Mohammed Basheeruddin Asdaq Santosh Fattepur Abdulhakeem S. Alamri Walaa F. Alsanie Majid Alhomrani Sreeharsha Nagaraja Md. Khalid Anwer Optimized Rivastigmine Nanoparticles Coated with Eudragit for Intranasal Application to Brain Delivery: Evaluation and Nasal Ciliotoxicity Studies
description	Rivastigmine, a reversible cholinesterase inhibitor, is frequently indicated in the management of demented conditions associated with Alzheimer disease. The major hurdle of delivering this drug through the oral route is its poor bioavailability, which prompted the development of novel delivery approaches for improved efficacy. Due to numerous beneficial properties associated with nanocarriers in the drug delivery system, rivastigmine nanoparticles were fabricated to be administer through the intranasal route. During the development of the nanoparticles, preliminary optimization of processing and formulation parameters was done by the design of an experimental approach. The drug–polymer ratio, stirrer speed, and crosslinking time were fixed as independent variables, to analyze the effect on the entrapment efficiency (% EE) and in vitro drug release of the drug. The formulation (D8) obtained from 2<sup>3</sup> full factorial designs was further coated using Eudragit EPO to extend the release pattern of the entrapped drug. Furthermore, the 1:1 ratio of core to polymer depicted spherical particle size of ~175 nm, % EE of 64.83%, 97.59% cumulative drug release, and higher flux (40.39 ± 3.52 µg.h/cm<sup>2</sup>). Finally, the intranasal ciliotoxicity study on sheep nasal mucosa revealed that the exposure of developed nanoparticles was similar to the negative control group, while destruction of normal architecture was noticed in the positive control test group. Overall, from the in vitro results it could be summarized that the optimization of nanoparticles’ formulation of rivastigmine for intranasal application would be retained at the application site for a prolonged duration to release the entrapped drug without producing any local toxicity at the mucosal region.
format	article
author	Mansi Bhanderi Jigar Shah Bapi Gorain Anroop B. Nair Shery Jacob Syed Mohammed Basheeruddin Asdaq Santosh Fattepur Abdulhakeem S. Alamri Walaa F. Alsanie Majid Alhomrani Sreeharsha Nagaraja Md. Khalid Anwer
author_facet	Mansi Bhanderi Jigar Shah Bapi Gorain Anroop B. Nair Shery Jacob Syed Mohammed Basheeruddin Asdaq Santosh Fattepur Abdulhakeem S. Alamri Walaa F. Alsanie Majid Alhomrani Sreeharsha Nagaraja Md. Khalid Anwer
author_sort	Mansi Bhanderi
title	Optimized Rivastigmine Nanoparticles Coated with Eudragit for Intranasal Application to Brain Delivery: Evaluation and Nasal Ciliotoxicity Studies
title_short	Optimized Rivastigmine Nanoparticles Coated with Eudragit for Intranasal Application to Brain Delivery: Evaluation and Nasal Ciliotoxicity Studies
title_full	Optimized Rivastigmine Nanoparticles Coated with Eudragit for Intranasal Application to Brain Delivery: Evaluation and Nasal Ciliotoxicity Studies
title_fullStr	Optimized Rivastigmine Nanoparticles Coated with Eudragit for Intranasal Application to Brain Delivery: Evaluation and Nasal Ciliotoxicity Studies
title_full_unstemmed	Optimized Rivastigmine Nanoparticles Coated with Eudragit for Intranasal Application to Brain Delivery: Evaluation and Nasal Ciliotoxicity Studies
title_sort	optimized rivastigmine nanoparticles coated with eudragit for intranasal application to brain delivery: evaluation and nasal ciliotoxicity studies
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/a9a7af170d3740dbb93f81d5536f7331
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Optimized Rivastigmine Nanoparticles Coated with Eudragit for Intranasal Application to Brain Delivery: Evaluation and Nasal Ciliotoxicity Studies

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