Silica particles with three levels of porosity for efficient melt amorphisation of drugs

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22340%2F19%3A43918383" target="_blank" >RIV/60461373:22340/19:43918383 - isvavai.cz</a>

Výsledek na webu

<a href="https://doi.org/10.1016/j.micromeso.2018.07.033" target="_blank" >https://doi.org/10.1016/j.micromeso.2018.07.033</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.micromeso.2018.07.033" target="_blank" >10.1016/j.micromeso.2018.07.033</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Silica particles with three levels of porosity for efficient melt amorphisation of drugs

Popis výsledku v původním jazyce

Silica particles with a unique multi-level pore structure have been prepared in order to enable efficient melt-in amorphisation of pharmaceutical substances. The dissolution rate of drugs with a low aqueous solubility can be enhanced by their conversion from a crystalline to an amorphous form. In order to avoid spontaneous recrystallisation over time, the amorphous form must be stabilised, in this case by melt-in sorption into a porous carrier. To stabilise the amorphous state, pore diameters not exceeding approximately ten times the equivalent molecular diameter are required. However, since the permeability of porous media scales with the square of the mean pore diameter, carrier particles with pores in the nanometer range suffer from slow melt-in rates. Therefore, silica particles with a novel multi-level porous structure have been proposed in this work. The particles combine a central hollow cavity, a network of conducting macro-pores for enhanced transport rate, and a mesoporous matrix for efficient stabilisation of the amorphous state. The particles were prepared by the hydrolysis of TEOS using a soft-templating method with octylamine. We show that by systematically modulating the hydrolysis rate by the presence of ethanol (a reaction by-product), particles with the desired pore structure, particle size and morphology can be formed. Furthermore, we demonstrate their superior transport properties during melt sorption, high drug loading capacity and the ability to stabilise the amorphous state of a drug.

Název v anglickém jazyce

Silica particles with three levels of porosity for efficient melt amorphisation of drugs

Popis výsledku anglicky

Silica particles with a unique multi-level pore structure have been prepared in order to enable efficient melt-in amorphisation of pharmaceutical substances. The dissolution rate of drugs with a low aqueous solubility can be enhanced by their conversion from a crystalline to an amorphous form. In order to avoid spontaneous recrystallisation over time, the amorphous form must be stabilised, in this case by melt-in sorption into a porous carrier. To stabilise the amorphous state, pore diameters not exceeding approximately ten times the equivalent molecular diameter are required. However, since the permeability of porous media scales with the square of the mean pore diameter, carrier particles with pores in the nanometer range suffer from slow melt-in rates. Therefore, silica particles with a novel multi-level porous structure have been proposed in this work. The particles combine a central hollow cavity, a network of conducting macro-pores for enhanced transport rate, and a mesoporous matrix for efficient stabilisation of the amorphous state. The particles were prepared by the hydrolysis of TEOS using a soft-templating method with octylamine. We show that by systematically modulating the hydrolysis rate by the presence of ethanol (a reaction by-product), particles with the desired pore structure, particle size and morphology can be formed. Furthermore, we demonstrate their superior transport properties during melt sorption, high drug loading capacity and the ability to stabilise the amorphous state of a drug.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

20402 - Chemical process engineering

Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2019

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Microporous and mesoporous materials

ISSN

1387-1811

e-ISSN

—

Svazek periodika

274

Číslo periodika v rámci svazku

15 January 2019

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

9

Strana od-do

61-69

Kód UT WoS článku

000450378300008

EID výsledku v databázi Scopus

2-s2.0-85050633962