Systematic Investigation of Wet-Milling Kinetics and Colloidal Stability of Pharmaceutical Nanocrystals

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60461373%3A22340%2F22%3A43924668" target="_blank" >RIV/60461373:22340/22:43924668 - isvavai.cz</a>

Výsledek na webu

<a href="https://pubs.acs.org/doi/full/10.1021/acs.cgd.2c00546" target="_blank" >https://pubs.acs.org/doi/full/10.1021/acs.cgd.2c00546</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1021/acs.cgd.2c00546" target="_blank" >10.1021/acs.cgd.2c00546</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Systematic Investigation of Wet-Milling Kinetics and Colloidal Stability of Pharmaceutical Nanocrystals

Popis výsledku v původním jazyce

The size reduction of poorly water-soluble crystalline active pharmaceutical ingredients (APIs) to submicrometer dimensions is an alternative to the formation of amorphous solid dispersions when aiming for dissolution rate and bioavailability enhancement. Pharmaceutical nanosuspensions can be produced by wet-stirred media milling, but there is no established classification for assessing the suitability of a given API for this process. The present work reports a systematic study of milling kinetics and colloidal stability of the resulting nanosuspension for 10 APIs (abiraterone acetate, apixaban, atorvastatin, candesartan cilexetil, deferasirox, hydrochlorothiazide, imiquimod, ivacaftor, tadalafil, and telmisartan) in combination with 6 different stabilizer systems that include SDS, Tween 80, HPMC, Poloxamer 188, DPPC, DPPG, MPEG-2000-DMPE, and their combinations. The combination of steric and electrostatic stabilization resulted in colloidally stable nanosuspensions for a broad spectrum of APIs not only for an already established combination of hydroxypropyl methylcellulose and sodium dodecyl sulfate but also for phospholipid-based stabilizers, which have so far not been widely used in the context of nanomilling. A new classification system of API suitability for nanosuspension formation by wet milling has been proposed on the basis of the texture and morphology of the crude crystals. © 2022 American Chemical Society.

Název v anglickém jazyce

Systematic Investigation of Wet-Milling Kinetics and Colloidal Stability of Pharmaceutical Nanocrystals

Popis výsledku anglicky

The size reduction of poorly water-soluble crystalline active pharmaceutical ingredients (APIs) to submicrometer dimensions is an alternative to the formation of amorphous solid dispersions when aiming for dissolution rate and bioavailability enhancement. Pharmaceutical nanosuspensions can be produced by wet-stirred media milling, but there is no established classification for assessing the suitability of a given API for this process. The present work reports a systematic study of milling kinetics and colloidal stability of the resulting nanosuspension for 10 APIs (abiraterone acetate, apixaban, atorvastatin, candesartan cilexetil, deferasirox, hydrochlorothiazide, imiquimod, ivacaftor, tadalafil, and telmisartan) in combination with 6 different stabilizer systems that include SDS, Tween 80, HPMC, Poloxamer 188, DPPC, DPPG, MPEG-2000-DMPE, and their combinations. The combination of steric and electrostatic stabilization resulted in colloidally stable nanosuspensions for a broad spectrum of APIs not only for an already established combination of hydroxypropyl methylcellulose and sodium dodecyl sulfate but also for phospholipid-based stabilizers, which have so far not been widely used in the context of nanomilling. A new classification system of API suitability for nanosuspension formation by wet milling has been proposed on the basis of the texture and morphology of the crude crystals. © 2022 American Chemical Society.

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/GX19-26127X" target="_blank" >GX19-26127X: Robotický nano-lékárník: Výrobní procesy budoucnosti pro personalisovaná terapeutika</a><br>

Návaznosti

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

Rok uplatnění

2022

Kód důvěrnosti údajů

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

Název periodika

Crystal Growth &amp; Design

ISSN

1528-7483

e-ISSN

1528-7505

Svazek periodika

22

Číslo periodika v rámci svazku

12

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

13

Strana od-do

6928-6940

Kód UT WoS článku

000878545900001

EID výsledku v databázi Scopus

2-s2.0-85140984200