A Systematic Approach to the Development of Cilostazol Nanosuspension by Liquid Antisolvent Precipitation (LASP) and Its Combination with Ultrasound

Nanosizing is an approach to improve the dissolution rate of poorly soluble drugs. The first aim of this work was to develop nanosuspension of cilostazol with liquid antisolvent precipitation (LASP) and its combination with ultrasound. Second, to systematically study the effect of bottom-up processi...

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Autores principales:	Emilia Jakubowska, Bartłomiej Milanowski, Janina Lulek
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	nanosuspension nanocrystals drug nanoparticles antisolvent precipitation sonoprecipitation cilostazol Biology (General) QH301-705.5 Chemistry QD1-999
Acceso en línea:	https://doaj.org/article/68d9a4dff8194ab39b4c8d8602a6e447
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spelling	oai:doaj.org-article:68d9a4dff8194ab39b4c8d8602a6e4472021-11-25T17:56:27ZA Systematic Approach to the Development of Cilostazol Nanosuspension by Liquid Antisolvent Precipitation (LASP) and Its Combination with Ultrasound10.3390/ijms2222124061422-00671661-6596https://doaj.org/article/68d9a4dff8194ab39b4c8d8602a6e4472021-11-01T00:00:00Zhttps://www.mdpi.com/1422-0067/22/22/12406https://doaj.org/toc/1661-6596https://doaj.org/toc/1422-0067Nanosizing is an approach to improve the dissolution rate of poorly soluble drugs. The first aim of this work was to develop nanosuspension of cilostazol with liquid antisolvent precipitation (LASP) and its combination with ultrasound. Second, to systematically study the effect of bottom-up processing factors on precipitated particles’ size and identify the optimal settings for the best reduction. After solvent and stabilizer screening, in-depth process characterization and optimization was performed using Design of Experiments. The work discusses the influence of critical factors found with statistical analysis: feed concentration, stabilizer amount, stirring speed and ultrasound energy governed by time and amplitude. LASP alone only generated particle size of a few microns, but combination with ultrasound was successful in nanosizing (d10 = 0.06, d50 = 0.33, d90 = 1.45 µm). Micro- and nanosuspension’s stability, particle morphology and solid state were studied. Nanosuspension displayed higher apparent solubility than equilibrium and superior dissolution rate over coarse cilostazol and microsuspension. A bottom-up method of precipitation-sonication was demonstrated to be a successful approach to improve the dissolution characteristics of poorly soluble, BCS class II drug cilostazol by reducing its particle size below micron scale, while retaining nanosuspension stability and unchanged crystalline form.Emilia JakubowskaBartłomiej MilanowskiJanina LulekMDPI AGarticlenanosuspensionnanocrystalsdrug nanoparticlesantisolvent precipitationsonoprecipitationcilostazolBiology (General)QH301-705.5ChemistryQD1-999ENInternational Journal of Molecular Sciences, Vol 22, Iss 12406, p 12406 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	nanosuspension nanocrystals drug nanoparticles antisolvent precipitation sonoprecipitation cilostazol Biology (General) QH301-705.5 Chemistry QD1-999
spellingShingle	nanosuspension nanocrystals drug nanoparticles antisolvent precipitation sonoprecipitation cilostazol Biology (General) QH301-705.5 Chemistry QD1-999 Emilia Jakubowska Bartłomiej Milanowski Janina Lulek A Systematic Approach to the Development of Cilostazol Nanosuspension by Liquid Antisolvent Precipitation (LASP) and Its Combination with Ultrasound
description	Nanosizing is an approach to improve the dissolution rate of poorly soluble drugs. The first aim of this work was to develop nanosuspension of cilostazol with liquid antisolvent precipitation (LASP) and its combination with ultrasound. Second, to systematically study the effect of bottom-up processing factors on precipitated particles’ size and identify the optimal settings for the best reduction. After solvent and stabilizer screening, in-depth process characterization and optimization was performed using Design of Experiments. The work discusses the influence of critical factors found with statistical analysis: feed concentration, stabilizer amount, stirring speed and ultrasound energy governed by time and amplitude. LASP alone only generated particle size of a few microns, but combination with ultrasound was successful in nanosizing (d10 = 0.06, d50 = 0.33, d90 = 1.45 µm). Micro- and nanosuspension’s stability, particle morphology and solid state were studied. Nanosuspension displayed higher apparent solubility than equilibrium and superior dissolution rate over coarse cilostazol and microsuspension. A bottom-up method of precipitation-sonication was demonstrated to be a successful approach to improve the dissolution characteristics of poorly soluble, BCS class II drug cilostazol by reducing its particle size below micron scale, while retaining nanosuspension stability and unchanged crystalline form.
format	article
author	Emilia Jakubowska Bartłomiej Milanowski Janina Lulek
author_facet	Emilia Jakubowska Bartłomiej Milanowski Janina Lulek
author_sort	Emilia Jakubowska
title	A Systematic Approach to the Development of Cilostazol Nanosuspension by Liquid Antisolvent Precipitation (LASP) and Its Combination with Ultrasound
title_short	A Systematic Approach to the Development of Cilostazol Nanosuspension by Liquid Antisolvent Precipitation (LASP) and Its Combination with Ultrasound
title_full	A Systematic Approach to the Development of Cilostazol Nanosuspension by Liquid Antisolvent Precipitation (LASP) and Its Combination with Ultrasound
title_fullStr	A Systematic Approach to the Development of Cilostazol Nanosuspension by Liquid Antisolvent Precipitation (LASP) and Its Combination with Ultrasound
title_full_unstemmed	A Systematic Approach to the Development of Cilostazol Nanosuspension by Liquid Antisolvent Precipitation (LASP) and Its Combination with Ultrasound
title_sort	systematic approach to the development of cilostazol nanosuspension by liquid antisolvent precipitation (lasp) and its combination with ultrasound
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/68d9a4dff8194ab39b4c8d8602a6e447
work_keys_str_mv	AT emiliajakubowska asystematicapproachtothedevelopmentofcilostazolnanosuspensionbyliquidantisolventprecipitationlaspanditscombinationwithultrasound AT bartłomiejmilanowski asystematicapproachtothedevelopmentofcilostazolnanosuspensionbyliquidantisolventprecipitationlaspanditscombinationwithultrasound AT janinalulek asystematicapproachtothedevelopmentofcilostazolnanosuspensionbyliquidantisolventprecipitationlaspanditscombinationwithultrasound AT emiliajakubowska systematicapproachtothedevelopmentofcilostazolnanosuspensionbyliquidantisolventprecipitationlaspanditscombinationwithultrasound AT bartłomiejmilanowski systematicapproachtothedevelopmentofcilostazolnanosuspensionbyliquidantisolventprecipitationlaspanditscombinationwithultrasound AT janinalulek systematicapproachtothedevelopmentofcilostazolnanosuspensionbyliquidantisolventprecipitationlaspanditscombinationwithultrasound
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A Systematic Approach to the Development of Cilostazol Nanosuspension by Liquid Antisolvent Precipitation (LASP) and Its Combination with Ultrasound

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