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微流控技术制备黄芩苷脂质体及其斑马鱼模型抗肿瘤活性评价

Preparation of Baicalin Liposomes Using Microfluidic Technology and Evaluation of Their Antitumor Activity by a Zebrafish Model.

作者信息

Gu Yuhao, Jin Liqiang, Wang Li, Ma Xianzheng, Tian Mingfa, Sohail Ammara, Wang Jianchun, Wang Daijie

机构信息

School of Light Industry Science and Engineering, Qilu University of Technology (Shandong Academy of Sciences), Jinan 250353, China.

Heze Branch of Qilu University of Technology (Shandong Academy of Sciences), Heze 274000, China.

出版信息

ACS Omega. 2024 Sep 24;9(40):41289-41300. doi: 10.1021/acsomega.4c03356. eCollection 2024 Oct 8.

Abstract

Baicalin (BCL), a well-known flavonoid molecule, has numerous therapeutic applications. However, its low water solubility and bioavailability limit its applicability. Microfluidics is a new method for liposome preparation that provides efficient and rapid control of the process, improving the stability and controllability. This study used microfluidic techniques to create baicalin liposomes (BCL-LPs), first screening for optimal total flow rates (TFR) and flow rate ratios (FRR), and then optimizing the phospholipid concentration, phospholipid-to-cholesterol ratio, and Tween-80 concentration using univariate and response surface methodology approaches. The study found that the ideal phospholipid content was 9.5%, the phospholipid-to-cholesterol ratio was 9:1 (:), and the Tween-80 concentration was 15%. BCL-LPs achieved 95.323% ± 0.481% encapsulation efficiency under the optimum circumstances. Characterization indicated that the BCL-LPs were spherical and uniform in size, with a mean diameter of 62.32 nm ± 0.42, a polydispersity index of 0.092 ± 0.009, and a zeta potential of -25.000 mV ± 0.216. experiments found that BCL-LPs had a better slow-release effect and stability than the BCL monomer. In zebrafish bioassays, BCL-LPs performed better than BCL monomer in terms of biological activity and bioavailability. The established method provided a feasible medicine delivery platform for BCL and could apply for the transport and encapsulation of more natural compounds, expanding the applications of drug delivery systems in healthcare and cancer therapies.

摘要

黄芩苷(BCL)是一种著名的黄酮类分子,具有多种治疗应用。然而,其低水溶性和生物利用度限制了其适用性。微流控技术是一种制备脂质体的新方法,可对该过程进行高效快速的控制,提高稳定性和可控性。本研究采用微流控技术制备黄芩苷脂质体(BCL-LPs),首先筛选最佳总流速(TFR)和流速比(FRR),然后采用单因素和响应面法优化磷脂浓度、磷脂与胆固醇的比例以及吐温-80浓度。研究发现,理想的磷脂含量为9.5%,磷脂与胆固醇的比例为9:1(:),吐温-80浓度为15%。在最佳条件下,BCL-LPs的包封率达到95.323%±0.481%。表征结果表明,BCL-LPs呈球形且大小均匀,平均直径为62.32 nm±0.42,多分散指数为0.092±0.009,ζ电位为-25.000 mV±0.216。实验发现,BCL-LPs比BCL单体具有更好的缓释效果和稳定性。在斑马鱼生物测定中,BCL-LPs在生物活性和生物利用度方面比BCL单体表现更好。所建立的方法为BCL提供了一个可行的药物递送平台,可应用于更多天然化合物的运输和包封,拓展了药物递送系统在医疗保健和癌症治疗中的应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9635/11465266/07d772e3c531/ao4c03356_0001.jpg

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