Use of transethosomes for enhancing the transdermal delivery of olmesartan medoxomil: in vitro, ex vivo, and in vivo evaluation
| Autor: | Aly A. Abdelbary, Hanan Refai, Mohamed A. El-Nabarawi, Rofida Albash |
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| Rok vydání: | 2019 |
| Předmět: |
Chemistry
Organic Chemistry Biophysics Pharmaceutical Science Bioengineering 02 engineering and technology General Medicine Factorial experiment Permeation 010402 general chemistry 021001 nanoscience & nanotechnology 01 natural sciences Transferosomes 0104 chemical sciences Bioavailability Biomaterials In vivo Drug Discovery medicine 0210 nano-technology Olmesartan Ex vivo Transdermal medicine.drug Biomedical engineering |
| Zdroj: | International Journal of Nanomedicine. 14:1953-1968 |
| ISSN: | 1178-2013 |
| Popis: | Introduction and aim Olmesartan medoxomil (OLM) is an antihypertensive drug with low oral bioavailability due to extensive first-pass metabolism. This study aimed to prepare transetho somes (TEs) for enhancing the transdermal delivery of OLM to avoid its oral problems. Methods TE formulae were prepared utilizing 51.31 full factorial design using various surfactants (SAAs) and different phospholipid-to-SAA ratios. The formulae were characterized regarding their entrapment efficiency percentage (EE%), particle size (PS), polydispersity index (PDI), zeta potential (ZP), and the amount of drug released after 6 hours (Q6h). Design Expert® software was employed to select the optimum formula. Results The optimum formula (TE14) had an EE% of 58.50%±1.30%, PS of 222.60±2.50 nm, PDI of 0.11±0.06, ZP of -20.80±0.30 mV, and Q6h of 67.40%±0.20%. In addition, TE14 was compared to transferosomes (TFs) in terms of elasticity and was found to show higher deformability index. Further, evaluation of ex vivo permeation using both rat and shed snake skin showed higher permeability of TE14 compared to TFs and OLM suspension. Confocal laser scanning microscopy confirmed the capability of the fluorolabeled TE14 to penetrate deep within the skin, while the histopathological study confirmed its safety. TE14 successfully maintained normal blood pressure values of rats up to 24 hours. Moreover, TE14 showed superiority in dermatokinetic study when compared with drug suspension. Conclusion Taken together, the obtained results confirmed the potential of employing TEs as a successful carrier for the transdermal delivery of OLM. |
| Databáze: | OpenAIRE |
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