Pharmacodynamic study of eprosartan mesylate-loaded transfersomes Carbopol® gel under Dermaroller® on rats with methyl prednisolone acetate-induced hypertension

Ahad, Abdul; Al-Saleh, Ahmad M.; Al-Mohizea, Abdullah M.; Al-Jenoobi, Fahad I.; Raish, Mohammad; Yassin, Alaa Eldeen B.; Alam, Mohammad Mumtaz

doi:10.1016/j.biopha.2017.01.164

Cited by 73 publications

(44 citation statements)

References 51 publications

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“…The carbopol dispersion was neutralized with the incorporation of triethanolamine to get a clear viscous gel. Then the optimized transethosomes formulation was slowly added into preformed gel with stirring [41,42]. The dermatokinetic study was performed to analyze the concentration of drug in different layers of Wistar rat skin.…”

Section: Dermatokinetic Studymentioning

confidence: 99%

Development of transethosomes formulation for dermal fisetin delivery: Box–Behnken design, optimization, in vitro skin penetration, vesicles–skin interaction and dermatokinetic studies

Moolakkadath

Aqil

Ahad

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

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106

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The present study was conducted for the optimization of transethosomes formulation for dermal fisetin delivery. The optimization of the formulation was carried out using "Box-Behnken design". The independent variables were Lipoid S 100, ethanol and sodium cholate. The prepared formulations were characterized for vesicle size, entrapment efficiency and in vitro skin penetration study. The vesicles-skin interaction, confocal laser scanning microscopy and dermatokinetic studies were performed with optimized formulation. Results of the present study demonstrated that the optimized formulation presented vesicle size of 74.21 ± 2.65 nm, zeta potential of -11.0 mV, entrapment efficiency of 68.31 ± 1.48% and flux of 4.13 ± 0.17 µg/cm/h. The TEM image of optimized formulation exhibited sealed and spherical shape vesicles. Results of thermoanalytical techniques demonstrated that the prepared transethosomes vesicles formulation had fluidized the rigid membrane of rat's skin for smoother penetration of fisetin transethosomes. The confocal study results presented well distribution and penetration of Rhodamine B loaded transethosomes vesicles formulation up to deeper layers of the rat's skin as compared to the Rhodamine B-hydro alcoholic solution. Present study data revealed that the developed transethosomes vesicles formulation was found to be a potentially useful drug carrier for fisetin dermal delivery.

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Section: Dermatokinetic Studymentioning

confidence: 99%

Development of transethosomes formulation for dermal fisetin delivery: Box–Behnken design, optimization, in vitro skin penetration, vesicles–skin interaction and dermatokinetic studies

Moolakkadath

Aqil

Ahad

et al. 2018

Artificial Cells, Nanomedicine, and Biotechnology

Self Cite

106

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“…The results indicated prolonged and better management of hypertension after the application of transfersomal gel to hypertensive rats pretreated with the Dermaroller when compared with the oral control formulation. This enhanced effect was further confirmed by the decreased levels of angiotensin II type-1 (AT1) mRNA and the AT1 receptor (AT1R) in the aorta smooth vascular muscles of the treated hypertensive rats, as measured by real-time polymerase chain reaction (RT-PCR) and Western blot analysis, respectively [133].…”

Section: Delivery Properties Of Transfersomes Incorporating Active Momentioning

confidence: 88%

“…No erythema or edema, as scored visually, were found on the guinea pigs' bare skin after applying the drug transfersomal formulation. In another in vivo investigation on rats, topical application for 24 h of eprosartan mesylate transfersomes, based on PL90G and Tween 80, was found to be safe and non-irritant [133]. Raj et al [129] conducted visual and histopathological skin irritation tests upon the application of cytarabine nanodeformable liposomes containing SPC and sodium deoxycholate to rats for 10 days.…”

Section: Safety Assessement For Systems Containing Altered Phospholipmentioning

confidence: 99%

“…Transfersomal-based carriers were also evaluated for the transdermal delivery of the anti-hypertensive drugs: felodipine [ 125 ], timolol maleate [ 131 , 132 ] and eprosartan mesylate [ 133 ]. Morsi et al [ 132 ] measured plasma levels of timolol following non-occlusive single administration of optimized timolol maleate transfersomes to rats in comparison with oral suspension of the drug.…”

Section: Phospholipid Nanovesicles For Dermal and Transdermal Delimentioning

confidence: 99%

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Phospholipid Vesicles for Dermal/Transdermal and Nasal Administration of Active Molecules: The Effect of Surfactants and Alcohols on the Fluidity of Their Lipid Bilayers and Penetration Enhancement Properties

