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 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.

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Publication Details

Journal
Pharmaceutics
Published
2024-12-04
DOI
https://doi.org/10.3390/pharmaceutics16121552
Citations
5
Primary Topic
Phase Equilibria and Thermodynamics
Type
article
Field-Weighted Citation Impact
0.92
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article

Eutectogel-Based Drug Delivery: An Innovative Approach for Atenolol Administration

Gabriella Calviello, Roberta Cassano, Noemi Baldino, Debora Procopio et al.
5 citations
Pharmaceutics
Phase Equilibria and Thermodynamics
0.92
article

Eutectogel-Based Drug Delivery: An Innovative Approach for Atenolol Administration

Gabriella Calviello, Roberta Cassano, Noemi Baldino, Debora Procopio, Olga Mileti, Federica Curcio, Simona Serini, Roberta Del Sole, Carlo Siciliano, Maria Luisa Di Gioia, Sonia Trombino
article en
5 citations

Abstract

<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.

PharmaceuticsVol. 16(12)
Università Cattolica del Sacro Cuore (IT), Agostino Gemelli University Polyclinic (IT), Istituti di Ricovero e Cura a Carattere Scientifico (IT), University of Calabria (IT)
Openalex Percentile: Top 27%
Phase Equilibria and Thermodynamics
0.92
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