Preparation of double-loaded bitter ginseng derivative B21-DOX liposomes co-modified with SP94 and BR2 ligand and its in vitro anti-hepatocarcinogenic effect.

IF 3 4区 医学 Q2 CHEMISTRY, APPLIED Journal of microencapsulation Pub Date : 2024-11-01 Epub Date: 2024-08-16 DOI:10.1080/02652048.2024.2390955
Lin Jing, Jiajia Zhang, Lili Li, Simei Luo, Zijun Tang, Xu Liu, Yonglong Zhong, Mingqing Yuan
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Abstract

Aim: To construct a novel liposomal drug delivery system co-modified with SP94 and BR2 ligands, encapsulating both the bitter ginseng derivative B21 and doxorubicin (DOX), to achieve superior anti-tumour efficacy and reduced toxic side effects.

Methods: Liposomes were prepared using an organic phase reaction method, with B21 encapsulated in the lipid phase and DOX in the aqueous phase. The liposomes were further modified with SP94 and BR2 peptides. The characterisations, cytotoxicity, and in vitro targeting effects were assessed through various methods including ultraviolet spectrophotometry, high-performance liquid chromatography, nano-size analysis, ultrafiltration centrifugation, dialysis, transmission electron microscopy, flow cytometry, Methylthiazolyldiphenyl-tetrazolium bromide assay, confocal laser scanning microscopy, transwell assay, and tumorsphere assay.

Results: SP94/BR2-B21/DOX-LP liposomes were spherical with an average diameter of 120.87 ± 1.00 nm, a polydispersity index (PDI) of 0.223 ± 0.006, and a surface charge of -23.1 ± 1.27 mV. The encapsulation efficiencies for B21 and DOX were greater than 85% and 97% (mg/mg), respectively. The results indicated that SP94/BR2-B21/DOX-LP exhibited enhanced targeting and cytotoxicity compared to single-ligand modified and unmodified liposomes, with the combined encapsulation of B21 and DOX showing synergistic anti-hepatocarcinogenic effects.

Conclusion: SP94/BR2-B21/DOX-LP liposomes represent a promising targeted drug delivery system for hepatocellular carcinoma, offering improved membrane penetration, enhanced therapeutic efficacy, and reduced systemic toxicity.

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SP94和BR2配体共同修饰的双载体苦参衍生物B21-DOX脂质体的制备及其体外抗肝癌作用
目的:构建一种新型脂质体给药系统,该系统由SP94和BR2配体共同修饰,同时包裹苦参衍生物B21和多柔比星(DOX),以实现卓越的抗肿瘤疗效并减少毒副作用:方法:采用有机相反应法制备脂质体,脂质相中封装 B21,水相中封装 DOX。用 SP94 和 BR2 肽进一步修饰脂质体。通过紫外分光光度法、高效液相色谱法、纳米粒度分析法、超滤离心法、透析法、透射电子显微镜法、流式细胞仪法、甲基噻唑二苯基溴化四氮唑检测法、激光共聚焦扫描显微镜法、经孔检测法和瘤球检测法等多种方法对脂质体的特性、细胞毒性和体外靶向效应进行了评估:SP94/BR2-B21/DOX-LP 脂质体呈球形,平均直径为 120.87 ± 1.00 nm,多分散指数(PDI)为 0.223 ± 0.006,表面电荷为 -23.1 ± 1.27 mV。B21 和 DOX 的封装效率分别大于 85% 和 97% (毫克/毫克)。结果表明,与单一配体修饰脂质体和未修饰脂质体相比,SP94/BR2-B21/DOX-LP具有更强的靶向性和细胞毒性,B21和DOX的联合包封具有协同抗肝癌作用:SP94/BR2-B21/DOX-LP脂质体是一种很有前景的肝细胞癌靶向给药系统,它能改善膜渗透性、提高疗效并降低全身毒性。
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来源期刊
Journal of microencapsulation
Journal of microencapsulation 工程技术-工程:化工
CiteScore
6.30
自引率
2.60%
发文量
39
审稿时长
3 months
期刊介绍: The Journal of Microencapsulation is a well-established, peer-reviewed journal dedicated to the publication of original research findings related to the preparation, properties and uses of individually encapsulated novel small particles, as well as significant improvements to tried-and-tested techniques relevant to micro and nano particles and their use in a wide variety of industrial, engineering, pharmaceutical, biotechnology and research applications. Its scope extends beyond conventional microcapsules to all other small particulate systems such as self assembling structures that involve preparative manipulation. The journal covers: Chemistry of encapsulation materials Physics of release through the capsule wall and/or desorption from carrier Techniques of preparation, content and storage Many uses to which microcapsules are put.
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