High-shear wet granulation of SMEDDS based on mesoporous carriers for improved carvedilol solubility

Kovačević, Mila (avtor), German Ilić, Ilija (avtor), Bolko Seljak, Katarina (avtor), Zvonar Pobirk, Alenka (avtor)

Mesoporous carriers are a convenient choice for the solidification of self-microemulsifying drug delivery systems (SMEDDS) designed to improve the solubility of poorly water-soluble drugs. They are known for high liquid load capacity and the ability to maintain characteristics of dry, free-flowing powders. Therefore, five different mesoporous carriers were used for the preparation of carvedilol-loaded SMEDDS granules by wet granulation methods—in paten (manually) and using a high-shear (HS) granulator. Granules with the highest SMEDDS content (63% and 66% of total granules mass, respectively) and suitable flow properties were obtained by Syloid$^®$ 244FP and Neusilin$^®$ US2. SMEDDS loaded granules produced by HS granulation showed superior flow characteristics compared to those obtained manually. All SMEDDS granules exhibited fast in vitro release, with 93% of carvedilol releasing from Syloid$^®$ 244FP-based granules in 5 min. Upon compaction into self-microemulsifying tablets, suitable tablet hardness and very fast disintegration time were achieved, thus producing orodispersible tablets. The compaction slightly slowed down the carvedilol release rate; nevertheless, upon 1 h (at pH 1.2) or 4 h (at pH 6.8) of in vitro dissolution testing, the amount of released drug was comparable with granules, confirming the suitability of orodispersible tablets for the production of the SMEDDS loaded single unit oral dosage form.

• Jezik: Angleški jezik
• Ključne besede: SMEDDS, mesoporous carriers, wet granulation, high-shear granulator
• Vrsta gradiva: Članek v reviji
• Tipologija: 1.01 - Izvirni znanstveni članek
• Organizacija: FFA - Fakulteta za farmacijo
• Status publikacije: Objavljeno
• Različica publikacije: Objavljena publikacija
• Leto izida: 2022
• Št. strani: 21 str.
• Številčenje: Vol. 14, iss. 10, art. 2077
• PID: 20.500.12556/RUL-141617
• UDK: 544.351.3:621.6.04
• ISSN pri članku: 1999-4923
• DOI: 10.3390/pharmaceutics14102077
• COBISS.SI-ID: 123836163
• Datum objave v RUL: 03.10.2022

Gradivo je del revije

• Naslov: Pharmaceutics
• Skrajšan naslov: Pharmaceutics
• Založnik: MDPI
• ISSN: 1999-4923
• COBISS.SI-ID: 517949977

Licence

• Licenca: CC BY 4.0, Creative Commons Priznanje avtorstva 4.0 Mednarodna
• Povezava: http://creativecommons.org/licenses/by/4.0/deed.sl
• Opis: To je standardna licenca Creative Commons, ki daje uporabnikom največ možnosti za nadaljnjo uporabo dela, pri čemer morajo navesti avtorja.

Sekundarni jezik

• Jezik: Slovenski jezik
• Ključne besede: SMEDDS, mezoporozni nosilci, mokra granulacija, visokostrižni granulator, granulat, topnost

Projekti

• Financer: ARRS - Agencija za raziskovalno dejavnost Republike Slovenije
• Številka projekta: P1-0189
• Naslov: Farmacevtska tehnologija: od dostavnih sistemov učinkovin do terapijskih izidov zdravil pri otrocih in starostnikih

• Financer: Drugi - Drug financer ali več financerjev
• Program financ.: Public Scholarship, Development, Disability and Maintenance Fund of Republic of Slovenia, Ad futura scholarship