Biopharmaceutical Study of Triamcinolone Acetonide Semisolid Formulations for Sublingual and Buccal Administration
The mouth can be affected by important inflammatory processes resulting from localized or systemic diseases such as diabetes, AIDS and leukemia, among others, and are manifested in various types of buccal sores typically presenting pain. This work focuses on the design, formulation, and characteriza...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-07-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/13/7/1080 |
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| author | Marta Márquez Valls Alejandra Martínez Labrador Lyda Halbaut Bellowa Doménica Bravo Torres Paulo C. Granda Montserrat Miñarro Carmona David Limón Ana C. Calpena Campmany |
| author_facet | Marta Márquez Valls Alejandra Martínez Labrador Lyda Halbaut Bellowa Doménica Bravo Torres Paulo C. Granda Montserrat Miñarro Carmona David Limón Ana C. Calpena Campmany |
| author_sort | Marta Márquez Valls |
| collection | DOAJ |
| description | The mouth can be affected by important inflammatory processes resulting from localized or systemic diseases such as diabetes, AIDS and leukemia, among others, and are manifested in various types of buccal sores typically presenting pain. This work focuses on the design, formulation, and characterization of four semisolid formulations for oral mucosa in order to symptomatically treat these painful processes. The formulations have two active pharmaceutical ingredients, triamcinolone acetonide (TA) and lidocaine hydrochloride (LIDO). The formula also contains, as an excipient, Orabase<sup>®</sup>, which is a protective, hydrophobic, and anhydrous adhesive vehicle, used to retain or facilitate the application of active pharmaceutical ingredients to the oral mucosa. After designing the formulations, an analytical method for TA was validated using HPLC so as to achieve reliable analytical results. Franz-type diffusion cells were used to perform drug release studies using synthetic membrane, and permeation studies using buccal mucosa, estimating the amount and rate of TA permeated across the tissue. Additionally, sublingual permeation studies were carried out to evaluate a scenario of a continuous contact of the tongue with the applied formulation. Permeation fluxes and the amount of TA retained within sublingual mucosa were similar to those in buccal mucosa, also implying anti-inflammatory activity in the part of the tongue that is in direct contact with the formulation. In addition, the dynamic conditions of the mouth were recreated in terms of the presence of phosphate buffered saline, constant movement of the tongue, pH, and temperature, using dissolution equipment. The amount of TA released into the phosphate buffered saline in dynamic conditions (subject to being ingested) is well below the normal oral doses of TA, for which the formulation can be considered safe. The formulations applied to buccal or sublingual mucosas under dynamic conditions permit the successful retention of TA within either tissue, where it exerts anti-inflammatory activity. The four formulations studied show a pseudoplastic and thixotropic behavior, ideal for topical application. These results evidence the potential of these topical formulations in the treatment of inflammatory processes in the buccal mucosa. |
| first_indexed | 2024-03-10T09:28:16Z |
| format | Article |
| id | doaj.art-3584faf2525a4b1786ac5489c02539be |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T09:28:16Z |
| publishDate | 2021-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-3584faf2525a4b1786ac5489c02539be2023-11-22T04:41:43ZengMDPI AGPharmaceutics1999-49232021-07-01137108010.3390/pharmaceutics13071080Biopharmaceutical Study of Triamcinolone Acetonide Semisolid Formulations for Sublingual and Buccal AdministrationMarta Márquez Valls0Alejandra Martínez Labrador1Lyda Halbaut Bellowa2Doménica Bravo Torres3Paulo C. Granda4Montserrat Miñarro Carmona5David Limón6Ana C. Calpena Campmany7Department of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Science, University of Barcelona, Av. Joan XXIII 29-31, 08028 Barcelona, SpainDepartment of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Science, University of Barcelona, Av. Joan XXIII 29-31, 08028 Barcelona, SpainDepartment of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Science, University of Barcelona, Av. Joan XXIII 29-31, 08028 Barcelona, SpainDepartment of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Science, University of Barcelona, Av. Joan XXIII 29-31, 08028 Barcelona, SpainDepartment