标题：山萘酚靶向脂质体的制备与评价

文献链接：https://xueshu.baidu.com/usercenter/paper/show?paperid=1g680vn0jq2m08y05w0v02a0ha417808&site=xueshu_se

作者：刘祖浩，雷玉杰，宋浩颖，常聪

摘要：

目的制备山萘酚靶向脂质体(cRGD-LP-KAE)并考察初步稳定性.方法 以L-α-磷脂酰胆碱(PC),胆固醇(CHO),二硬脂酰基磷脂酰乙醇胺-聚乙二醇-环精氨酰甘氨酰天冬氨酸(DSPE-PEG-cRGD),山萘酚(KAE)为材料,采用薄膜分散法结合微孔滤膜法制备cRGD-LP-KAE;以粒径,包封率等指标筛选胆脂比,药脂比,聚脂比与冻干保护剂,确定脂质体的最优处方工艺;用透射电镜观察脂质体形貌,粒度电位仪检测脂质体粒径及其分布,zeta电位,紫外分光光度法检测脂质体载药量与包封率;以脂质体复溶后粒径,包封率的变化为指标考察初步稳定性.结果 最优处方工艺是CHO,KAE,DSPE-PEG-cRGD和PC的摩尔比为15 ︰ 6 ︰ 4 ︰ 120,蔗糖作为冻干保护剂,其与PC的质量比是4 ︰ 1.根据该处方工艺制备的脂质体呈类球形结构,粒径和zeta电位分别是(148.60±0.20)nm和(-21.97±0.15)mV,包封率和载药量分别是(98.97±0.27)%和(1.12±0.06)%,在低温存储15天时粒径增加2.76%,包封率降低2.71%.结论cRGD-LP-KAE粒径小且分布均匀,包封率高,在低温存储时稳定性良好。

译文：

Objective to prepare kaempferol targeted liposomes (crgd LP KAE) and investigate its preliminary stability Methods using L - α - phosphatidylcholine (PC), cholesterol (CHO), distearoyl phosphatidylethanolamine polyethylene glycol cycloarginyl glycyl aspartic acid (DSPE peg crgd), kaempferol (KAE) as materials, crgd LP KAE was prepared by membrane dispersion method combined with microporous filtration membrane method; The optimal formulation and technology of liposomes were determined by selecting the bile lipid ratio, drug lipid ratio, polyester ratio and freeze-drying protectants according to particle size, entrapment efficiency and other indicators; The morphology of liposomes was observed by transmission electron microscope, the particle size and distribution of liposomes were detected by particle size potential meter, the zeta potential, and the drug loading and entrapment efficiency of liposomes were detected by UV spectrophotometry; The initial stability of liposomes was evaluated by the changes of particle size and entrapment efficiency after re dissolution Results the optimal formulation process was that the molar ratio of CHO, KAE, DSPE peg crgd and PC was 15 ∶ 6 ∶ 4 ∶ 120, and the mass ratio of sucrose to PC was 4 ∶ 1. The liposomes prepared according to the formulation process were spherical like structure, with particle size and zeta potential of (148.60 ± 0.20) nm and (-21.97 ± 0.15) MV, respectively. The entrapment efficiency and drug loading were (98.97 ± 0.27)% and (1.12 ± 0.06)% respectively. When stored at low temperature for 15 days, the particle size increased by 2.76%, and the entrapment efficiency decreased by 2.71%.It is necessary to Conclusion crgd LP KAE has small particle size, uniform distribution, high encapsulation efficiency and good stability in low temperature storage.

DOI：10.3969/j.issn.1008-987x.2021.03.09

研究背景

山萘酚（α-mangostin）是一种来源于山竹果皮的天然产物，具有一定的*氧化、*微生物等生物活性。由于其水溶性差、生物利用度低、在体分布不均等问题，其直接应用受到限制。脂质体作为一种包载性强、生物相容性良好的载药系统，在改善山萘酚药代行为方面具有潜力。

此外，为提升山萘酚在特定细胞或组织中的富集效率，可将脂质体进一步修饰以实现主动靶向。例如，通过引入小分子配体（如RGD、多肽、糖类）、抗体片段或其他识别结构，可增强其细胞识别性和转运能力。

山萘酚脂质体系统结合了纳米递送平台与天然活性分子的优势，具备一定的开发前景。通过PEG修饰可以显著延长脂质体在体内的循环时间，而引入RGD、叶酸或其他配体实现主动靶向，可增强在疾病部位的聚集与摄取能力。

本体系的后续优化方向可包括：

• 不同PEG链长与密度对靶向效果的影响；

• 多肽序列选择与排列对亲和力的调节；

• 与其他天然药物（如姜黄素、白藜芦醇）组合递送的协同效果；

• 体内药动学、组织分布及安全性评估。

西安齐岳生物提供相关产品：

Peptides PEG DSPE

RGD-PEG-DSPE

cRGD-PEG-Hyd-DSPE

cRGD(c[RGDfc])-PEG-DSPE

cRGD(c[RGDfK])-PEG-DSPE

cRGD(c[RGDyK])-PEG-DSPE

iRGD-PEG-DSPE

TAT-PEG-DSPE

Cy3-iRGD-PEG-DSPE

FITC-iRGD-PEG-DSPE

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