薄荷醇修饰紫杉醇阳离子脂质体处方优选及体外靶向性评价

Prescription Optimization and in vitro Targeting Evaluation of Menthol-modified Paclitaxel Cationic Liposomes

目的 制备薄荷醇修饰紫杉醇阳离子脂质体(Men-PCLPs)并优化处方,评价Men-PCLPs体外靶向性。方法 采用薄膜分散法制备Men-PCLPs。使用Box-Benhken响应面法选出Men-PCLPs最优处方工艺。评价各组脂质体对C6细胞存活率的影响。用流式细胞仪检测C6和bEnd.3细胞对不同脂质体的摄取情况。结果 脂质体最优处方为磷脂106 mg、人参皂苷Rh_(2) 20 mg、PTX 2.200 mg、DC-Chol5 mg,总处方量5 mL,紫杉醇的平均包封率为(93.800±0.006)%。紫杉醇阳离子脂质体和Men-PCLPs能明显抑制C6细胞的生长,且Men-PCLPs对C6细胞和bEnd.3细胞的靶向性显著增强。结论 优化后的Men-PCLPs具有较好的主动靶向性,对C6细胞有一定的抑制作用。

Objective To prepare menthol-modified paclitaxel cationic liposomes(Men-PCLPs),and optimize the formulation and evaluate Men-PCLPs targeting ability in vitro.Methods Men-PCLPs were prepared by thin film dispersion method.The Box-Benhken response surface method was used to select the optimal formulation process of Men-PCLPs.To evaluate the effect of liposome on the survival rate of C6 cells.The uptake of different liposomes by C6 and bEnd.3 cells was determined by flow cytometry.Results The optimal liposome prescription was phospholipid 106 mg,ginsenoside Rh_(2) 20 mg,PTX 2.200 mg,DC-Chol 5 mg,the total prescription volume was 5 mL.The average encapsulation rate of paclitaxel was(93.800 ± 0.006) %.Paclitaxel cationic liposomes and Men-PCLPs inhibited the growth of C6 cells.Moreover,the targeting of MenPCLPs to C6 cells and bEnd.3 cells was significantly enhanced.Conclusion The optimized Men-PCLPs show good active targeting,which has certain inhibitory effect on C6 cells.