of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Science, University of Barcelona, Av. Joan XXIII 29-31, 08028 Barcelona, SpainDepartment of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Science, University of Barcelona, Av. Joan XXIII 29-31, 08028 Barcelona, SpainDepartment of Pharmacology, Toxicology and Therapeutic Chemistry, Faculty of Pharmacy and Food Science, University of Barcelona, Av. Joan XXIII 29-31, 08028 Barcelona, SpainDepartment of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Science, University of Barcelona, Av. Joan XXIII 29-31, 08028 Barcelona, SpainThe mouth can be affected by important inflammatory processes resulting from localized or systemic diseases such as diabetes, AIDS and leukemia, among others, and are manifested in various types of buccal sores typically presenting pain. This work focuses on the design, formulation, and characterization of four semisolid formulations for oral mucosa in order to symptomatically treat these painful processes. The formulations have two active pharmaceutical ingredients, triamcinolone acetonide (TA) and lidocaine hydrochloride (LIDO). The formula also contains, as an excipient, Orabase<sup>®</sup>, which is a protective, hydrophobic, and anhydrous adhesive vehicle, used to retain or facilitate the application of active pharmaceutical ingredients to the oral mucosa. After designing the formulations, an analytical method for TA was validated using HPLC so as to achieve reliable analytical results. Franz-type diffusion cells were used to perform drug release studies using synthetic membrane, and permeation studies using buccal mucosa, estimating the amount and rate of TA permeated across the tissue. Additionally, sublingual permeation studies were carried out to evaluate a scenario of a continuous contact of the tongue with the applied formulation. Permeation fluxes and the amount of TA retained within sublingual mucosa were similar to those in buccal mucosa, also implying anti-inflammatory activity in the part of the tongue that is in direct contact with the formulation. In addition, the dynamic conditions of the mouth were recreated in terms of the presence of phosphate buffered saline, constant movement of the tongue, pH, and temperature, using dissolution equipment. The amount of TA released into the phosphate buffered saline in dynamic conditions (subject to being ingested) is well below the normal oral doses of TA, for which the formulation can be considered safe. The formulations applied to buccal or sublingual mucosas under dynamic conditions permit the successful retention of TA within either tissue, where it exerts anti-inflammatory activity. The four formulations studied show a pseudoplastic and thixotropic behavior, ideal for topical application. These results evidence the potential of these topical formulations in the treatment of inflammatory processes in the buccal mucosa.https://www.mdpi.com/1999-4923/13/7/1080triamcinolone acetonidebuccal administrationsemisolid formulationsthixotropic behaviourlidocaine hydrochlorideFranz-type diffusion cells |
| spellingShingle | Marta Márquez Valls Alejandra Martínez Labrador Lyda Halbaut Bellowa Doménica Bravo Torres Paulo C. Granda Montserrat Miñarro Carmona David Limón Ana C. Calpena Campmany Biopharmaceutical Study of Triamcinolone Acetonide Semisolid Formulations for Sublingual and Buccal Administration Pharmaceutics triamcinolone acetonide buccal administration semisolid formulations thixotropic behaviour lidocaine hydrochloride Franz-type diffusion cells |
| title | Biopharmaceutical Study of Triamcinolone Acetonide Semisolid Formulations for Sublingual and Buccal Administration |
| title_full | Biopharmaceutical Study of Triamcinolone Acetonide Semisolid Formulations for Sublingual and Buccal Administration |
| title_fullStr | Biopharmaceutical Study of Triamcinolone Acetonide Semisolid Formulations for Sublingual and Buccal Administration |
| title_full_unstemmed | Biopharmaceutical Study of Triamcinolone Acetonide Semisolid Formulations for Sublingual and Buccal Administration |
| title_short | Biopharmaceutical Study of Triamcinolone Acetonide Semisolid Formulations for Sublingual and Buccal Administration |
| title_sort | biopharmaceutical study of triamcinolone acetonide semisolid formulations for sublingual and buccal administration |
| topic | triamcinolone acetonide buccal administration semisolid formulations thixotropic behaviour lidocaine hydrochloride Franz-type diffusion cells |
| url | https://www.mdpi.com/1999-4923/13/7/1080 |
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