Carbamazepine Gel Formulation as a Sustained Release Epilepsy Medication for Pediatric Use
This study aimed to develop a carbamazepine (CBZ) sustained release formulation suitable for pediatric use with a lower risk of precipitation. The CBZ was first prepared as sustained release microparticles, and then the microparticles were embedded in alginate beads, and finally, the beads were susp...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2019-09-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/11/10/488 |
| _version_ | 1818005613116915712 |
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| author | Saeid Mezail Mawazi Sinan Mohammed Abdullah Al-Mahmood Bappaditya Chatterjee Hazrina AB. Hadi Abd Almonem Doolaanea |
| author_facet | Saeid Mezail Mawazi Sinan Mohammed Abdullah Al-Mahmood Bappaditya Chatterjee Hazrina AB. Hadi Abd Almonem Doolaanea |
| author_sort | Saeid Mezail Mawazi |
| collection | DOAJ |
| description | This study aimed to develop a carbamazepine (CBZ) sustained release formulation suitable for pediatric use with a lower risk of precipitation. The CBZ was first prepared as sustained release microparticles, and then the microparticles were embedded in alginate beads, and finally, the beads were suspended in a gel vehicle. The microparticles were prepared by a solvent evaporation method utilizing ethyl cellulose as a sustained release polymer and were evaluated for particle size, encapsulation efficiency, and release profile. The beads were fabricated by the dropwise addition of sodium alginate in calcium chloride solution and characterized for size, shape, and release properties. The gel was prepared using iota carrageenan as the gelling agent and evaluated for appearance, syneresis, drug content uniformity, rheology, release profile, and stability. The microparticles exhibited a particle size of 135.01 ± 0.61 µm with a monodisperse distribution and an encapsulation efficiency of 83.89 ± 3.98%. The beads were monodispersed with an average size of 1.4 ± 0.05 mm and a sphericity factor of less than 0.05. The gel was prepared using a 1:1 ratio (gel vehicle to beads) and exhibited no syneresis, good homogeneity, and good shear-thinning properties. The release profile from the beads and from the gel was not significantly affected, maintaining similarity to the tablet form. The gel properties were maintained for one month real time stability, but the accelerated stability showed reduced viscosity and pH with time. In conclusion, CBZ in a gel sustained release dosage form combines the advantages of the suspension form in terms of dosing flexibility, and the advantages of the tablet form in regards to the sustained release profile. This dosage form should be further investigated in vivo in animal models before being considered in clinical trials. |
| first_indexed | 2024-04-14T04:46:39Z |
| format | Article |
| id | doaj.art-747b1dde62a944978e3f02266ea67765 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-14T04:46:39Z |
| publishDate | 2019-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-747b1dde62a944978e3f02266ea677652022-12-22T02:11:26ZengMDPI AGPharmaceutics1999-49232019-09-01111048810.3390/pharmaceutics11100488pharmaceutics11100488Carbamazepine Gel Formulation as a Sustained Release Epilepsy Medication for Pediatric UseSaeid Mezail Mawazi0Sinan Mohammed Abdullah Al-Mahmood1Bappaditya Chatterjee2Hazrina AB. Hadi3Abd Almonem Doolaanea4Department of Pharmaceutical Technology, Kulliyyah of Pharmacy, International Islamic University Malaysia, Kuantan 25200, MalaysiaPharmacy College, Al-Kitab University, Kirkuk 36010, IraqDepartment of Pharmaceutical Technology, Kulliyyah of Pharmacy, International Islamic University Malaysia, Kuantan 25200, MalaysiaDepartment of Pharmaceutical Technology, Kulliyyah of Pharmacy, International Islamic University Malaysia, Kuantan 25200, MalaysiaDepartment of Pharmaceutical Technology, Kulliyyah of Pharmacy, International Islamic University Malaysia, Kuantan 25200, MalaysiaThis study aimed to develop a carbamazepine (CBZ) sustained release formulation suitable for pediatric use with a lower risk of precipitation. The CBZ was first prepared as sustained release microparticles, and then the microparticles were embedded in alginate beads, and finally, the beads were suspended in a gel vehicle. The microparticles were prepared by a solvent evaporation method utilizing ethyl cellulose as a sustained release polymer and were evaluated for particle size, encapsulation efficiency, and release profile. The beads were fabricated by the dropwise addition of sodium alginate in calcium chloride solution and characterized for size, shape, and release properties. The gel was prepared using iota carrageenan as the gelling agent and evaluated for appearance, syneresis, drug content uniformity, rheology, release profile, and stability. The microparticles exhibited a particle size of 135.01 ± 0.61 µm with a monodisperse distribution and an encapsulation efficiency of 83.89 ± 3.98%. The beads were monodispersed with an average size of 1.4 ± 0.05 mm and a sphericity factor of less than 0.05. The gel was prepared using a 1:1 ratio (gel vehicle to beads) and exhibited no syneresis, good homogeneity, and good shear-thinning properties. The release profile from the beads and from the gel was not significantly affected, maintaining similarity to the tablet form. The gel properties were maintained for one month real time stability, but the accelerated stability showed reduced viscosity and pH with time. In conclusion, CBZ in a gel sustained release dosage form combines the advantages of the suspension form in terms of dosing flexibility, and the advantages of the tablet form in regards to the sustained release profile. This dosage form should be further investigated in vivo in animal models before being considered in clinical trials.https://www.mdpi.com/1999-4923/11/10/488gelsustained releasecarbamazepineepilepsypediatric |
| spellingShingle | Saeid Mezail Mawazi Sinan Mohammed Abdullah Al-Mahmood Bappaditya Chatterjee Hazrina AB. Hadi Abd Almonem Doolaanea Carbamazepine Gel Formulation as a Sustained Release Epilepsy Medication for Pediatric Use Pharmaceutics gel sustained release carbamazepine epilepsy pediatric |
| title | Carbamazepine Gel Formulation as a Sustained Release Epilepsy Medication for Pediatric Use |
| title_full | Carbamazepine Gel Formulation as a Sustained Release Epilepsy Medication for Pediatric Use |
| title_fullStr | Carbamazepine Gel Formulation as a Sustained Release Epilepsy Medication for Pediatric Use |
| title_full_unstemmed | Carbamazepine Gel Formulation as a Sustained Release Epilepsy Medication for Pediatric Use |
| title_short | Carbamazepine Gel Formulation as a Sustained Release Epilepsy Medication for Pediatric Use |
| title_sort | carbamazepine gel formulation as a sustained release epilepsy medication for pediatric use |
| topic | gel sustained release carbamazepine epilepsy pediatric |
| url | https://www.mdpi.com/1999-4923/11/10/488 |
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