Nicotinamide-based agglomerates of ibuprofen: formulation, solid state characterization and evaluation of tableting performance with in-silico investigation
Abstract Background The objective of the present investigation was to obtain directly compressible agglomerates of ibuprofen with nicotinamide by a quasi-emulsification solvent diffusion technique. Ibuprofen-nicotinamide agglomerates were prepared by quasi-emulsification solvent diffusion technique...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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SpringerOpen
2023-08-01
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| Series: | Future Journal of Pharmaceutical Sciences |
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| Online Access: | https://doi.org/10.1186/s43094-023-00521-0 |
| _version_ | 1797577607188840448 |
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| author | Prerna Hemant Sidwadkar Nitin Hindurao Salunkhe Kailas Krishnat Mali Vijay Bapu Metkari Durgesh Paresh Bidye |
| author_facet | Prerna Hemant Sidwadkar Nitin Hindurao Salunkhe Kailas Krishnat Mali Vijay Bapu Metkari Durgesh Paresh Bidye |
| author_sort | Prerna Hemant Sidwadkar |
| collection | DOAJ |
| description | Abstract Background The objective of the present investigation was to obtain directly compressible agglomerates of ibuprofen with nicotinamide by a quasi-emulsification solvent diffusion technique. Ibuprofen-nicotinamide agglomerates were prepared by quasi-emulsification solvent diffusion technique using ethanol (good solvent), water (poor solvent), and chloroform (bridging liquid). The prepared agglomerates were characterized by ATR-FTIR, powder X-ray diffraction, differential scanning calorimetry, and scanning electron microscopy and were evaluated for tableting performance and in vitro drug release. To appropriately identify the hydrogen bonding sites, a thorough understanding of the structures of API and coformer is necessary, hence molecular docking approach was implemented to depict the interaction between the proposed coformer and COX-2 protein (PDB Id:4PH9). Results The percent yield of agglomerates was in the range of 85–98 w/w%, and drug content for all batches was in the range of 96–99%. The microphotographs showed irregular circularly shaped agglomerates. ATR-FTIR study showed a strong possibility of hydrogen bonding between ibuprofen and nicotinamide. The crystallinity of ibuprofen was slightly reduced and confirmed by P-XRD and DSC. Crushing strength and friability studies showed good handling qualities of ibuprofen agglomerates. Heckel plot studies showed low mean yield pressure and high tensile strength, indicating excellent compressibility and compactibility of ibuprofen agglomerates. More than 90% drug release was obtained within 60 min in PBS (pH 7.4). The docking studies revealed that nicotinamide individually has –CDOCKER energy 16.8109 where coformer showed 29.0584, which indicates coformer has a better binding affinity to target as compared to nicotinamide individual. Conclusions It can be concluded that the agglomerates improved the dissolution, tableting performance, and solid-state properties of ibuprofen and hence can be useful to improve the therapeutic performance of ibuprofen. Graphic Abstract |
| first_indexed | 2024-03-10T22:11:30Z |
| format | Article |
| id | doaj.art-7fc8996107b3433d9c28b750e237d84a |
| institution | Directory Open Access Journal |
| issn | 2314-7253 |
| language | English |
| last_indexed | 2024-03-10T22:11:30Z |
| publishDate | 2023-08-01 |
| publisher | SpringerOpen |
| record_format | Article |
| series | Future Journal of Pharmaceutical Sciences |
