含磷脂复合物的（L.）提取物的研发与评估：一种在啮齿动物模型中治疗神经性疼痛的临床前方法。
Development and evaluation of (L.) extract containing phytosomes: a preclinical approach for treatment of neuropathic pain in rodent model.
作者信息
Kumar Nitin, Goel Radha, Singh Monika, Sharma Neeraj Kant, Gaur Praveen Kumar, Sharma Pradeep Kumar
机构信息
Department of Pharmacy, Meerut Institute of Technology, Meerut, India.
Department of Pharmacology, Lloyd Institute of Management and Technology, Greater Noida, India.
出版信息
J Microencapsul. 2023 May;40(3):186-196. doi: 10.1080/02652048.2023.2188938. Epub 2023 Mar 20.
PURPOSE
The study was aimed to encapsulate extract (HCE) into phytosomes to improve its therapeutic efficacy in neuropathic pain by enhancing the bioavailability of chief chemical constituent Hedycoryside -A (HCA).
METHODS
For preparing phytosomes complexes (F1, F2, and F3), HCE and phospholipids were reacted in disparate ratio. F2 was chosen to assess its therapeutic efficacy in neuropathic pain induced by partial sciatic nerve ligation. Nociceptive threshold and oral bioavailability were also estimated for F2.
RESULTS
Particle size, zeta potential and entrapment efficiency for F2 were analysed as 298.1 ± 1.1 nm, -3.92 ± 0.41 mV and 72.12 ± 0.72% respectively. F2 gave enhanced relative bioavailability (158.92%) of HCA along with a greater neuroprotective potential showing a significant antioxidant effect and augmentation (p < 0.05) in nociceptive threshold with the diminution in damage to nerves.
CONCLUSION
F2 is an optimistic formulation for enhancing the HCE delivery for the effective treatment of neuropathic pain.
目的
本研究旨在将提取物（HCE）包封到磷脂体中，通过提高主要化学成分海得可苷 -A（HCA）的生物利用度来提高其对神经性疼痛的治疗效果。
方法
为制备磷脂体复合物（F1、F2和F3），HCE与磷脂以不同比例反应。选择F2评估其对坐骨神经部分结扎诱导的神经性疼痛的治疗效果。还对F2的痛觉阈值和口服生物利用度进行了评估。
结果
F2的粒径、zeta电位和包封率分别分析为298.1±1.1nm、-3.92±0.41mV和72.12±0.72%。F2使HCA的相对生物利用度提高（158.92%），同时具有更大的神经保护潜力，表现出显著的抗氧化作用，痛觉阈值增加（p<0.05），神经损伤减少。
结论
F2是一种用于增强HCE递送以有效治疗神经性疼痛的理想制剂。
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