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Mechanistic aspects of drug loading in liquisolid systems with hydrophilic lipid-based mixtures

B. Vraníková, A. Niederquell, F. Ditzinger, Z. Šklubalová, M. Kuentz,

. 2020 ; 578 (-) : 119099. [pub] 20200130

Language English Country Netherlands

Document type Journal Article

Despite the increasing interest in pharmaceutical use of mesoporous silica, there is still only limited knowledge on mechanisms of pore loading and subsequent drug desorption and release. Hence the aim of this work was to address the mechanistic aspects of drug loading into the mesoporous silica pores and to minimise the risk of pore clogging. Hydrophilic solvents (polysorbate 20 and polyethylene glycol 200) with high dissolving capacity for the model drug celecoxib were studied for their surface tension as well as dynamic viscosity by considering hydration. As an innovation in liquisolid systems preparation, a rather simple drug loading method on a mesoporous carrier was introduced by using semi-volatile solvent mixtures. Fast liquid loading into the pores was achieved due to the lowered viscosity and surface tension of the whole solvent system. Drug release kinetics suggested that lipid-based formulations belonging to class IV of Lipid Formulation Classification System may exhibit a lower risk of incomplete desorption from a carrier. The utilisation of volatile solvents during preparation had no negative impact on the liquisolid systems' dissolution behaviour. All prepared formulations showed similar significantly faster dissolution profiles compared to the physical mixture. The novel approach has potential to promote liquisolid applications in pharmaceutics.

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$a Vraníková, Barbora $u Department of Pharmaceutical Technology, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic; Institute for Pharma Technology, University of Applied Sciences and Arts Northwestern Switzerland, School of Life Sciences FHNW, Hofackerstr. 30, 4132 Muttenz, Switzerland. Electronic address: vranikovab@faf.cuni.cz.
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$a Despite the increasing interest in pharmaceutical use of mesoporous silica, there is still only limited knowledge on mechanisms of pore loading and subsequent drug desorption and release. Hence the aim of this work was to address the mechanistic aspects of drug loading into the mesoporous silica pores and to minimise the risk of pore clogging. Hydrophilic solvents (polysorbate 20 and polyethylene glycol 200) with high dissolving capacity for the model drug celecoxib were studied for their surface tension as well as dynamic viscosity by considering hydration. As an innovation in liquisolid systems preparation, a rather simple drug loading method on a mesoporous carrier was introduced by using semi-volatile solvent mixtures. Fast liquid loading into the pores was achieved due to the lowered viscosity and surface tension of the whole solvent system. Drug release kinetics suggested that lipid-based formulations belonging to class IV of Lipid Formulation Classification System may exhibit a lower risk of incomplete desorption from a carrier. The utilisation of volatile solvents during preparation had no negative impact on the liquisolid systems' dissolution behaviour. All prepared formulations showed similar significantly faster dissolution profiles compared to the physical mixture. The novel approach has potential to promote liquisolid applications in pharmaceutics.
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$a Niederquell, Andreas $u Institute for Pharma Technology, University of Applied Sciences and Arts Northwestern Switzerland, School of Life Sciences FHNW, Hofackerstr. 30, 4132 Muttenz, Switzerland. Electronic address: andreas.niederquell@fhnw.ch.
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$a Ditzinger, Felix $u Institute for Pharma Technology, University of Applied Sciences and Arts Northwestern Switzerland, School of Life Sciences FHNW, Hofackerstr. 30, 4132 Muttenz, Switzerland; Department of Pharmaceutical Sciences, University of Basel, Klingelbergstr. 50, 4056 Basel, Switzerland. Electronic address: felix.ditzinger@fhnw.ch.
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$a Šklubalová, Zdenka $u Department of Pharmaceutical Technology, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic. Electronic address: sklubalova@faf.cuni.cz.
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$a Kuentz, Martin $u Institute for Pharma Technology, University of Applied Sciences and Arts Northwestern Switzerland, School of Life Sciences FHNW, Hofackerstr. 30, 4132 Muttenz, Switzerland. Electronic address: martin.kuentz@fhnw.ch.
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