Eutectogel-Based Drug Delivery: An Innovative Approach for Atenolol Administration
<b>Background:</b> Hypertension affects 32% of adults worldwide, leading to a significant global consumption of cardiovascular medications. Atenolol, a β-adrenergic receptor blocker, is widely prescribed for cardiovascular diseases such as hypertension, angina pectoris, and myocardial in...
Saved in:
| Main Authors: | , , , , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2024-12-01
|
| Series: | Pharmaceutics |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1999-4923/16/12/1552 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| _version_ | 1850036026067648512 |
|---|---|
| author | Roberta Cassano Roberta Sole Carlo Siciliano Noemi Baldino Olga Mileti Debora Procopio Federica Curcio Gabriella Calviello Simona Serini Sonia Trombino Maria Luisa Di Gioia |
| author_facet | Roberta Cassano Roberta Sole Carlo Siciliano Noemi Baldino Olga Mileti Debora Procopio Federica Curcio Gabriella Calviello Simona Serini Sonia Trombino Maria Luisa Di Gioia |
| author_sort | Roberta Cassano |
| collection | DOAJ |
| description | <b>Background:</b> Hypertension affects 32% of adults worldwide, leading to a significant global consumption of cardiovascular medications. Atenolol, a β-adrenergic receptor blocker, is widely prescribed for cardiovascular diseases such as hypertension, angina pectoris, and myocardial infarction. According to the Biopharmaceutics Classification System (BCS), atenolol belongs to Class III, characterized by high solubility but low permeability. Currently, atenolol is commercially available in oral formulations. Increasing attention is being directed towards developing cost-effective transdermal delivery systems, due to their ease of use and better patient compliance. Eutectogels represent next-generation systems that are attracting great interest in the scientific community. Typically obtained from deep eutectic solvents (DESs) combined with gelling agents, these systems exhibit unique properties due to the intrinsic characteristics of DESs. <b>Methods:</b> In this study, a DES based on choline chloride as a hydrogen bond acceptor (HBA) and propylene glycol as a hydrogen bond donor (HBD) was explored to enhance the topical delivery of atenolol. The solubility of atenolol in the DES was evaluated using spectroscopic and thermodynamic measurements which confirmed the formation of hydrogen bonds between the drug and DES components. Additionally, the safety of the DES was assessed in a cell viability assay. Subsequently, we formulated eutectogels with different concentrations using animal gelatin and Tego Carbomer 140, and characterized these formulations through rheological measurements, swelling percentage, and permeation studies with Franz cells. <b>Results:</b> These novel eutectogels exhibit superior performance over conventional hydrogels, with a release rate of approximately 86% and 51% for Carbomer- and gelatin-based eutectogels, respectively. In contrast, comparable hydrogels released only about 27% and 35%. <b>Conclusions:</b> These findings underscore the promising potential of eutectogels for the transdermal delivery of atenolol. |
| format | Article |
| id | doaj-art-d33f9b985e9c40cd92f3a9916732aa8e |
| institution | DOAJ |
| issn | 1999-4923 |
| language | English |
| publishDate | 2024-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj-art-d33f9b985e9c40cd92f3a9916732aa8e2025-08-20T02:57:20ZengMDPI AGPharmaceutics1999-49232024-12-011612155210.3390/pharmaceutics16121552Eutectogel-Based Drug Delivery: An Innovative Approach for Atenolol AdministrationRoberta Cassano0Roberta Sole1Carlo Siciliano2Noemi Baldino3Olga Mileti4Debora Procopio5Federica Curcio6Gabriella Calviello7Simona Serini8Sonia Trombino9Maria Luisa Di Gioia10Dipartimento di Farmacia, Salute e Scienze della Nutrizione, Università della Calabria, Arcavacata di Rende, 87036 Cosenza, ItalyDipartimento di Farmacia, Salute e Scienze della Nutrizione, Università della Calabria, Arcavacata di Rende, 87036 Cosenza, ItalyDipartimento di Farmacia, Salute e Scienze della Nutrizione, Università della Calabria, Arcavacata di Rende, 87036 Cosenza, ItalyDipartimento di Ingegneria Informatica, Modellistica, Elettronica e Sistemistica, Università della Calabria, Arcavacata di Rende, 87036 Cosenza, ItalyDipartimento di Ingegneria Informatica, Modellistica, Elettronica e Sistemistica, Università della Calabria, Arcavacata di Rende, 87036 Cosenza, ItalyDipartimento di Farmacia, Salute e Scienze della Nutrizione, Università della Calabria, Arcavacata di Rende, 87036 Cosenza, ItalyDipartimento di Farmacia, Salute e Scienze della Nutrizione, Università della Calabria, Arcavacata di Rende, 87036 Cosenza, ItalyDipartimento di Medicina e Chirurgia Traslazionale, Sezione di Patologia Generale, Facoltà di Medicina e