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Formulation, characterization, in vitro and in vivo evaluations of self-nanoemulsifying drug delivery system of luteolin
Journal of Taibah University for Science ( IF 2.8 ) Pub Date : 2020-09-26 , DOI: 10.1080/16583655.2020.1812269
Mohammad Javed Ansari 1 , Abdullah Alshetaili 1 , Ibrahim Abdulaziz Aldayel 1 , Faisal Mohammed Alablan 1 , Bader Alsulays 1 , Saad Alshahrani 1 , Ahmad Alalaiwe 1 , Mohd Nazam Ansari 2 , Najeeb Ur Rehman 2 , Faiyaz Shakeel 3
Affiliation  

The purpose of this study was to develop a self-nanoemulsifying drug delivery system (SNEDDS) for the improvement of solubility and bioavailability of luteolin in order to enhance its therapeutic benefits. Formulations were prepared by spontaneous emulsification method which involved low energy mixing of appropriate amounts ofcastor oil, kolliphor & polyethylene glycol 200. The developed formulae were optimized and characterized for self-nanoemulsifying capacity, thermodynamic stability, size behaviour and solubility. The globule size of the optimized formula F1–A1:1 was 112 ± 15 nm, with narrow PDI (0.31 ± 0.09) and good zeta potential (−16.2 ± 3.2 mV). The optimized formula exhibited approximately 83, 17 and 3-fold enhancement in the solubility in vitro release and ex vivo permeation respectively. The luteolin SNEDD exhibited better antioxidant activity (DPPH scavenging activity) than ascorbic acid. Per cent inhibition in rat paw oedema by the SNEDDS formulation was statistically significant when compared with luteolin suspension at equivalent dose (P < 0.05).



中文翻译:

木犀草素自纳米乳化药物递送系统的配制,表征,体外和体内评价

这项研究的目的是开发一种自纳米乳化药物递送系统(SNEDDS),以提高木犀草素的溶解度和生物利用度,从而增强其治疗效果。通过自发乳化法制备配方,该配方涉及低能量混合适量的蓖麻油,kolliphor和聚乙二醇200。对开发的配方进行了优化,并针对其自纳米乳化能力,热力学稳定性,尺寸行为和溶解度进行了表征。优化公式F1-A1:1的球尺寸为112±15 nm,具有窄的PDI(0.31±0.09)和良好的ζ电势(-16.2±3.2 mV)。优化配方在体外释放和离体渗透中分别显示出约83、17和3倍的溶解度增强。木犀草素SNEDD表现出比抗坏血酸更好的抗氧化活性(DPPH清除活性)。与同等剂量的木犀草素混悬液相比,SNEDDS制剂对大鼠爪水肿的抑制百分比具有统计学意义(P  <0.05)。

更新日期:2020-09-26
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