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Formulation of Intranasal Mucoadhesive Thermotriggered In Situ Gel Containing Mirtazapine as an Antidepressant Drug

The purpose of the present work was to develop nanoemulsion-based formulations of mirtazapine for intranasal delivery using a spray actuator to target the brain for treating depression. Research on the solubility of medications in different oils, surfactants, co-surfactants, and solvents has been do...

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Autores principales: Ghazwani, Mohammed, Vasudevan, Rajalakshimi, Kandasamy, Geetha, Manusri, Naredla., Devanandan, Praveen, Puvvada, Ranadheer Chowdary, Veeramani, Vinoth Prabhu, Paulsamy, Premalatha, Venkatesan, Krishnaraju, Chidmabaram, Kumarappan, Dhurke, Rajeshri
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2023
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10297899/
https://www.ncbi.nlm.nih.gov/pubmed/37367128
http://dx.doi.org/10.3390/gels9060457
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author Ghazwani, Mohammed
Vasudevan, Rajalakshimi
Kandasamy, Geetha
Manusri, Naredla.
Devanandan, Praveen
Puvvada, Ranadheer Chowdary
Veeramani, Vinoth Prabhu
Paulsamy, Premalatha
Venkatesan, Krishnaraju
Chidmabaram, Kumarappan
Dhurke, Rajeshri
author_facet Ghazwani, Mohammed
Vasudevan, Rajalakshimi
Kandasamy, Geetha
Manusri, Naredla.
Devanandan, Praveen
Puvvada, Ranadheer Chowdary
Veeramani, Vinoth Prabhu
Paulsamy, Premalatha
Venkatesan, Krishnaraju
Chidmabaram, Kumarappan
Dhurke, Rajeshri
author_sort Ghazwani, Mohammed
collection PubMed
description The purpose of the present work was to develop nanoemulsion-based formulations of mirtazapine for intranasal delivery using a spray actuator to target the brain for treating depression. Research on the solubility of medications in different oils, surfactants, co-surfactants, and solvents has been done. Using pseudo-ternary phase diagrams, the various ratios of the surfactant and co-surfactant mix were computed. Thermotriggered nanoemulsion was formulated using different concentrations of poloxamer 407 (i.e., 15%, 15.5%, 16%, 16.5% up to 22%). Similarly, mucoadhesive nanoemulsion using 0.1% Carbopol and water-based plain nanoemulsions were also prepared for comparative assessment. The developed nanoemulsions were analyzed for physicochemical properties, i.e., physical appearance, pH, viscosity, and drug content. Drug-excipient incompatibility was determined by Fourier transform infrared spectral (FTIR) analysis and differential scanning calorimetry (DSC). In vitro drug diffusion studies were conducted for optimized formulations. Among the three formulations, RD1 showed the highest percentage of drug release. Ex vivo drug diffusion studies were conducted on freshly excised sheep nasal mucosa with Franz diffusion cell simulated nasal fluid (SNF) for all three formulations up to 6 h, and the thermotriggered nanoemulsion (RD1) showed 71.42% drug release with 42.64 nm particle size and a poly dispersity index of 0.354. The zeta potential was found to be −6.58. Based on the above data, it was concluded that thermotriggered nanoemulsion (RD1) has great potential to be used as an intranasal gel for treating depression in patients. It can offer great benefits by reducing dosing frequency and improving bioavailability of mirtazapine by direct nose-to-brain delivery.
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spelling pubmed-102978992023-06-28 Formulation of Intranasal Mucoadhesive Thermotriggered In Situ Gel Containing Mirtazapine as an Antidepressant Drug Ghazwani, Mohammed Vasudevan, Rajalakshimi Kandasamy, Geetha Manusri, Naredla. Devanandan, Praveen Puvvada, Ranadheer Chowdary Veeramani, Vinoth Prabhu Paulsamy, Premalatha Venkatesan, Krishnaraju Chidmabaram, Kumarappan Dhurke, Rajeshri Gels Article The purpose of the present work was to develop nanoemulsion-based formulations of mirtazapine for intranasal delivery using a spray actuator to target the brain for treating depression. Research on the solubility of medications in different oils, surfactants, co-surfactants, and solvents has been done. Using pseudo-ternary phase diagrams, the various ratios of the surfactant and co-surfactant mix were computed. Thermotriggered nanoemulsion was formulated using different concentrations of poloxamer 407 (i.e., 15%, 15.5%, 16%, 16.5% up to 22%). Similarly, mucoadhesive nanoemulsion using 0.1% Carbopol and water-based plain nanoemulsions were also prepared for comparative assessment. The developed nanoemulsions were analyzed for physicochemical properties, i.e., physical appearance, pH, viscosity, and drug content. Drug-excipient incompatibility was determined by Fourier transform infrared spectral (FTIR) analysis and differential scanning calorimetry (DSC). In vitro drug diffusion studies were conducted for optimized formulations. Among the three formulations, RD1 showed the highest percentage of drug release. Ex vivo drug diffusion studies were conducted on freshly excised sheep nasal mucosa with Franz diffusion cell simulated nasal fluid (SNF) for all three formulations up to 6 h, and the thermotriggered nanoemulsion (RD1) showed 71.42% drug release with 42.64 nm particle size and a poly dispersity index of 0.354. The zeta potential was found to be −6.58. Based on the above data, it was concluded that thermotriggered nanoemulsion (RD1) has great potential to be used as an intranasal gel for treating depression in patients. It can offer great benefits by reducing dosing frequency and improving bioavailability of mirtazapine by direct nose-to-brain delivery. MDPI 2023-06-02 /pmc/articles/PMC10297899/ /pubmed/37367128 http://dx.doi.org/10.3390/gels9060457 Text en © 2023 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Ghazwani, Mohammed
Vasudevan, Rajalakshimi
Kandasamy, Geetha
Manusri, Naredla.
Devanandan, Praveen
Puvvada, Ranadheer Chowdary
Veeramani, Vinoth Prabhu
Paulsamy, Premalatha
Venkatesan, Krishnaraju
Chidmabaram, Kumarappan
Dhurke, Rajeshri
Formulation of Intranasal Mucoadhesive Thermotriggered In Situ Gel Containing Mirtazapine as an Antidepressant Drug
title Formulation of Intranasal Mucoadhesive Thermotriggered In Situ Gel Containing Mirtazapine as an Antidepressant Drug
title_full Formulation of Intranasal Mucoadhesive Thermotriggered In Situ Gel Containing Mirtazapine as an Antidepressant Drug
title_fullStr Formulation of Intranasal Mucoadhesive Thermotriggered In Situ Gel Containing Mirtazapine as an Antidepressant Drug
title_full_unstemmed Formulation of Intranasal Mucoadhesive Thermotriggered In Situ Gel Containing Mirtazapine as an Antidepressant Drug
title_short Formulation of Intranasal Mucoadhesive Thermotriggered In Situ Gel Containing Mirtazapine as an Antidepressant Drug
title_sort formulation of intranasal mucoadhesive thermotriggered in situ gel containing mirtazapine as an antidepressant drug
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10297899/
https://www.ncbi.nlm.nih.gov/pubmed/37367128
http://dx.doi.org/10.3390/gels9060457
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