| spelling | doaj.art-7fc8996107b3433d9c28b750e237d84a2023-11-19T12:36:40ZengSpringerOpenFuture Journal of Pharmaceutical Sciences2314-72532023-08-019111310.1186/s43094-023-00521-0Nicotinamide-based agglomerates of ibuprofen: formulation, solid state characterization and evaluation of tableting performance with in-silico investigationPrerna Hemant Sidwadkar0Nitin Hindurao Salunkhe1Kailas Krishnat Mali2Vijay Bapu Metkari3Durgesh Paresh Bidye4Department of Pharmaceutics, Adarsh College of PharmacyDepartment of Pharmaceutics, Adarsh College of PharmacyDepartment of Pharmaceutics, Adarsh College of PharmacyDepartment of Pharmaceutics, Adarsh College of PharmacyDepartment of Pharmaceutical Chemistry, JSS College of PharmacyAbstract Background The objective of the present investigation was to obtain directly compressible agglomerates of ibuprofen with nicotinamide by a quasi-emulsification solvent diffusion technique. Ibuprofen-nicotinamide agglomerates were prepared by quasi-emulsification solvent diffusion technique using ethanol (good solvent), water (poor solvent), and chloroform (bridging liquid). The prepared agglomerates were characterized by ATR-FTIR, powder X-ray diffraction, differential scanning calorimetry, and scanning electron microscopy and were evaluated for tableting performance and in vitro drug release. To appropriately identify the hydrogen bonding sites, a thorough understanding of the structures of API and coformer is necessary, hence molecular docking approach was implemented to depict the interaction between the proposed coformer and COX-2 protein (PDB Id:4PH9). Results The percent yield of agglomerates was in the range of 85–98 w/w%, and drug content for all batches was in the range of 96–99%. The microphotographs showed irregular circularly shaped agglomerates. ATR-FTIR study showed a strong possibility of hydrogen bonding between ibuprofen and nicotinamide. The crystallinity of ibuprofen was slightly reduced and confirmed by P-XRD and DSC. Crushing strength and friability studies showed good handling qualities of ibuprofen agglomerates. Heckel plot studies showed low mean yield pressure and high tensile strength, indicating excellent compressibility and compactibility of ibuprofen agglomerates. More than 90% drug release was obtained within 60 min in PBS (pH 7.4). The docking studies revealed that nicotinamide individually has –CDOCKER energy 16.8109 where coformer showed 29.0584, which indicates coformer has a better binding affinity to target as compared to nicotinamide individual. Conclusions It can be concluded that the agglomerates improved the dissolution, tableting performance, and solid-state properties of ibuprofen and hence can be useful to improve the therapeutic performance of ibuprofen. Graphic Abstracthttps://doi.org/10.1186/s43094-023-00521-0IbuprofenNicotinamideAgglomeratesDissolution rateQuasi-emulsification methodMolecular docking |
| spellingShingle | Prerna Hemant Sidwadkar Nitin Hindurao Salunkhe Kailas Krishnat Mali Vijay Bapu Metkari Durgesh Paresh Bidye Nicotinamide-based agglomerates of ibuprofen: formulation, solid state characterization and evaluation of tableting performance with in-silico investigation Future Journal of Pharmaceutical Sciences Ibuprofen Nicotinamide Agglomerates Dissolution rate Quasi-emulsification method Molecular docking |
| title | Nicotinamide-based agglomerates of ibuprofen: formulation, solid state characterization and evaluation of tableting performance with in-silico investigation |
| title_full | Nicotinamide-based agglomerates of ibuprofen: formulation, solid state characterization and evaluation of tableting performance with in-silico investigation |
| title_fullStr | Nicotinamide-based agglomerates of ibuprofen: formulation, solid state characterization and evaluation of tableting performance with in-silico investigation |
| title_full_unstemmed | Nicotinamide-based agglomerates of ibuprofen: formulation, solid state characterization and evaluation of tableting performance with in-silico investigation |
| title_short | Nicotinamide-based agglomerates of ibuprofen: formulation, solid state characterization and evaluation of tableting performance with in-silico investigation |
| title_sort | nicotinamide based agglomerates of ibuprofen formulation solid state characterization and evaluation of tableting performance with in silico investigation |
| topic | Ibuprofen Nicotinamide Agglomerates Dissolution rate Quasi-emulsification method Molecular docking |
| url | https://doi.org/10.1186/s43094-023-00521-0 |
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