Development of Transdermal Oleogel Containing Olmesartan Medoxomil: Statistical Optimization and Pharmacological Evaluation

被引：3
作者：
El-Dahmy, Rania Moataz [1 ]
Elsayed, Ibrahim [2 ,3 ]
Hussein, Jihan [4 ]
Althubiti, Mohammad [5 ]
Almaimani, Riyad A. [5 ]
El-Readi, Mahmoud Zaki [5 ,6 ]
Elbaset, Marawan A. [7 ]
Ibrahim, Bassant M. M. [7 ]
机构：
[1] October 6 Univ, Fac Pharm, Dept Pharmaceut & Ind Pharm, Cent Axis, Cairo 12585, Egypt
[2] Cairo Univ, Fac Pharm, Dept Pharmaceut & Ind Pharm, Cairo 11562, Egypt
[3] Gulf Med Univ, Coll Pharm, Dept Pharmaceut Sci, Ajman 04184, U Arab Emirates
[4] Natl Res Ctr, Med & Clin Studies Res Inst, Med Biochem Dept, Giza 12622, Egypt
[5] Umm Al Qura Univ, Fac Med, Dept Biochem, Al Abdeyah 24381, Makkah, Saudi Arabia
[6] Al Azhar Univ, Fac Pharm, Biochem Dept, Assiut 71524, Egypt
[7] Natl Res Ctr, Med & Clin Studies Res Inst, Pharmacol Dept, Giza 12622, Egypt
来源：
PHARMACEUTICS | 2023年 / 15卷 / 04期
关键词：
oleogel; olmesartan medoxomil; central composite design; texture analysis; ex vivo permeation; pharmacodynamic study; pharmacokinetic study; IN-VITRO CHARACTERIZATION; EX-VIVO PERMEATION; SOFT NANO-CARRIERS; DRUG-DELIVERY; PENETRATION ENHANCERS; SKIN PERMEATION; FORMULATION; DESIGN; GEL; SURFACTANTS;
D O I：
10.3390/pharmaceutics15041083
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
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.
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页数：25
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