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Hesperetin loaded proposomal gel for topical antioxidant activity
Journal of Drug Delivery Science and Technology ( IF 4.5 ) Pub Date : 2021-10-23 , DOI: 10.1016/j.jddst.2021.102873
Vanessa Marcia Vaz 1 , Srinivas Reddy Jitta 1 , Ruchi Verma 2 , Lalit Kumar 1
Affiliation  

The present study was aimed at formulating and evaluating hesperetin-loaded proposomal gel for topical antioxidant activity. Hesperetin-loaded proposomes were first formulated and optimized with the central composite design and were characterized for particle size, polydispersity index, zeta potential and entrapment efficiency. In vitro release studies were also performed for the formulation. Various polymeric gel bases were assessed and one of them was selected to formulate the proposomal gel. The gels were characterized for their appearance, content uniformity, viscosity, spreadability and swelling index. In vitro diffusion studies were also carried out on the proposomal gel. Finally, in vitro antioxidant potentials of hesperetin and the proposomal formulation was determined using the 2,2- diphenyl-1-picrylhydrazyl hydrate (DPPH) assay. The optimized proposomal formulation showed enhanced in vitro drug release with a release of 95.51 ± 8.85% after 84 h compared to the hesperetin dispersion which released only 34.00 ± 1.71%. 1% carbopol was selected as a suitable gel base for the proposomal gel. The proposomal gel formulated showed good properties and was able to further sustain the drug release from the proposomes by releasing 42.63 ± 2.11% of the drug after 144 h. Finally, hesperetin and hesperetin-loaded proposomes showed comparable in vitro antioxidant activities with IC50 values of 82.15 μg/mL and 88.07 μg/mL, respectively. We can conclude that hesperetin-loaded proposomal gel can be an effective formulation with a controlled release profile and could be used to treat topical oxidative conditions.



中文翻译:

橙皮素载药体凝胶具有局部抗氧化活性

本研究旨在配制和评估负载橙皮素的提议体凝胶的局部抗氧化活性。负载橙皮素的提议体首先通过中心复合设计进行配制和优化,并针对粒度、多分散指数、zeta 电位和截留效率进行表征。还对制剂进行了体外释放研究。对各种聚合物凝胶基质进行了评估,并选择其中一种来配制提议体凝胶。凝胶的特征在于它们的外观、含量均匀性、粘度、铺展性和溶胀指数。还对提议体凝胶进行了体外扩散研究。最后,橙皮素和提案体制剂的体外抗氧化潜力使用 2,2-二苯基-1-苦基肼水合物 (DPPH) 测定法测定。与仅释放 34.00 ± 1.71% 的橙皮素分散体相比,优化的提案体制剂显示出增强的体外药物释放,84 小时后释放率为 95.51 ± 8.85%。选择 1% carbopol 作为合适的凝胶基质用于建议体凝胶。配制的提议体凝胶显示出良好的特性,并且能够通过在 144 小时后释放 42.63 ± 2.11% 的药物来进一步维持药物从提议体中的释放。最后,橙皮素和橙皮素载药体显示出与 IC 相当的体外抗氧化活性 配制的提议体凝胶显示出良好的特性,并且能够通过在 144 小时后释放 42.63 ± 2.11% 的药物来进一步维持药物从提议体中的释放。最后,橙皮素和负载橙皮素的载体表现出与 IC 相当的体外抗氧化活性 配制的提议体凝胶显示出良好的特性,并且能够通过在 144 小时后释放 42.63 ± 2.11% 的药物来进一步维持药物从提议体中的释放。最后,橙皮素和负载橙皮素的载体表现出与 IC 相当的体外抗氧化活性50 个值分别为 82.15 μg/mL 和 88.07 μg/mL。我们可以得出结论,橙皮素载药体凝胶是一种具有控释特性的有效制剂,可用于治疗局部氧化病症。

更新日期:2021-10-24
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