Design of Olmesartan Medoxomil-Loaded Nanosponges for Hypertension and Lung Cancer Treatments
Olmesartan medoxomil (OLM) is one of the prominent antihypertensive drug that suffers from low aqueous solubility and dissolution rate leading to its low bioavailability. To improve the oral bioavailability of OLM, a delivery system based on ethylcellulose (EC, a biobased polymer) nanosponges (NSs)...
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MDPI AG
2021-07-01
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| Series: | Polymers |
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| Online Access: | https://www.mdpi.com/2073-4360/13/14/2272 |
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| author | Bjad K. Almutairy Abdullah Alshetaili Amer S. Alali Mohammed Muqtader Ahmed Md. Khalid Anwer M. Ali Aboudzadeh |
| author_facet | Bjad K. Almutairy Abdullah Alshetaili Amer S. Alali Mohammed Muqtader Ahmed Md. Khalid Anwer M. Ali Aboudzadeh |
| author_sort | Bjad K. Almutairy |
| collection | DOAJ |
| description | Olmesartan medoxomil (OLM) is one of the prominent antihypertensive drug that suffers from low aqueous solubility and dissolution rate leading to its low bioavailability. To improve the oral bioavailability of OLM, a delivery system based on ethylcellulose (EC, a biobased polymer) nanosponges (NSs) was developed and evaluated for cytotoxicity against the A549 lung cell lines and antihypertensive potential in a rat model. Four OLM-loaded NSs (ONS1-ONS4) were prepared and fully evaluated in terms of physicochemical properties. Among these formulations, ONS4 was regarded as the optimized formulation with particle size (487 nm), PDI (0.386), zeta potential (ζP = −18.1 mV), entrapment efficiency (EE = 91.2%) and drug loading (DL = 0.88%). In addition, a nanosized porous morphology was detected for this optimized system with NS surface area of about 63.512 m<sup>2</sup>/g, pore volume and pore radius Dv(r) of 0.149 cc/g and 15.274 Å, respectively, measured by nitrogen adsorption/desorption analysis. The observed morphology plus sustained release rate of OLM caused that the optimized formulation showed higher cytotoxicity against A549 lung cell lines in comparison to the pure OLM. Finally, this system (ONS4) reduced the systolic blood pressure (SBP) significantly (<i>p</i> < 0.01) as compared to control and pure OLM drug in spontaneously hypertensive rats. Overall, this study provides a scientific basis for future studies on the encapsulation efficiency of NSs as promising drug carriers for overcoming pharmacokinetic limitations. |
| first_indexed | 2024-03-10T09:28:02Z |
| format | Article |
| id | doaj.art-e3fed21aa319445f8760621ff1bebc0b |
| institution | Directory Open Access Journal |
| issn | 2073-4360 |
| language | English |
| last_indexed | 2024-03-10T09:28:02Z |
| publishDate | 2021-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Polymers |
| spelling | doaj.art-e3fed21aa319445f8760621ff1bebc0b2023-11-22T04:45:46ZengMDPI AGPolymers2073-43602021-07-011314227210.3390/polym13142272Design of Olmesartan Medoxomil-Loaded Nanosponges for Hypertension and Lung Cancer TreatmentsBjad K. Almutairy0Abdullah Alshetaili1Amer S. Alali2Mohammed Muqtader Ahmed3Md. Khalid Anwer4M. Ali Aboudzadeh5Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Alkharj 11942, Saudi ArabiaInstitut des Sciences Analytiques et de Physico-Chimie pour l’Environnement et les Matériaux, University Pau & Pays Adour, 64000 Pau, FranceOlmesartan medoxomil (OLM) is one of the prominent antihypertensive drug that suffers from low aqueous solubility and dissolution rate leading to its low bioavailability. To improve the oral bioavailability of OLM, a delivery system based on ethylcellulose (EC, a biobased polymer) nanosponges (NSs) was developed and evaluated for cytotoxicity against the A549 lung cell lines and antihypertensive potential in a rat model. Four OLM-loaded NSs (ONS1-ONS4) were prepared and fully evaluated in terms of physicochemical properties. Among these formulations, ONS4 was regarded as the optimized formulation with particle size (487 nm), PDI (0.386), zeta potential (ζP = −18.1 mV), entrapment efficiency (EE = 91.2%) and drug loading (DL = 0.88%). In addition, a nanosized porous morphology was detected for this optimized system with NS surface area of about 63.512 m<sup>2</sup>/g, pore volume and pore radius Dv(r) of 0.149 cc/g and 15.274 Å, respectively, measured by nitrogen adsorption/desorption analysis. The observed morphology plus sustained release rate of OLM caused that the optimized formulation showed higher cytotoxicity against A549 lung cell lines in comparison to the pure OLM. Finally, this system (ONS4) reduced the systolic blood pressure (SBP) significantly (<i>p</i> < 0.01) as compared to control and pure OLM drug in spontaneously hypertensive rats. Overall, this study provides a scientific basis for future studies on the encapsulation efficiency of NSs as promising drug carriers for overcoming pharmacokinetic limitations.https://www.mdpi.com/2073-4360/13/14/2272ethylcelluloseencapsulationlung cancernanospongeoral bioavailabilitysystolic blood pressure |
| spellingShingle | Bjad K. Almutairy Abdullah Alshetaili Amer S. Alali Mohammed Muqtader Ahmed Md. Khalid Anwer M. Ali Aboudzadeh Design of Olmesartan Medoxomil-Loaded Nanosponges for Hypertension and Lung Cancer Treatments Polymers ethylcellulose encapsulation lung cancer nanosponge oral bioavailability systolic blood pressure |
| title | Design of Olmesartan Medoxomil-Loaded Nanosponges for Hypertension and Lung Cancer Treatments |
| title_full | Design of Olmesartan Medoxomil-Loaded Nanosponges for Hypertension and Lung Cancer Treatments |
| title_fullStr | Design of Olmesartan Medoxomil-Loaded Nanosponges for Hypertension and Lung Cancer Treatments |
| title_full_unstemmed | Design of Olmesartan Medoxomil-Loaded Nanosponges for Hypertension and Lung Cancer Treatments |
| title_short | Design of Olmesartan Medoxomil-Loaded Nanosponges for Hypertension and Lung Cancer Treatments |
| title_sort | design of olmesartan medoxomil loaded nanosponges for hypertension and lung cancer treatments |
| topic | ethylcellulose encapsulation lung cancer nanosponge oral bioavailability systolic blood pressure |
| url | https://www.mdpi.com/2073-4360/13/14/2272 |
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