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小檗碱负载的纳米复合胶对角叉菜胶诱导的大鼠急性爪肿胀抗炎反应的评估

Evaluation of anti-inflammatory response of berberine-loaded gum nanocomplexes in carrageenan-induced acute paw edema in rats.

作者信息

Bakshi Jyoti, Lathar Prity, Mehra Meenakshi, Grewal Sapna, Dhingra Dinesh, Kumari Santosh

机构信息

Department of Bio and Nano Technology, Guru Jambheshwar University of Science and Technology, Hisar, India.

Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar, India.

出版信息

Pharmacol Rep. 2022 Apr;74(2):392-405. doi: 10.1007/s43440-021-00350-z. Epub 2022 Jan 5.

Abstract

BACKGROUND

Berberine is a natural plant alkaloid and has been reported to possess anti-inflammatory activity. However, berberine's poor bioavailability and low solubility have limited its clinical applicability. Nanoencapsulation of berberine using a suitable carrier can be a promising strategy to improve its efficacy. Therefore, this study aimed to produce berberine-loaded gum nanocomplexes to evaluate their therapeutic effects in a carrageenan-induced rat model.

METHODS

Berberine-loaded gum nanocomplexes were prepared by the ionic complexation between the negative charges of the gums (tragacanth and acacia gum) using a cross-linker for loading cationic berberine and their anti-inflammatory activity was evaluated against carrageenan-induced paw edema in rats. ELISA and qRT-PCR were employed to measure the concentration and mRNA expression level of inflammatory mediators in plasma and paw tissue, respectively.

RESULTS

Berberine nanocomplexes were characterized for particle size (219.5 nm), zeta potential by the dynamic light scattering (DLS), and for entrapment efficiency (93.2%) Infrared spectroscopy affirmed the loading of berberine in gum nanocomplexes. Transmission electron microscopy of formulation showed the spherical shape of nanocomplexes and small particle size (100-150 nm). Pretreatment of rats with berberine nanocomplexes significantly reduced the paw edema in inflamed rat paws, decreased the production of nitrite and TNF-α in plasma and repressed the mRNA expression levels of TNF-α and IL-1β in paw tissue in comparison to berberine per se treated rats.

CONCLUSION

The obtained berberine-loaded gum nanocomplexes produced a better anti-inflammatory effect as compared to berberine alone and hence can be used as an efficient candidate in the treatment of inflammation. The schematic representation of the preparation of the preparation of berberine-loaded tragacanth/acacia gum nanocomplexes and the evaluation in vivo for anti-inflammatory effects.

摘要

背景

黄连素是一种天然植物生物碱,据报道具有抗炎活性。然而,黄连素较差的生物利用度和低溶解度限制了其临床应用。使用合适的载体对黄连素进行纳米包封可能是提高其疗效的一种有前景的策略。因此,本研究旨在制备载黄连素的树胶纳米复合物,以评估其在角叉菜胶诱导的大鼠模型中的治疗效果。

方法

通过使用交联剂使树胶(黄芪胶和阿拉伯胶)的负电荷与阳离子黄连素进行离子络合,制备载黄连素的树胶纳米复合物,并评估其对大鼠角叉菜胶诱导的爪肿胀的抗炎活性。采用酶联免疫吸附测定法(ELISA)和定量逆转录聚合酶链反应(qRT-PCR)分别测量血浆和爪组织中炎症介质的浓度和mRNA表达水平。

结果

通过动态光散射(DLS)对黄连素纳米复合物的粒径(219.5nm)、zeta电位进行了表征,并测定了包封率(93.2%)。红外光谱证实了黄连素负载于树胶纳米复合物中。制剂的透射电子显微镜显示纳米复合物呈球形且粒径较小(100 - 150nm)。与单独使用黄连素治疗的大鼠相比,用黄连素纳米复合物预处理大鼠可显著减轻炎症大鼠爪的爪肿胀,降低血浆中亚硝酸盐和肿瘤坏死因子-α(TNF-α)的产生,并抑制爪组织中TNF-α和白细胞介素-1β(IL-1β)的mRNA表达水平。

结论

与单独的黄连素相比,所制备的载黄连素的树胶纳米复合物具有更好的抗炎效果,因此可作为治疗炎症的有效候选药物。载黄连素的黄芪胶/阿拉伯胶纳米复合物的制备及其体内抗炎效果评估的示意图。

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