Development of Transdermal Oleogel Containing Olmesartan Medoxomil: Statistical Optimization and Pharmacological Evaluation
Olmesartan medoxomil (OLM) is a first-line antihypertensive drug with low oral bioavailability (28.6%). This study aimed to develop oleogel formulations to decrease OLM side effects and boost its therapeutic efficacy and bioavailability. OLM oleogel formulations were composed of Tween 20, Aerosil 20...
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MDPI AG
2023-03-01
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| Online Access: | https://www.mdpi.com/1999-4923/15/4/1083 |
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| author | Rania Moataz El-Dahmy Ibrahim Elsayed Jihan Hussein Mohammad Althubiti Riyad A. Almaimani Mahmoud Zaki El-Readi Marawan A. Elbaset Bassant M. M. Ibrahim |
| author_facet | Rania Moataz El-Dahmy Ibrahim Elsayed Jihan Hussein Mohammad Althubiti Riyad A. Almaimani Mahmoud Zaki El-Readi Marawan A. Elbaset Bassant M. M. Ibrahim |
| author_sort | Rania Moataz El-Dahmy |
| collection | DOAJ |
| description | Olmesartan medoxomil (OLM) is a first-line antihypertensive drug with low oral bioavailability (28.6%). This study aimed to develop oleogel formulations to decrease OLM side effects and boost its therapeutic efficacy and bioavailability. OLM oleogel formulations were composed of Tween 20, Aerosil 200, and lavender oil. A central composite response surface design chose the optimized formulation, containing Oil/Surfactant (SAA) ratio of 1:1 and Aerosil % of 10.55%, after showing the lowest firmness and compressibility, and the highest viscosity, adhesiveness, and bioadhesive properties (Fmax and Wad). The optimized oleogel increased OLM release by 4.21 and 4.97 folds than the drug suspension and gel, respectively. The optimized oleogel formulation increased OLM permeation by 5.62 and 7.23 folds than the drug suspension and gel, respectively. The pharmacodynamic study revealed the superiority of the optimized formulation in maintaining normal blood pressure and heart rate for 24 h. The biochemical analysis revealed that the optimized oleogel achieved the best serum electrolyte balance profile, preventing OLM-induced tachycardia. The pharmacokinetic study showed that the optimized oleogel increased OLM’s bioavailability by more than 4.5- and 2.5-folds compared to the standard gel and the oral market tablet, respectively. These results confirmed the success of oleogel formulations in the transdermal delivery of OLM. |
| first_indexed | 2024-03-11T04:38:35Z |
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| id | doaj.art-bf002335d0c140d5a0f43c5403eb7fb3 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-11T04:38:35Z |
| publishDate | 2023-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-bf002335d0c140d5a0f43c5403eb7fb32023-11-17T20:52:28ZengMDPI AGPharmaceutics1999-49232023-03-01154108310.3390/pharmaceutics15041083Development of Transdermal Oleogel Containing Olmesartan Medoxomil: Statistical Optimization and Pharmacological EvaluationRania Moataz El-Dahmy0Ibrahim Elsayed1Jihan Hussein2Mohammad Althubiti3Riyad A. Almaimani4Mahmoud Zaki El-Readi5Marawan A. Elbaset6Bassant M. M. Ibrahim7Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, October 6 University, Central Axis, Cairo 12585, EgyptDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo 11562, EgyptMedical Biochemistry Department, Medicine and Clinical Studies Research Institute, National Research Centre, Giza 12622, EgyptDepartment of Biochemistry, Faculty of Medicine, Umm Al-Qura University, Al Abdeyah, Makkah 24381, Saudi ArabiaDepartment of Biochemistry, Faculty of Medicine, Umm Al-Qura University, Al Abdeyah, Makkah 24381, Saudi ArabiaDepartment of Biochemistry, Faculty of Medicine, Umm Al-Qura University, Al Abdeyah, Makkah 24381, Saudi ArabiaPharmacology Department, Medicine and Clinical Studies Research Institute, National Research Centre, Giza 12622, EgyptPharmacology Department, Medicine and Clinical Studies Research Institute, National Research Centre, Giza 12622, EgyptOlmesartan medoxomil (OLM) is a first-line antihypertensive drug with low oral bioavailability (28.6%). This study aimed to develop oleogel formulations to decrease OLM side effects and boost its therapeutic efficacy and bioavailability. OLM oleogel formulations were composed of Tween 20, Aerosil 200, and lavender oil. A central composite response surface design chose the optimized formulation, containing Oil/Surfactant (SAA) ratio of 1:1 and Aerosil % of 10.55%, after showing the lowest firmness and compressibility, and the highest viscosity, adhesiveness, and bioadhesive properties (Fmax and Wad). The optimized oleogel increased OLM release by 4.21 and 4.97 folds than the drug suspension and gel, respectively. The optimized oleogel formulation increased OLM permeation by 5.62 and 7.23 folds than the drug suspension and gel, respectively. The pharmacodynamic study revealed the superiority of the optimized formulation in maintaining normal blood pressure and heart rate for 24 h. The biochemical analysis revealed that the optimized oleogel achieved the best serum electrolyte balance profile, preventing OLM-induced tachycardia. The pharmacokinetic study showed that the optimized oleogel increased OLM’s bioavailability by more than 4.5- and 2.5-folds compared to the standard gel and the oral market tablet, respectively. These results confirmed the success of oleogel formulations in the transdermal delivery of OLM.https://www.mdpi.com/1999-4923/15/4/1083oleogelolmesartan medoxomilcentral composite designtexture analysisex vivo permeationpharmacodynamic study |
| spellingShingle | Rania Moataz El-Dahmy Ibrahim Elsayed Jihan Hussein Mohammad Althubiti Riyad A. Almaimani Mahmoud Zaki El-Readi Marawan A. Elbaset Bassant M. M. Ibrahim Development of Transdermal Oleogel Containing Olmesartan Medoxomil: Statistical Optimization and Pharmacological Evaluation Pharmaceutics oleogel olmesartan medoxomil central composite design texture analysis ex vivo permeation pharmacodynamic study |
| title | Development of Transdermal Oleogel Containing Olmesartan Medoxomil: Statistical Optimization and Pharmacological Evaluation |
| title_full | Development of Transdermal Oleogel Containing Olmesartan Medoxomil: Statistical Optimization and Pharmacological Evaluation |
| title_fullStr | Development of Transdermal Oleogel Containing Olmesartan Medoxomil: Statistical Optimization and Pharmacological Evaluation |
| title_full_unstemmed | Development of Transdermal Oleogel Containing Olmesartan Medoxomil: Statistical Optimization and Pharmacological Evaluation |
| title_short | Development of Transdermal Oleogel Containing Olmesartan Medoxomil: Statistical Optimization and Pharmacological Evaluation |
| title_sort | development of transdermal oleogel containing olmesartan medoxomil statistical optimization and pharmacological evaluation |
| topic | oleogel olmesartan medoxomil central composite design texture analysis ex vivo permeation pharmacodynamic study |
| url | https://www.mdpi.com/1999-4923/15/4/1083 |
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