Bamankar Suraj, Londhe Vaishali
Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, Vile Parle [W], 400056 Mumbai, Maharashtra, India.
Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS, Vile Parle [W], 400056 Mumbai, Maharashtra, India.
Ann Pharm Fr. 2023 Nov;81(6):985-996. doi: 10.1016/j.pharma.2023.09.001. Epub 2023 Sep 12.
Major depressive disorder (also known as depression) is a serious mental health condition that has a detrimental impact on a person's mood, thoughts, and behaviour. The presence of oxidative stress is associated with an increased risk of developing depression. A flavonoid called hesperidin (HSP) has been proven to be helpful in experimental depression because of its powerful antioxidant properties. However, due to its limited bioavailability, gastro-intestinal degradation, inadequate permeability, and low water solubility, the clinical development of HSP has been impeded. The objective of the present research was to develop HSP nanoparticles (NPs) loaded in-situ gel for nose-to-brain delivery to provide neuroprotective action.
HSP NPs were prepared by nanoprecipitation technique and were tailored to the size by using ultrasonication technique. Optimisation of NPs was conducted using the central composite design. Prepared particles were analysed by Fourier transformed infrared spectroscopy (FTIR), DSC, and UV technique. Forced swim test was conducted as a behavioural assessment to gauze the neuroprotective antidepressant activity of the prepared formulation.
The particle size was found to be in the range of 76.5±0.86nm to 239.2+0.31nm, zeta potential in the range of -8.37±0.6mV to 22.4±1.37mV, and entrapment efficiency in the range of 54.92±1.36% to 74.53±1.28%. Pharmacodynamic study showed formulation significantly decreased the immobility time in experimental animals.
This study showed the potential of HSP NPs to be an effective neuroprotective agent.
重度抑郁症(也称为抑郁症)是一种严重的心理健康状况,会对人的情绪、思维和行为产生不利影响。氧化应激的存在与患抑郁症风险的增加有关。一种名为橙皮苷(HSP)的类黄酮因其强大的抗氧化特性,已被证明在实验性抑郁症中具有帮助作用。然而,由于其生物利用度有限、胃肠道降解、通透性不足和水溶性低,HSP的临床开发受到了阻碍。本研究的目的是开发负载于原位凝胶中的HSP纳米颗粒(NPs)用于鼻脑递送,以提供神经保护作用。
通过纳米沉淀技术制备HSP NPs,并使用超声技术调整其大小。采用中心复合设计对NPs进行优化。通过傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)和紫外技术对制备的颗粒进行分析。进行强迫游泳试验作为行为评估,以评估所制备制剂的神经保护抗抑郁活性。
发现粒径在76.5±0.86nm至239.2+0.31nm范围内,zeta电位在-8.37±0.6mV至22.4±1.37mV范围内,包封率在54.92±1.36%至74.53±1.28%范围内。药效学研究表明,该制剂显著缩短了实验动物的不动时间。
本研究表明HSP NPs有潜力成为一种有效的神经保护剂。