Affiliation:
1. Mansoura University Faculty of Pharmacy
Abstract
Abstract
Pravastatin sodium (PVS) is a hypolipidemic drug with poor oral bioavailability as a result of the first pass effect. This study aims to formulate and evaluate transdermal patch containing PVS loaded nanoemulsions (PVS-NEs) in order to increase PVS's hypolipidemic and hepatoprotective activities. PVS-NEs were prepared using the aqueous titration method. Oleic acid was chosen as an oil phase, span 80 and tween 80 were used as surfactant and cosurfactant respectively. Droplet size (DS), polydispersity index (PDI), zeta potential (ZP), clarity, Fourier-infrared spectroscopy (FT-IR) and thermodynamic stability of NEs were all characterized. PVS-NEs (NE2) with 50% oil phase, 40% SC mix 2:1 and 10% water was selected as an optimum formula based on the results of DS (251 ± 16), PDI (0.4 ± 0.16), and ZP (-70 ±10.4) to be incorporated into transdermal patch. PVS-NE2 loaded transdermal patches (PVS-NE2-TDPs) F1 were prepared by solvent evaporation method. F1 patch with HPMC E15 and PVP K30 in a ratio of 3:1 represented satisfactory patch properties with good drug-excipients compatibility thus, it was selected as an optimum patch formula. The optimized formula (F1) was prepared using hydroxypropyl methylcellulose E15 (HPMC, 15MPa.s), Polyvinylpyrrolidone (PVP) K30, polyethylene glycol 400 (PEG) and dimethyl sulfoxide (DMSO). F1 patch was characterized for thickness, moisture content, weight variation and drug- excipients incompatibility. F1 patch was subjected to ex vivo skin permeation and finally pharmacodynamic studies. Ex vivo permeation studies of F1 revealed that, the cumulative amount of PVS permeated across rat skin was (271.66 ± 19 µg/cm2) in 72h. Pharmacodynamic studies demonstrated that, F1 patch was more effective in treating hyperlipidemia than PVS-TDP (control patch) based on both blood analysis and histopathological examination.
Publisher
Research Square Platform LLC
Cited by
1 articles.
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1. Selecting an Appropriate Animal Model for Dyslipidemia;Indian Journal of Pharmaceutical Education and Research;2024-08-10