HPG-PLGA Nanoparticles for Enhanced Baicalin Delivery in Ulcerative Colitis Treatment

IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Qi Tan, Yuwei Hu, Bo Wang, Songwei Tan, Yang Guan, Li Zhou, Qing Tang
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Abstract

Ulcerative colitis (UC) is a chronic inflammatory bowel disease with a need for more effective and less invasive treatment options. This study aimed to develop a targeted drug delivery system using hyperbranched polyglycidylglycerol-poly(lactic acid)-hydroxyacetic acid (HPG-PLGA)nanoparticles (NPs) loaded with baicalin (BN), a flavonoid with potent anti-inflammatory properties, to enhance therapeutic efficacy in UC. HPG-PLGA NPs are synthesized, characterized, and loaded with BN. The particle size, polydispersity index (PDI), encapsulation efficiency, and in vitro release profile of the NPs are evaluated. The in vivo biodistribution and therapeutic efficacy of the NPs are assessed in a dextran sulfate sodium-induced UC mouse model. The synthesized HPG-PLGA NPs demonstrated good stability and a controlled release of BN. In vivo studies showed significant accumulation of NPs in the inflamed colon, with a subsequent reduction in disease activity and inflammation markers. The treatment group exhibited lower levels of tumor necrosis factor-alpha, interleukin-1 beta, and interleukin-6 compared to the model group, indicating effective alleviation of inflammation. Furthermore, the NPs showed no significant toxicity to major organs. This study provides a promising approach for the development of targeted UC treatments, offering a potential clinical application by enhancing the bioavailability and specificity of BN to inflammatory sites.

Abstract Image

HPG-PLGA纳米颗粒增强黄芩苷在溃疡性结肠炎治疗中的传递
溃疡性结肠炎(UC)是一种慢性炎症性肠病,需要更有效和更少侵入性的治疗方案。本研究旨在开发一种靶向给药系统,利用超支化聚甘油三酯-聚乳酸-羟基乙酸(HPG-PLGA)纳米颗粒(NPs)负载黄芩苷(BN),以提高UC的治疗效果。黄芩苷是一种具有强抗炎特性的类黄酮。合成了HPG-PLGA NPs,对其进行了表征,并负载了BN。评价了NPs的粒径、多分散指数(PDI)、包封效率和体外释放特性。在葡聚糖硫酸钠诱导UC小鼠模型中评估NPs的体内生物分布和治疗效果。合成的HPG-PLGA NPs具有良好的稳定性和BN的缓释性。体内研究表明,NPs在发炎的结肠中显著积累,随后疾病活动性和炎症标志物减少。与模型组相比,治疗组肿瘤坏死因子- α、白细胞介素-1 β和白细胞介素-6水平较低,表明炎症得到有效缓解。此外,NPs对主要器官没有明显的毒性作用。本研究为UC靶向治疗的发展提供了一条有希望的途径,通过提高BN对炎症部位的生物利用度和特异性,提供了潜在的临床应用。
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来源期刊
Advanced Therapeutics
Advanced Therapeutics Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.10
自引率
2.20%
发文量
130
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