High-Shear Wet Granulation of SMEDDS Based on Mesoporous Carriers for Improved Carvedilol Solubility
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 p...
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MDPI AG
2022-09-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/14/10/2077 |
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| author | Mila Kovačević Ilija German Ilić Katarina Bolko Seljak Alenka Zvonar Pobirk |
| author_facet | Mila Kovačević Ilija German Ilić Katarina Bolko Seljak Alenka Zvonar Pobirk |
| author_sort | Mila Kovačević |
| collection | DOAJ |
| description | 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<sup>®</sup> 244FP and Neusilin<sup>®</sup> 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<sup>®</sup> 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. |
| first_indexed | 2024-03-09T19:35:30Z |
| format | Article |
| id | doaj.art-4fc238a9b9dc49c59672b234f32a5f10 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-09T19:35:30Z |
| publishDate | 2022-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-4fc238a9b9dc49c59672b234f32a5f102023-11-24T01:55:23ZengMDPI AGPharmaceutics1999-49232022-09-011410207710.3390/pharmaceutics14102077High-Shear Wet Granulation of SMEDDS Based on Mesoporous Carriers for Improved Carvedilol SolubilityMila Kovačević0Ilija German Ilić1Katarina Bolko Seljak2Alenka Zvonar Pobirk3Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Ljubljana, 1000 Ljubljana, SloveniaDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Ljubljana, 1000 Ljubljana, SloveniaDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Ljubljana, 1000 Ljubljana, SloveniaDepartment of Pharmaceutical Technology, Faculty of Pharmacy, University of Ljubljana, 1000 Ljubljana, SloveniaMesoporous 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<sup>®</sup> 244FP and Neusilin<sup>®</sup> 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<sup>®</sup> 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.https://www.mdpi.com/1999-4923/14/10/2077SMEDDSmesoporous carrierswet granulationhigh-shear granulator |
| spellingShingle | Mila Kovačević Ilija German Ilić Katarina Bolko Seljak Alenka Zvonar Pobirk High-Shear Wet Granulation of SMEDDS Based on Mesoporous Carriers for Improved Carvedilol Solubility Pharmaceutics SMEDDS mesoporous carriers wet granulation high-shear granulator |
| title | High-Shear Wet Granulation of SMEDDS Based on Mesoporous Carriers for Improved Carvedilol Solubility |
| title_full | High-Shear Wet Granulation of SMEDDS Based on Mesoporous Carriers for Improved Carvedilol Solubility |
| title_fullStr | High-Shear Wet Granulation of SMEDDS Based on Mesoporous Carriers for Improved Carvedilol Solubility |
| title_full_unstemmed | High-Shear Wet Granulation of SMEDDS Based on Mesoporous Carriers for Improved Carvedilol Solubility |
| title_short | High-Shear Wet Granulation of SMEDDS Based on Mesoporous Carriers for Improved Carvedilol Solubility |
| title_sort | high shear wet granulation of smedds based on mesoporous carriers for improved carvedilol solubility |
| topic | SMEDDS mesoporous carriers wet granulation high-shear granulator |
| url | https://www.mdpi.com/1999-4923/14/10/2077 |
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