Development of Carvedilol-Loaded Albumin-Based Nanoparticles with Factorial Design to Optimize In Vitro and In Vivo Performance
Carvedilol, an anti-hypertensive medication commonly prescribed by healthcare providers, falls under the BCS class II category due to its low-solubility and high-permeability characteristics, resulting in limited dissolution and low absorption when taken orally. Herein, carvedilol was entrapped into...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-05-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/5/1425 |
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| author | Mohamed S. Attia Mohamed F. Radwan Tarek S. Ibrahim Tarek M. Ibrahim |
| author_facet | Mohamed S. Attia Mohamed F. Radwan Tarek S. Ibrahim Tarek M. Ibrahim |
| author_sort | Mohamed S. Attia |
| collection | DOAJ |
| description | Carvedilol, an anti-hypertensive medication commonly prescribed by healthcare providers, falls under the BCS class II category due to its low-solubility and high-permeability characteristics, resulting in limited dissolution and low absorption when taken orally. Herein, carvedilol was entrapped into bovine serum albumin (BSA)-based nanoparticles using the desolvation method to obtain a controlled release profile. Carvedilol-BSA nanoparticles were prepared and optimized using 3<sup>2</sup> factorial design. The nanoparticles were characterized for their particle size (Y<sub>1</sub>), entrapment efficiency (Y<sub>2</sub>), and time to release 50% of carvedilol (Y<sub>3</sub>). The optimized formulation was assessed for its in vitro and in vivo performance by solid-state, microscopical, and pharmacokinetic evaluations. The factorial design showed that an increment of BSA concentration demonstrated a significant positive effect on Y<sub>1</sub> and Y<sub>2</sub> responses with a negative effect on Y<sub>3</sub> response. Meanwhile, the carvedilol percentage in BSA nanoparticles represented its obvious positive impact on both Y<sub>1</sub> and Y<sub>3</sub> responses, along with a negative impact on Y<sub>2</sub> response. The optimized nanoformulation entailed BSA at a concentration of 0.5%, whereas the carvedilol percentage was 6%. The DSC thermograms indicated the amorphization of carvedilol inside the nanoparticles, which confirmed its entrapment into the BSA structure. The plasma concentrations of carvedilol released were observable from optimized nanoparticles up to 72 h subsequent to their injection into rats, revealing their longer in vivo circulation time compared to pure carvedilol suspension. This study offers new insight into the significance of BSA-based nanoparticles in sustaining the release of carvedilol and presents a potential value-added in the remediation of hypertension. |
| first_indexed | 2024-03-11T03:24:13Z |
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| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T03:24:13Z |
| publishDate | 2023-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-3c62fbd0d8be422ba5da43c06cb183f42023-11-18T02:51:24ZengMDPI AGPharmaceutics1999-49232023-05-01155142510.3390/pharmaceutics15051425Development of Carvedilol-Loaded Albumin-Based Nanoparticles with Factorial Design to Optimize In Vitro and In Vivo PerformanceMohamed S. Attia0Mohamed F. Radwan1Tarek S. Ibrahim2Tarek M. Ibrahim3Department of Pharmaceutics, Faculty of Pharmacy, Zagazig University, Zagazig 44519, EgyptDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, Zagazig University, Zagazig 44519, EgyptCarvedilol, an anti-hypertensive medication commonly prescribed by healthcare providers, falls under the BCS class II category due to its low-solubility and high-permeability characteristics, resulting in limited dissolution and low absorption when taken orally. Herein, carvedilol was entrapped into bovine serum albumin (BSA)-based nanoparticles using the desolvation method to obtain a controlled release profile. Carvedilol-BSA nanoparticles were prepared and optimized using 3<sup>2</sup> factorial design. The nanoparticles were characterized for their particle size (Y<sub>1</sub>), entrapment efficiency (Y<sub>2</sub>), and time to release 50% of carvedilol (Y<sub>3</sub>). The optimized formulation was assessed for its in vitro and in vivo performance by solid-state, microscopical, and pharmacokinetic evaluations. The factorial design showed that an increment of BSA concentration demonstrated a significant positive effect on Y<sub>1</sub> and Y<sub>2</sub> responses with a negative effect on Y<sub>3</sub> response. Meanwhile, the carvedilol percentage in BSA nanoparticles represented its obvious positive impact on both Y<sub>1</sub> and Y<sub>3</sub> responses, along with a negative impact on Y<sub>2</sub> response. The optimized nanoformulation entailed BSA at a concentration of 0.5%, whereas the carvedilol percentage was 6%. The DSC thermograms indicated the amorphization of carvedilol inside the nanoparticles, which confirmed its entrapment into the BSA structure. The plasma concentrations of carvedilol released were observable from optimized nanoparticles up to 72 h subsequent to their injection into rats, revealing their longer in vivo circulation time compared to pure carvedilol suspension. This study offers new insight into the significance of BSA-based nanoparticles in sustaining the release of carvedilol and presents a potential value-added in the remediation of hypertension.https://www.mdpi.com/1999-4923/15/5/1425carvedilolhealthcarebovine serum albuminnanoparticlesdesolvationfactorial design |
| spellingShingle | Mohamed S. Attia Mohamed F. Radwan Tarek S. Ibrahim Tarek M. Ibrahim Development of Carvedilol-Loaded Albumin-Based Nanoparticles with Factorial Design to Optimize In Vitro and In Vivo Performance Pharmaceutics carvedilol healthcare bovine serum albumin nanoparticles desolvation factorial design |
| title | Development of Carvedilol-Loaded Albumin-Based Nanoparticles with Factorial Design to Optimize In Vitro and In Vivo Performance |
| title_full | Development of Carvedilol-Loaded Albumin-Based Nanoparticles with Factorial Design to Optimize In Vitro and In Vivo Performance |
| title_fullStr | Development of Carvedilol-Loaded Albumin-Based Nanoparticles with Factorial Design to Optimize In Vitro and In Vivo Performance |
| title_full_unstemmed | Development of Carvedilol-Loaded Albumin-Based Nanoparticles with Factorial Design to Optimize In Vitro and In Vivo Performance |
| title_short | Development of Carvedilol-Loaded Albumin-Based Nanoparticles with Factorial Design to Optimize In Vitro and In Vivo Performance |
| title_sort | development of carvedilol loaded albumin based nanoparticles with factorial design to optimize in vitro and in vivo performance |
| topic | carvedilol healthcare bovine serum albumin nanoparticles desolvation factorial design |
| url | https://www.mdpi.com/1999-4923/15/5/1425 |
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