Orodispersible Films with Rupatadine Fumarate Enclosed in Ethylcellulose Microparticles as Drug Delivery Platform with Taste-Masking Effect
Orally disintegrating (orodispersible) films provide a versatile tool for drug administration, especially in the pediatric and geriatric population, since they reduce the risk of choking and do not necessitate drinking water during application. By considering their direct contact with the taste buds...
| Main Authors: | , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2022-03-01
|
| Series: | Materials |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1996-1944/15/6/2126 |
| _version_ | 1797445663889293312 |
|---|---|
| author | Katarzyna Olechno Bartosz Maciejewski Klaudia Głowacz Joanna Lenik Patrycja Ciosek-Skibińska Anna Basa Katarzyna Winnicka |
| author_facet | Katarzyna Olechno Bartosz Maciejewski Klaudia Głowacz Joanna Lenik Patrycja Ciosek-Skibińska Anna Basa Katarzyna Winnicka |
| author_sort | Katarzyna Olechno |
| collection | DOAJ |
| description | Orally disintegrating (orodispersible) films provide a versatile tool for drug administration, especially in the pediatric and geriatric population, since they reduce the risk of choking and do not necessitate drinking water during application. By considering their direct contact with the taste buds, palatability is an influential aspect related to patient compliance. The microparticles based on taste-masking polymers containing drugs enclosed inside effectively mask the unpleasant taste of medicines. Ethylcellulose is a hydrophobic polymer widely used as a taste-masking material. Rupatadine fumarate, a second-generation antihistamine drug, is characterised by an intense bitter taste; therefore, it is crucial to achieve a tolerable taste whilst developing orodispersible formulations with its content. The objective of this study was to develop orally disintegrating films with rupatadine fumarate in the form of ethylcellulose-based microparticles obtained from aqueous dispersions of ethylcellulose—Surelease<sup>®</sup> or Aquacoat<sup>®</sup> ECD. It was a technological challenge to achieve homogenous drug content per dosage unit and sufficient mechanical properties for film operating due to the necessity to suspend the microparticles in the casting solution. Although the process of obtaining films consisted of several steps (mixing, pouring, drying), the particles were homogeneously dispersed, and each film of the desired size contained the proper dose of the drug. The taste-masking effect was also maintained. This parameter was confirmed by three independent methods: in vivo by healthy volunteers, an electronic tongue and a dissolution test. The applied taste-evaluation techniques showed that the films containing Aquacoat<sup>®</sup> ECD microparticles have the highest degree of bitter taste reduction, which confirms the results obtained in our previous studies. |
| first_indexed | 2024-03-09T13:29:06Z |
| format | Article |
| id | doaj.art-478466b244cc47679f8666bcc4c7853a |
| institution | Directory Open Access Journal |
| issn | 1996-1944 |
| language | English |
| last_indexed | 2024-03-09T13:29:06Z |
| publishDate | 2022-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Materials |
| spelling | doaj.art-478466b244cc47679f8666bcc4c7853a2023-11-30T21:19:58ZengMDPI AGMaterials1996-19442022-03-01156212610.3390/ma15062126Orodispersible Films with Rupatadine Fumarate Enclosed in Ethylcellulose Microparticles as Drug Delivery Platform with Taste-Masking EffectKatarzyna Olechno0Bartosz Maciejewski1Klaudia Głowacz2Joanna Lenik3Patrycja Ciosek-Skibińska4Anna Basa5Katarzyna Winnicka6Department of Pharmaceutical Technology, Medical University of Bialystok, Mickiewicza 2c, 15-222 Bialystok, PolandDepartment of Pharmaceutical Technology, Medical University of Gdansk, Hallera 107, 80-416 Gdansk, PolandChair of Medical Biotechnology, Warsaw University of Technology, Noakowskiego 3, 00-664 Warsaw, PolandDepartment of Analytical Chemistry, Institute of Chemical Sciences, Faculty of Chemistry, Maria Curie-Skłodowska University, M. Curie-Skłodowska Sq. 3, 20-031 Lublin, PolandChair of Medical Biotechnology, Warsaw University of Technology, Noakowskiego 3, 00-664 Warsaw, PolandInstitute of Chemistry, University of Bialystok, Ciolkowskiego 1k, 15-245 Bialystok, PolandDepartment of Pharmaceutical Technology, Medical University of Bialystok, Mickiewicza 2c, 15-222 Bialystok, PolandOrally disintegrating (orodispersible) films provide