In order to improve the bioavailability of poorly water soluble drugs, an effective technique is the coprecipitation of the drug with a hydrophilic polymer. In this work, the coprecipitation of polyvinylpyrrolidone/nimesulide (PVP/NIM) nanostructured microparticles using Supercritical Antisolvent (SAS) was proposed. The effects of the main process parameters, such as polymer/drug ratio, overall concentration, operating pressure and temperature were investigated to identify successful operating conditions for SAS coprecipitation. Microparticles with a mean diameter ranging between 1.7 and 4 μm (calculated in number of particles) were successfully produced; they were characterized using different analytical techniques, to demonstrate the occurred coprecipitation. Precipitation yield was found to be about 100% with respect to the amount of solute dissolved in the starting solution. Drug release analyses revealed that Nimesulide dissolution rate from PVP/NIM microparticles in a phosphate buffered saline solution (PBS) was 2.5 times faster with respect to unprocessed drug. The possible precipitation mechanisms involved in the process were discussed.
Formation of PVP/nimesulide microspheres by supercritical antisolvent coprecipitation
PROSAPIO, VALENTINA;REVERCHON, Ernesto;DE MARCO, Iolanda
2016
Abstract
In order to improve the bioavailability of poorly water soluble drugs, an effective technique is the coprecipitation of the drug with a hydrophilic polymer. In this work, the coprecipitation of polyvinylpyrrolidone/nimesulide (PVP/NIM) nanostructured microparticles using Supercritical Antisolvent (SAS) was proposed. The effects of the main process parameters, such as polymer/drug ratio, overall concentration, operating pressure and temperature were investigated to identify successful operating conditions for SAS coprecipitation. Microparticles with a mean diameter ranging between 1.7 and 4 μm (calculated in number of particles) were successfully produced; they were characterized using different analytical techniques, to demonstrate the occurred coprecipitation. Precipitation yield was found to be about 100% with respect to the amount of solute dissolved in the starting solution. Drug release analyses revealed that Nimesulide dissolution rate from PVP/NIM microparticles in a phosphate buffered saline solution (PBS) was 2.5 times faster with respect to unprocessed drug. The possible precipitation mechanisms involved in the process were discussed.File | Dimensione | Formato | |
---|---|---|---|
178 De Marco Definitivo.pdf
non disponibili
Tipologia:
Versione editoriale (versione pubblicata con il layout dell'editore)
Licenza:
NON PUBBLICO - Accesso privato/ristretto
Dimensione
1.97 MB
Formato
Adobe PDF
|
1.97 MB | Adobe PDF | Visualizza/Apri Richiedi una copia |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.