Chirurgia, Università Cattolica del Sacro Cuore, Largo F. Vito, 00168 Roma, ItalyDipartimento di Medicina e Chirurgia Traslazionale, Sezione di Patologia Generale, Facoltà di Medicina e Chirurgia, Università Cattolica del Sacro Cuore, Largo F. Vito, 00168 Roma, ItalyDipartimento di Farmacia, Salute e Scienze della Nutrizione, Università della Calabria, Arcavacata di Rende, 87036 Cosenza, ItalyDipartimento di Farmacia, Salute e Scienze della Nutrizione, Università della Calabria, Arcavacata di Rende, 87036 Cosenza, Italy<b>Background:</b> Hypertension affects 32% of adults worldwide, leading to a significant global consumption of cardiovascular medications. Atenolol, a β-adrenergic receptor blocker, is widely prescribed for cardiovascular diseases such as hypertension, angina pectoris, and myocardial infarction. According to the Biopharmaceutics Classification System (BCS), atenolol belongs to Class III, characterized by high solubility but low permeability. Currently, atenolol is commercially available in oral formulations. Increasing attention is being directed towards developing cost-effective transdermal delivery systems, due to their ease of use and better patient compliance. Eutectogels represent next-generation systems that are attracting great interest in the scientific community. Typically obtained from deep eutectic solvents (DESs) combined with gelling agents, these systems exhibit unique properties due to the intrinsic characteristics of DESs. <b>Methods:</b> In this study, a DES based on choline chloride as a hydrogen bond acceptor (HBA) and propylene glycol as a hydrogen bond donor (HBD) was explored to enhance the topical delivery of atenolol. The solubility of atenolol in the DES was evaluated using spectroscopic and thermodynamic measurements which confirmed the formation of hydrogen bonds between the drug and DES components. Additionally, the safety of the DES was assessed in a cell viability assay. Subsequently, we formulated eutectogels with different concentrations using animal gelatin and Tego Carbomer 140, and characterized these formulations through rheological measurements, swelling percentage, and permeation studies with Franz cells. <b>Results:</b> These novel eutectogels exhibit superior performance over conventional hydrogels, with a release rate of approximately 86% and 51% for Carbomer- and gelatin-based eutectogels, respectively. In contrast, comparable hydrogels released only about 27% and 35%. <b>Conclusions:</b> These findings underscore the promising potential of eutectogels for the transdermal delivery of atenolol.https://www.mdpi.com/1999-4923/16/12/1552deep eutectic solventsgreen solventsatenololeutectogeldrug deliveryβ-blockers |
| spellingShingle | Roberta Cassano Roberta Sole Carlo Siciliano Noemi Baldino Olga Mileti Debora Procopio Federica Curcio Gabriella Calviello Simona Serini Sonia Trombino Maria Luisa Di Gioia Eutectogel-Based Drug Delivery: An Innovative Approach for Atenolol Administration Pharmaceutics deep eutectic solvents green solvents atenolol eutectogel drug delivery β-blockers |
| title | Eutectogel-Based Drug Delivery: An Innovative Approach for Atenolol Administration |
| title_full | Eutectogel-Based Drug Delivery: An Innovative Approach for Atenolol Administration |
| title_fullStr | Eutectogel-Based Drug Delivery: An Innovative Approach for Atenolol Administration |
| title_full_unstemmed | Eutectogel-Based Drug Delivery: An Innovative Approach for Atenolol Administration |
| title_short | Eutectogel-Based Drug Delivery: An Innovative Approach for Atenolol Administration |
| title_sort | eutectogel based drug delivery an innovative approach for atenolol administration |
| topic | deep eutectic solvents green solvents atenolol eutectogel drug delivery β-blockers |
| url | https://www.mdpi.com/1999-4923/16/12/1552 |
| work_keys_str_mv | AT robertacassano eutectogelbaseddrugdeliveryaninnovativeapproachforatenololadministration AT robertasole eutectogelbaseddrugdeliveryaninnovativeapproachforatenololadministration AT carlosiciliano eutectogelbaseddrugdeliveryaninnovativeapproachforatenololadministration AT noemibaldino eutectogelbaseddrugdeliveryaninnovativeapproachforatenololadministration AT olgamileti eutectogelbaseddrugdeliveryaninnovativeapproachforatenololadministration AT deboraprocopio eutectogelbaseddrugdeliveryaninnovativeapproachforatenololadministration AT federicacurcio eutectogelbaseddrugdeliveryaninnovativeapproachforatenololadministration AT gabriellacalviello eutectogelbaseddrugdeliveryaninnovativeapproachforatenololadministration AT simonaserini eutectogelbaseddrugdeliveryaninnovativeapproachforatenololadministration AT soniatrombino eutectogelbaseddrugdeliveryaninnovativeapproachforatenololadministration AT marialuisadigioia eutectogelbaseddrugdeliveryaninnovativeapproachforatenololadministration |