Jangde Rajendra, Elhassan Gamal Osman, Khute Sulekha, Singh Deependra, Singh Manju, Sahu Ram Kumar, Khan Jiyauddin
University Institute of Pharmacy, Pt. Ravishankar Shukla University, Raipur 492010, India.
Department of Pharmaceutics, Unaizah College of Pharmacy, Qassim University, Unaizah 51911, Saudi Arabia.
Pharmaceuticals (Basel). 2022 Feb 10;15(2):211. doi: 10.3390/ph15020211.
Hesperidin is a bioflavonoid constituent that among many other biological activities shows significant wound healing properties. However, the bioavailability of hesperidin when applied topically is limited due to its low solubility and systemic absorption, so novel dosage forms are needed to improve its therapeutic efficacy. The objectives of this study were to develop hesperidin-loaded lipid-polymer hybrid nanoparticles (HLPHNs) to enhance the delivery of hesperidin to endogenous sites in the wound bed and promote the efficacy of hesperidin. HLPHNs were optimized by response surface methodology (RSM) using the Box-Behnken design. HLPHNs were prepared using an emulsion-solvent evaporation method based on a double emulsion of water-in-oil-in-water (w/o/w) followed by freeze-drying to obtain nanoparticles. The prepared formulations were characterized using various evaluation parameters. In addition, the antioxidant activity of HLPHN 4 was investigated in vitro using the DPPH model. Seventeen different HLPHNs were prepared and the HLPHN4 exhibited the best mean particle size distribution, zeta potential, drug release and entrapment efficiency. The values are 91.43 nm, +23 mV, 79.97% and 92.8%, respectively. Transmission electron microscope showed similar spherical morphology as HLPHN4. Differential scanning calorimetry verified the physical stability of the loaded drug in a hybrid system. In vitro release studies showed uniform release of the drug over 24 h. HLPHN4 showed potent antioxidant activity in vitro in the DPPH model. The results of this study suggest that HLPHNs can achieve sustained release of the drug at the wound site and exhibit potent in vitro antioxidant activity.
橙皮苷是一种生物类黄酮成分，在许多其他生物活性中表现出显著的伤口愈合特性。然而，由于其低溶解度和全身吸收，局部应用时橙皮苷的生物利用度有限，因此需要新型剂型来提高其治疗效果。本研究的目的是开发载有橙皮苷的脂质-聚合物杂化纳米粒（HLPHNs），以增强橙皮苷向伤口床内源性部位的递送，并提高橙皮苷的疗效。使用Box-Behnken设计的响应面法（RSM）对HLPHNs进行优化。基于水包油包水（w/o/w）的双重乳液，采用乳化溶剂蒸发法制备HLPHNs，然后冷冻干燥以获得纳米粒。使用各种评估参数对制备的制剂进行表征。此外，使用DPPH模型在体外研究了HLPHN 4的抗氧化活性。制备了17种不同的HLPHNs，HLPHN4表现出最佳的平均粒径分布、zeta电位、药物释放和包封率。其值分别为91.43 nm、+23 mV、79.97%和92.8%。透射电子显微镜显示HLPHN4具有相似的球形形态。差示扫描量热法验证了载药在杂化体系中的物理稳定性。体外释放研究表明药物在24小时内均匀释放。HLPHN4在DPPH模型中体外表现出强大的抗氧化活性。本研究结果表明，HLPHNs可以在伤口部位实现药物的持续释放，并在体外表现出强大的抗氧化活性。
