Nose to brain delivery of Efavirenz nanosuspension for effective neuro AIDS therapy: in-vitro, in-vivo and pharmacokinetic assessment

Efavirenz is inhibitor of non-nucleoside reverse transcriptase enzyme; BCS class II drug. The objective of the present research was to prepare and evaluate nanosuspension of Efavirenz for the treatment of neuro-AIDS. Efavirenz is the substrate for drug resistant proteins at BBB prone to efflux and c...

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Autores principales:	Smita Kakad, Sanjay Kshirsagar
Formato:	article
Lenguaje:	EN
Publicado:	Elsevier 2021
Materias:	Blood brain barrier Brain targeting Efavirenz Intranasal Nanosuspension Neuro-AIDS Science (General) Q1-390 Social sciences (General) H1-99
Acceso en línea:	https://doaj.org/article/a15b63c5c8614a12a54416b697025aab
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spelling	oai:doaj.org-article:a15b63c5c8614a12a54416b697025aab2021-12-02T05:02:52ZNose to brain delivery of Efavirenz nanosuspension for effective neuro AIDS therapy: in-vitro, in-vivo and pharmacokinetic assessment2405-844010.1016/j.heliyon.2021.e08368https://doaj.org/article/a15b63c5c8614a12a54416b697025aab2021-11-01T00:00:00Zhttp://www.sciencedirect.com/science/article/pii/S2405844021024713https://doaj.org/toc/2405-8440Efavirenz is inhibitor of non-nucleoside reverse transcriptase enzyme; BCS class II drug. The objective of the present research was to prepare and evaluate nanosuspension of Efavirenz for the treatment of neuro-AIDS. Efavirenz is the substrate for drug resistant proteins at BBB prone to efflux and could not reach brain with effective levels. Current need of the therapy is to develop drug delivery systems targeting viral reservoirs at effective concentration in the brain. With this need we developed Efavirenz nanosuspension for nose to brain drug transport to bypass blood brain barrier. Nanosuspension prepared with high-pressure homogenization had a mean particle size of 223 nm, PDI of 0.2 and -21.2 mV zeta potential. Histopathology study on goat nasal mucosa showed no adverse effects of formulation on nasal tissues. Gamma scintigraphy study and in-vivo study on Wistar rat model reveals drug transport to the CNS after nasal administration. Pharmacokinetic parameters and drug targeting potential of 99.46 % suggest direct nose to brain transport of Efavirenz nanoparticle. Results reveal that nose to brain delivery of Efavirenz is the best possible alternative for neuro –AIDS treatment.Smita KakadSanjay KshirsagarElsevierarticleBlood brain barrierBrain targetingEfavirenzIntranasalNanosuspensionNeuro-AIDSScience (General)Q1-390Social sciences (General)H1-99ENHeliyon, Vol 7, Iss 11, Pp e08368- (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	Blood brain barrier Brain targeting Efavirenz Intranasal Nanosuspension Neuro-AIDS Science (General) Q1-390 Social sciences (General) H1-99
spellingShingle	Blood brain barrier Brain targeting Efavirenz Intranasal Nanosuspension Neuro-AIDS Science (General) Q1-390 Social sciences (General) H1-99 Smita Kakad Sanjay Kshirsagar Nose to brain delivery of Efavirenz nanosuspension for effective neuro AIDS therapy: in-vitro, in-vivo and pharmacokinetic assessment
description	Efavirenz is inhibitor of non-nucleoside reverse transcriptase enzyme; BCS class II drug. The objective of the present research was to prepare and evaluate nanosuspension of Efavirenz for the treatment of neuro-AIDS. Efavirenz is the substrate for drug resistant proteins at BBB prone to efflux and could not reach brain with effective levels. Current need of the therapy is to develop drug delivery systems targeting viral reservoirs at effective concentration in the brain. With this need we developed Efavirenz nanosuspension for nose to brain drug transport to bypass blood brain barrier. Nanosuspension prepared with high-pressure homogenization had a mean particle size of 223 nm, PDI of 0.2 and -21.2 mV zeta potential. Histopathology study on goat nasal mucosa showed no adverse effects of formulation on nasal tissues. Gamma scintigraphy study and in-vivo study on Wistar rat model reveals drug transport to the CNS after nasal administration. Pharmacokinetic parameters and drug targeting potential of 99.46 % suggest direct nose to brain transport of Efavirenz nanoparticle. Results reveal that nose to brain delivery of Efavirenz is the best possible alternative for neuro –AIDS treatment.
format	article
author	Smita Kakad Sanjay Kshirsagar
author_facet	Smita Kakad Sanjay Kshirsagar
author_sort	Smita Kakad
title	Nose to brain delivery of Efavirenz nanosuspension for effective neuro AIDS therapy: in-vitro, in-vivo and pharmacokinetic assessment
title_short	Nose to brain delivery of Efavirenz nanosuspension for effective neuro AIDS therapy: in-vitro, in-vivo and pharmacokinetic assessment
title_full	Nose to brain delivery of Efavirenz nanosuspension for effective neuro AIDS therapy: in-vitro, in-vivo and pharmacokinetic assessment
title_fullStr	Nose to brain delivery of Efavirenz nanosuspension for effective neuro AIDS therapy: in-vitro, in-vivo and pharmacokinetic assessment
title_full_unstemmed	Nose to brain delivery of Efavirenz nanosuspension for effective neuro AIDS therapy: in-vitro, in-vivo and pharmacokinetic assessment
title_sort	nose to brain delivery of efavirenz nanosuspension for effective neuro aids therapy: in-vitro, in-vivo and pharmacokinetic assessment
publisher	Elsevier
publishDate	2021
url	https://doaj.org/article/a15b63c5c8614a12a54416b697025aab
work_keys_str_mv	AT smitakakad nosetobraindeliveryofefavirenznanosuspensionforeffectiveneuroaidstherapyinvitroinvivoandpharmacokineticassessment AT sanjaykshirsagar nosetobraindeliveryofefavirenznanosuspensionforeffectiveneuroaidstherapyinvitroinvivoandpharmacokineticassessment
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Nose to brain delivery of Efavirenz nanosuspension for effective neuro AIDS therapy: in-vitro, in-vivo and pharmacokinetic assessment

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