a versatile tool for drug administration, especially in the pediatric and geriatric population, since they reduce the risk of choking and do not necessitate drinking water during application. By considering their direct contact with the taste buds, palatability is an influential aspect related to patient compliance. The microparticles based on taste-masking polymers containing drugs enclosed inside effectively mask the unpleasant taste of medicines. Ethylcellulose is a hydrophobic polymer widely used as a taste-masking material. Rupatadine fumarate, a second-generation antihistamine drug, is characterised by an intense bitter taste; therefore, it is crucial to achieve a tolerable taste whilst developing orodispersible formulations with its content. The objective of this study was to develop orally disintegrating films with rupatadine fumarate in the form of ethylcellulose-based microparticles obtained from aqueous dispersions of ethylcellulose—Surelease<sup>®</sup> or Aquacoat<sup>®</sup> ECD. It was a technological challenge to achieve homogenous drug content per dosage unit and sufficient mechanical properties for film operating due to the necessity to suspend the microparticles in the casting solution. Although the process of obtaining films consisted of several steps (mixing, pouring, drying), the particles were homogeneously dispersed, and each film of the desired size contained the proper dose of the drug. The taste-masking effect was also maintained. This parameter was confirmed by three independent methods: in vivo by healthy volunteers, an electronic tongue and a dissolution test. The applied taste-evaluation techniques showed that the films containing Aquacoat<sup>®</sup> ECD microparticles have the highest degree of bitter taste reduction, which confirms the results obtained in our previous studies.https://www.mdpi.com/1996-1944/15/6/2126orodispersible filmethylcellulosemicroparticlesspray dryingrupatadine fumaratetaste-masking |
| spellingShingle | Katarzyna Olechno Bartosz Maciejewski Klaudia Głowacz Joanna Lenik Patrycja Ciosek-Skibińska Anna Basa Katarzyna Winnicka Orodispersible Films with Rupatadine Fumarate Enclosed in Ethylcellulose Microparticles as Drug Delivery Platform with Taste-Masking Effect Materials orodispersible film ethylcellulose microparticles spray drying rupatadine fumarate taste-masking |
| title | Orodispersible Films with Rupatadine Fumarate Enclosed in Ethylcellulose Microparticles as Drug Delivery Platform with Taste-Masking Effect |
| title_full | Orodispersible Films with Rupatadine Fumarate Enclosed in Ethylcellulose Microparticles as Drug Delivery Platform with Taste-Masking Effect |
| title_fullStr | Orodispersible Films with Rupatadine Fumarate Enclosed in Ethylcellulose Microparticles as Drug Delivery Platform with Taste-Masking Effect |
| title_full_unstemmed | Orodispersible Films with Rupatadine Fumarate Enclosed in Ethylcellulose Microparticles as Drug Delivery Platform with Taste-Masking Effect |
| title_short | Orodispersible Films with Rupatadine Fumarate Enclosed in Ethylcellulose Microparticles as Drug Delivery Platform with Taste-Masking Effect |
| title_sort | orodispersible films with rupatadine fumarate enclosed in ethylcellulose microparticles as drug delivery platform with taste masking effect |
| topic | orodispersible film ethylcellulose microparticles spray drying rupatadine fumarate taste-masking |
| url | https://www.mdpi.com/1996-1944/15/6/2126 |
| work_keys_str_mv | AT katarzynaolechno orodispersiblefilmswithrupatadinefumarateenclosedinethylcellulosemicroparticlesasdrugdeliveryplatformwithtastemaskingeffect AT bartoszmaciejewski orodispersiblefilmswithrupatadinefumarateenclosedinethylcellulosemicroparticlesasdrugdeliveryplatformwithtastemaskingeffect AT klaudiagłowacz orodispersiblefilmswithrupatadinefumarateenclosedinethylcellulosemicroparticlesasdrugdeliveryplatformwithtastemaskingeffect AT joannalenik orodispersiblefilmswithrupatadinefumarateenclosedinethylcellulosemicroparticlesasdrugdeliveryplatformwithtastemaskingeffect AT patrycjaciosekskibinska orodispersiblefilmswithrupatadinefumarateenclosedinethylcellulosemicroparticlesasdrugdeliveryplatformwithtastemaskingeffect AT annabasa orodispersiblefilmswithrupatadinefumarateenclosedinethylcellulosemicroparticlesasdrugdeliveryplatformwithtastemaskingeffect AT katarzynawinnicka orodispersiblefilmswithrupatadinefumarateenclosedinethylcellulosemicroparticlesasdrugdeliveryplatformwithtastemaskingeffect |