Effect of solvent selection on drug loading and amorphisation in mesoporous silica particles

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22340%2F19%3A43919133" target="_blank" >RIV/60461373:22340/19:43919133 - isvavai.cz</a>

Výsledek na webu

<a href="https://doi.org/10.1016/j.ijpharm.2018.10.075" target="_blank" >https://doi.org/10.1016/j.ijpharm.2018.10.075</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.ijpharm.2018.10.075" target="_blank" >10.1016/j.ijpharm.2018.10.075</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Effect of solvent selection on drug loading and amorphisation in mesoporous silica particles

Popis výsledku v původním jazyce

Increasing the dissolution rate of poorly water-soluble active pharmaceutical ingredients (APIs) is a key strategy used for improving their oral bioavailability. One of the formulation approaches is API loading to mesoporous carrier particles, which can increase the dissolution rate through the combination of improved powder wett-ability and dispersion, higher surface area, and API conversion from crystalline to the amorphous state. From the formulation process point of view, the maximum achievable drug loading is a crucial parameter, which depends on the loading method. Drug loading by sorption from a solution is a technologically attractive approach, since it involves familiar unit operations (mixing, filtration, drying). However, the success of the equilibrium sorption approach depends on the choice of the solvent. In this work we present an experimental study of loading efficiency to mesoporous silica particles, based on a set of 10 APIs combined with 6 different solvents at a range of concentrations. We show that due to the competitive nature of the adsorption process, the solvent with the highest API solubility is not necessarily the best candidate for maximising the API loading. Based on the investigated drug-solvent combinations, we show that the dielectric constant of the solvent is a good predictor of loading efficiency and can be used as a general guideline for solvent selection. On the other hand, we did not find any systematic correlation between commonly measured API properties such as logP and their loading efficiency.

Název v anglickém jazyce

Effect of solvent selection on drug loading and amorphisation in mesoporous silica particles

Popis výsledku anglicky

Increasing the dissolution rate of poorly water-soluble active pharmaceutical ingredients (APIs) is a key strategy used for improving their oral bioavailability. One of the formulation approaches is API loading to mesoporous carrier particles, which can increase the dissolution rate through the combination of improved powder wett-ability and dispersion, higher surface area, and API conversion from crystalline to the amorphous state. From the formulation process point of view, the maximum achievable drug loading is a crucial parameter, which depends on the loading method. Drug loading by sorption from a solution is a technologically attractive approach, since it involves familiar unit operations (mixing, filtration, drying). However, the success of the equilibrium sorption approach depends on the choice of the solvent. In this work we present an experimental study of loading efficiency to mesoporous silica particles, based on a set of 10 APIs combined with 6 different solvents at a range of concentrations. We show that due to the competitive nature of the adsorption process, the solvent with the highest API solubility is not necessarily the best candidate for maximising the API loading. Based on the investigated drug-solvent combinations, we show that the dielectric constant of the solvent is a good predictor of loading efficiency and can be used as a general guideline for solvent selection. On the other hand, we did not find any systematic correlation between commonly measured API properties such as logP and their loading efficiency.

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

20401 - Chemical engineering (plants, products)

Projekt

<a href="/cs/project/GA16-12291S" target="_blank" >GA16-12291S: Hierarchický přístup ke studiu rovnováhy mezi pevnou a kapalnou fází v komplexních systémech: teorie, simulace a experiment</a><br>

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

International Journal of Pharmaceutics

ISSN

0378-5173

e-ISSN

—

Svazek periodika

555

Číslo periodika v rámci svazku

30 January 2019

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

9

Strana od-do

19-27

Kód UT WoS článku

000455009300003

EID výsledku v databázi Scopus

2-s2.0-85056837463