Baicalein Long-Circulating Liposomes Improve Histological and Functional Outcomes After Traumatic Brain Injury.

IF 2.1 Q3 PHARMACOLOGY & PHARMACY
Advances in Pharmacological and Pharmaceutical Sciences Pub Date : 2024-11-22 eCollection Date: 2024-01-01 DOI:10.1155/adpp/2869332
Dong Yuan, Wenbo Xu, Faisal Raza, Hajra Zafar, Shuangxian Guan, Zhen Wang, Kamran Hidayat Ullah, Hongchao Shi
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Abstract

High mortality and disability have been principally linked with traumatic brain injury (TBI) with this condition being a principal issue in public health. Currently, there is no reliable pharmaceutical agent to salvage the damage caused by TBI. Baicalein (BCL), a traditional Chinese medicine active ingredient, has preliminarily shown repair activity on brain injury. However, BCL has poor water solubility and bioavailability, which culminates in rapid elimination in vivo. Herein, we sought to solve the above-mentioned challenges that are associated with the application of this flavonoid by preparing BCL-loaded long-circulating liposomes (BLC-Lips) via thin-film hydration method. Subsequently, BLC-Lips were applied to TBI model mice to evaluate their effect on brain injury repair. The results showed that the prepared BLC-Lips exhibited smaller sized nanoparticles, excellent polydispersed index (PDI), and zeta (ζ)-potential with stable property. After loading of BCL into the liposomes, we estimated the physicochemical properties of BLC-Lips to be roughly 87.98% (encapsulation efficiency [EE]) and 7.56% (loading capacity of the drug). Administration of BLC-Lips through oral route increased aqueous solubility, bioavailability, and time for in vivo circulation of BCL. Moreover, the BLC-Lips could improve outcomes of histological and neurological motor function and reduce inflammatory cytokines and neurotoxicity after TBI. Taken together, the long-circulating liposomes may serve as a new approach to potentially prolong drug circulation in vivo and increased bioavailability of BCL for TBI treatment.

黄芩素长循环脂质体改善创伤性脑损伤后的组织学和功能预后。
高死亡率和残疾主要与创伤性脑损伤有关,这种情况是公共卫生的一个主要问题。目前,还没有可靠的药物来挽救创伤性脑损伤。黄芩素(Baicalein, BCL)是一种中药活性成分,已初步显示出对脑损伤的修复作用。然而,BCL具有较差的水溶性和生物利用度,最终导致体内快速消除。为此,我们试图通过薄膜水合法制备bcl负载的长循环脂质体(BLC-Lips)来解决上述与该类黄酮应用相关的挑战。随后,将BLC-Lips应用于TBI模型小鼠,评估其对脑损伤的修复作用。结果表明,制备的BLC-Lips具有较小的纳米颗粒尺寸,优异的多分散指数(PDI)和ζ (ζ)电位,性能稳定。将BCL装入脂质体后,我们估计BLC-Lips的理化性质约为87.98%(包封效率[EE])和7.56%(药物的载药量)。口服给药可增加BCL的水溶性、生物利用度和体内循环时间。此外,BLC-Lips可以改善TBI后的组织学和神经运动功能,降低炎症细胞因子和神经毒性。综上所述,长循环脂质体可能作为一种新的方法,可以潜在地延长药物在体内的循环,提高BCL治疗TBI的生物利用度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
4.30
自引率
3.60%
发文量
0
审稿时长
17 weeks
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