Natsheh

Touítou

2020

Molecules

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This is a comprehensive review on the use of phospholipid nanovesicles for dermal/transdermal and nasal drug administration. Phospholipid-based vesicular carriers have been widely investigated for enhanced drug delivery via dermal/transdermal routes. Classic phospholipid vesicles, liposomes, do not penetrate the deep layers of the skin, but remain confined to the upper stratum corneum. The literature describes several approaches with the aim of altering the properties of these vesicles to improve their penetration properties. Transfersomes and ethosomes are the most investigated penetration-enhancing phospholipid nanovesicles, obtained by the incorporation of surfactant edge activators and high concentrations of ethanol, respectively. These two types of vesicles differ in terms of their structure, characteristics, mechanism of action and mode of application on the skin. Edge activators contribute to the deformability and elasticity of transfersomes, enabling them to penetrate through pores much smaller than their own size. The ethanol high concentration in ethosomes generates a soft vesicle by fluidizing the phospholipid bilayers, allowing the vesicle to penetrate deeper into the skin. Glycerosomes and transethosomes, phospholipid vesicles containing glycerol or a mixture of ethanol and edge activators, respectively, are also covered. This review discusses the effects of edge activators, ethanol and glycerol on the phospholipid vesicle, emphasizing the differences between a soft and an elastic nanovesicle, and presents their different preparation methods. To date, these differences have not been comparatively discussed. The review presents a large number of active molecules incorporated in these carriers and investigated in vitro, in vivo or in clinical human tests.

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“…They were marked on tail for easy identification. To lessen the deviations in SBP, animals were trained to accommodate in rat holder for 5 days before the commencement of the experiment, so that the rats acquired to remain in the holder without aggressiveness and were become acquainted with the experimental conditions ( Ahad et al, 2017 , Ahad et al, 2016b , Ahad et al, 2018 ).…”

Section: Methodsmentioning

confidence: 99%

Potential pharmacodynamic and pharmacokinetic interactions of Nigella Sativa and Trigonella Foenum-graecum with losartan in L-NAME induced hypertensive rats

Ahad

Raish

Jardan

et al. 2020

Saudi Journal of Biological Sciences

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The objective of this investigation was to study whether Nigella Sativa and Trigonella Foenum-graecum , could modulate the losartan pharmacodynamic (PD) and pharmacokinetic (PK) in experimental L-NAME induced hypertensive rats. For in vivo study, the systolic blood pressure (SBP) of rats was measured by the “tail-cuff system” after the treatment of rats with herb alone and herb + losartan in hypertensive rats. The SBP of rats treated with L-NAME + losartan also recorded. For the PK study, blood samples were obtained for up to 12 h to determine the concentrations of the drug, and various PK parameters were calculated. The data displayed that the SBP was significantly (p < 0.05) decreased in the rats when administered with L-NAME + N. Sativa or L-NAME + T. Foenum-graecum in contrast to the rats administered with L-NAME alone. A more prominent decline (p < 0.05) in SBP was detected in rats administered with L-NAME + N. Sativa + losartan and L-NAME + T. Foenum-graecum + losartan. In a PK study, higher losartan C max and AUC 0-t were noted in rats treated with N. Sativa + losartan and T. Foenum-graecum + losartan, although the difference was not significant in contrast to the control group. This study proposed that the interaction between N. Sativa & losartan and T. Foenum-graecum & losartan could take place on concurrent administration; consequently, the dose of losartan may need to be accustomed when they are utilized simultaneously.

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Pharmacodynamic study of eprosartan mesylate-loaded transfersomes Carbopol® gel under Dermaroller® on rats with methyl prednisolone acetate-induced hypertension

Cited by 73 publications

References 51 publications

Development of transethosomes formulation for dermal fisetin delivery: Box–Behnken design, optimization, in vitro skin penetration, vesicles–skin interaction and dermatokinetic studies

Development of transethosomes formulation for dermal fisetin delivery: Box–Behnken design, optimization, in vitro skin penetration, vesicles–skin interaction and dermatokinetic studies

Phospholipid Vesicles for Dermal/Transdermal and Nasal Administration of Active Molecules: The Effect of Surfactants and Alcohols on the Fluidity of Their Lipid Bilayers and Penetration Enhancement Properties

Potential pharmacodynamic and pharmacokinetic interactions of Nigella Sativa and Trigonella Foenum-graecum with losartan in L-NAME induced hypertensive rats

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