The Preparation and Evaluation of Cyanocobalamin Mucoadhesive Sublingual Tablets
Cobalamin (vitamin B<sub>12</sub>), an essential vitamin with low oral bioavailability, plays a vital role in cellular functions. This research aimed to enhance the absorption of vitamin B<sub>12</sub> using sublingual mucoadhesive tablets by increasing the residence time of...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-10-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/16/10/1412 |
| _version_ | 1797572622928576512 |
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| author | Anwar Ma’ali Hani Naseef Moammal Qurt Abdallah Damin Abukhalil Abdullah K. Rabba Israr Sabri |
| author_facet | Anwar Ma’ali Hani Naseef Moammal Qurt Abdallah Damin Abukhalil Abdullah K. Rabba Israr Sabri |
| author_sort | Anwar Ma’ali |
| collection | DOAJ |
| description | Cobalamin (vitamin B<sub>12</sub>), an essential vitamin with low oral bioavailability, plays a vital role in cellular functions. This research aimed to enhance the absorption of vitamin B<sub>12</sub> using sublingual mucoadhesive tablets by increasing the residence time of the drug at the administration site. This research involved the preparation of different 50 mg placebo formulas using different methods. Formulas with disintegration times less than one minute and appropriate physical characteristics were incorporated into 1 mg of cyanocobalamin (S1–S20) using the direct compression method. The tablets obtained were evaluated ex vivo for residence time, and only those remaining for >15 min were included. The final formulas (S5, S8, S11, and S20) were evaluated in several ways, including pre- and post-compression, drug content, mucoadhesive strength, dissolution, and Permeapad<sup>®</sup> permeation test employed in the Franz diffusion cell. After conducting the evaluation, formula S11 (Eudragit L100-55) emerged as the most favorable formulation. It exhibited a mucoadhesive residence time of 118.2 ± 2.89 min, required a detachment force of 26 ± 1 g, maintained a drug content of 99.124 ± 0.001699%, and achieved a 76.85% drug release over 22 h, fitting well with the Peppas–Sahlin kinetic model (R<sup>2</sup>: 0.9949). This suggests that the drug release process encompasses the Fickian and non-Fickian kinetic mechanisms. Furthermore, Eudragit L100-55 demonstrated the highest permeability, boasting a flux value of 6.387 ± 1.860 µg/h/cm<sup>2</sup>; over 6 h. These findings indicate that including this polymer in the formulation leads to an improved residence time, which positively impacts bioavailability. |
| first_indexed | 2024-03-10T20:58:35Z |
| format | Article |
| id | doaj.art-4e1a8ba14dd54e5aa7867de072ff3671 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-10T20:58:35Z |
| publishDate | 2023-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-4e1a8ba14dd54e5aa7867de072ff36712023-11-19T17:42:08ZengMDPI AGPharmaceuticals1424-82472023-10-011610141210.3390/ph16101412The Preparation and Evaluation of Cyanocobalamin Mucoadhesive Sublingual TabletsAnwar Ma’ali0Hani Naseef1Moammal Qurt2Abdallah Damin Abukhalil3Abdullah K. Rabba4Israr Sabri5Pharmacy Department, Faculty of Pharmacy, Nursing and Health Professions, Birzeit University, Ramallah P.O. Box 14, PalestinePharmacy Department, Faculty of Pharmacy, Nursing and Health Professions, Birzeit University, Ramallah P.O. Box 14, PalestinePharmacy Department, Faculty of Pharmacy, Nursing and Health Professions, Birzeit University, Ramallah P.O. Box 14, PalestinePharmacy Department, Faculty of Pharmacy, Nursing and Health Professions, Birzeit University, Ramallah P.O. Box 14, PalestinePharmacy Department, Faculty of Pharmacy, Nursing and Health Professions, Birzeit University, Ramallah P.O. Box 14, PalestinePharmacy Department, Faculty of Pharmacy, Nursing and Health Professions, Birzeit University, Ramallah P.O. Box 14, PalestineCobalamin (vitamin B<sub>12</sub>), an essential vitamin with low oral bioavailability, plays a vital role in cellular functions. This research aimed to enhance the absorption of vitamin B<sub>12</sub> using sublingual mucoadhesive tablets by increasing the residence time of the drug at the administration site. This research involved the preparation of different 50 mg placebo formulas using different methods. Formulas with disintegration times less than one minute and appropriate physical characteristics were incorporated into 1 mg of cyanocobalamin (S1–S20) using the direct compression method. The tablets obtained were evaluated ex vivo for residence time, and only those remaining for >15 min were included. The final formulas (S5, S8, S11, and S20) were evaluated in several ways, including pre- and post-compression, drug content, mucoadhesive strength, dissolution, and Permeapad<sup>®</sup> permeation test employed in the Franz diffusion cell. After conducting the evaluation, formula S11 (Eudragit L100-55) emerged as the most favorable formulation. It exhibited a mucoadhesive residence time of 118.2 ± 2.89 min, required a detachment force of 26 ± 1 g, maintained a drug content of 99.124 ± 0.001699%, and achieved a 76.85% drug release over 22 h, fitting well with the Peppas–Sahlin kinetic model (R<sup>2</sup>: 0.9949). This suggests that the drug release process encompasses the Fickian and non-Fickian kinetic mechanisms. Furthermore, Eudragit L100-55 demonstrated the highest permeability, boasting a flux value of 6.387 ± 1.860 µg/h/cm<sup>2</sup>; over 6 h. These findings indicate that including this polymer in the formulation leads to an improved residence time, which positively impacts bioavailability.https://www.mdpi.com/1424-8247/16/10/1412mucoadhesivecyanocobalaminPermeapad<sup>®</sup> permeation testEudragit L100-55xanthan gumHPC and HPMC |
| spellingShingle | Anwar Ma’ali Hani Naseef Moammal Qurt Abdallah Damin Abukhalil Abdullah K. Rabba Israr Sabri The Preparation and Evaluation of Cyanocobalamin Mucoadhesive Sublingual Tablets Pharmaceuticals mucoadhesive cyanocobalamin Permeapad<sup>®</sup> permeation test Eudragit L100-55 xanthan gum HPC and HPMC |
| title | The Preparation and Evaluation of Cyanocobalamin Mucoadhesive Sublingual Tablets |
| title_full | The Preparation and Evaluation of Cyanocobalamin Mucoadhesive Sublingual Tablets |
| title_fullStr | The Preparation and Evaluation of Cyanocobalamin Mucoadhesive Sublingual Tablets |
| title_full_unstemmed | The Preparation and Evaluation of Cyanocobalamin Mucoadhesive Sublingual Tablets |
| title_short | The Preparation and Evaluation of Cyanocobalamin Mucoadhesive Sublingual Tablets |
| title_sort | preparation and evaluation of cyanocobalamin mucoadhesive sublingual tablets |
| topic | mucoadhesive cyanocobalamin Permeapad<sup>®</sup> permeation test Eudragit L100-55 xanthan gum HPC and HPMC |
| url | https://www.mdpi.com/1424-8247/16/10/1412 |
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