本研究旨在开发一种脂质纳米平台，命名为“BAL-PTX-LN”，共负载手性黄芩苷衍生物（BAL）和紫杉醇（PTX），以提高紫杉醇的抗肺癌功效并降低紫杉醇的毒性。化疗药物。基于单因素实验，通过中心组合设计优化BAL-PTX-LN。通过 TEM、粒径、包封率、溶血率、释放动力学和稳定性评价 BAL-PTX-LN。并通过药代动力学评价并研究体外和体内的抗肿瘤功效。使用苏木精和伊红 (HE) 染色评估制剂的体内安全性。BAL-PTX-LN 呈球形，粒径为 134.36 ± 3.18 nm，PDI 为 0.24 ± 0.02，包封率超过 90 %，BAL-PTX-LN 储存 180 天后保持稳定。体外释放研究揭示了脂质体制剂中 PTX 的零级动力学模型。制剂组未见溶血现象。 BAL-PTX-LN 组中 PTX 的药代动力学分析显示，与原料药组相比，其生物利​​用度高出约三倍，t1/2 长两倍。此外，与PTX组相比，24 h时BAL-PTX-LN的IC50降低了2.35倍（13.48 μg/mL vs 31.722 μg/mL），细胞凋亡率增加了1.82倍（29.38% vs 16.13%）。在荷瘤裸鼠中，BAL-PTX-LN 制剂的肿瘤抑制率比 PTX 组高出两倍（62.83% vs 29.95%），同时 Ki67 表达降低十倍（4.26% vs. 45.88%）。有趣的是，HE染色显示BAL-PTX-LN组组织无病理变化，而PTX组组织出现病理变化和肿瘤细胞浸润。BAL-PTX-LN提高了难溶性化疗药物对肺癌的治疗效果，预计将在临床应用中成为一种可行的肺癌治疗剂。© 2024 Chen 等人。

The present study aimed to develop a lipid nanoplatform, denoted as "BAL-PTX-LN", co-loaded with chiral baicalin derivatives (BAL) and paclitaxel (PTX) to promote the anti-lung cancer efficacy of paclitaxel and reduce the toxicity of chemotherapeutic drugs.BAL-PTX-LN was optimized through central composite design based on a single-factor experiments. BAL-PTX-LN was evaluated by TEM, particle size, encapsulation efficiency, hemolysis rate, release kinetics and stability. And was evaluated by pharmacokinetics and the antitumor efficacy studied both in vitro and in vivo. The in vivo safety profile of the formulation was assessed using hematoxylin and eosin (HE) staining.BAL-PTX-LN exhibited spherical morphology with a particle size of 134.36 ± 3.18 nm, PDI of 0.24 ± 0.02, and with an encapsulation efficiency exceeding 90%, BAL-PTX-LN remained stable after 180 days storage. In vitro release studies revealed a zero-order kinetic model of PTX from the liposomal formulation. No hemolysis was observed in the preparation group. Pharmacokinetic analysis of PTX in the BAL-PTX-LN group revealed an approximately three-fold higher bioavailability and twice longer t1/2 compared to the bulk drug group. Furthermore, the IC50 of BAL-PTX-LN decreased by 2.35 times (13.48 μg/mL vs 31.722 μg/mL) and the apoptosis rate increased by 1.82 times (29.38% vs 16.13%) at 24 h compared to the PTX group. In tumor-bearing nude mice, the BAL-PTX-LN formulation exhibited a two-fold higher tumor inhibition rate compared to the PTX group (62.83% vs 29.95%), accompanied by a ten-fold decrease in Ki67 expression (4.26% vs 45.88%). Interestingly, HE staining revealed no pathological changes in tissues from the BAL-PTX-LN group, whereas tissues from the PTX group exhibited pathological changes and tumor cell infiltration.BAL-PTX-LN improves the therapeutic effect of poorly soluble chemotherapeutic drugs on lung cancer, which is anticipated to emerge as a viable therapeutic agent for lung cancer in clinical applications.© 2024 Chen et al.