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优化多西紫杉醇在脂质体中的载药条件：为转移性乳腺癌化疗提出潜在产品。

Optimization of Docetaxel Loading Conditions in Liposomes: proposing potential products for metastatic breast carcinoma chemotherapy.

机构信息

Department of Medical Nanotechnology, School of Advanced Technologies in Medicine, Tehran University of Medical Sciences, Tehran, Iran.

Department of Pharmacology, School of Medicine, Tehran University of Medical Sciences, Tehran, Iran.

出版信息

Sci Rep. 2020 Mar 27;10(1):5569. doi: 10.1038/s41598-020-62501-1.

DOI:10.1038/s41598-020-62501-1
PMID:32221371
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7101339/
Abstract

Docetaxel (DTX) was loaded in nanoliposomes based on a new remote loading method using mannitol and acetic acid as hydration buffer. DTX loading conditions were optimized, and the final formulations were prepared according to the best parameters which were HSPC/mPEG2000-DSPE/Chol (F1), HSPC/mPEG2000-DSPE/DPPG/Chol (F2), HSPC/mPEG2000-DSPE/DSPG/Chol (F3), at molar ratios of 85/5/10, 80/5/5/10, 80/5/5/10, respectively. DTX-liposomes were found of desired size (~115 nm) and homogeneity (PDI ≤ 0.2), high drug encapsulation efficacy (34-67%) and DTX concentration, and favorable stability. Passive loaded counterparts liposomes showed three times lower encapsulation efficacy compared to the remote loaded liposomes. The drug release of remote loaded liposomes in plasma 50% was significantly more controlled and less in comparison with their passive loaded counterparts (p < 0.0001). The IC50 values of formulations were determined on MCF-7, 4T1, TUBO, NIH/3T3 cell lines. The biodistribution of iodinated docetaxel as free or liposomal form exhibited significantly greater accumulation of DTX-liposomes in tumors than that of free docetaxel due to the EPR effect. In vivo experiment with BALB/c mice bearing 4T1 or TUBO breast carcinoma tumors also showed that DTX-liposomes could significantly delay tumor growth and prolonged the survival time in comparison with control and Taxotere groups at the similar dose of 8 mg/kg. F1 and F2 formulations were stable and showed good anti-tumor activity and merit further investigation.

摘要

多西他赛（DTX）被载入基于甘露醇和乙酸作为水合缓冲液的新型远程载入方法的纳米脂质体中。对 DTX 载入条件进行了优化，并根据最佳参数（摩尔比分别为 85/5/10、80/5/5/10、80/5/5/10 的 HSPC/mPEG2000-DSPE/Chol（F1）、HSPC/mPEG2000-DSPE/DPPG/Chol（F2）、HSPC/mPEG2000-DSPE/DSPG/Chol（F3））制备了最终配方。载药脂质体具有理想的粒径（~115nm）和均一性（PDI≤0.2）、高药物包封效率（34-67%）和 DTX 浓度以及良好的稳定性。与被动载入脂质体相比，远程载入脂质体的药物释放具有更高的 50%血浆控释能力（p<0.0001）。对 MCF-7、4T1、TUBO、NIH/3T3 细胞系进行了制剂的 IC50 值测定。游离或脂质体形式的碘代多西他赛的生物分布显示，由于 EPR 效应，载药脂质体在肿瘤中的积累明显大于游离多西他赛。荷 4T1 或 TUBO 乳腺癌肿瘤的 BALB/c 小鼠体内实验也表明，与对照组和 Taxotere 组相比，在 8mg/kg 相似剂量下，DTX 脂质体能够显著延缓肿瘤生长并延长生存时间。F1 和 F2 制剂稳定，表现出良好的抗肿瘤活性，值得进一步研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e67/7101339/b40c2fd28c8f/41598_2020_62501_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e67/7101339/d52b223b865b/41598_2020_62501_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e67/7101339/56210677ac41/41598_2020_62501_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e67/7101339/c7333f15afdb/41598_2020_62501_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e67/7101339/d34b2afde311/41598_2020_62501_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e67/7101339/4fb24e69f705/41598_2020_62501_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e67/7101339/1198e7d1c04c/41598_2020_62501_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e67/7101339/b40c2fd28c8f/41598_2020_62501_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e67/7101339/d52b223b865b/41598_2020_62501_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e67/7101339/56210677ac41/41598_2020_62501_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e67/7101339/c7333f15afdb/41598_2020_62501_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e67/7101339/d34b2afde311/41598_2020_62501_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e67/7101339/4fb24e69f705/41598_2020_62501_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e67/7101339/1198e7d1c04c/41598_2020_62501_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/0e67/7101339/b40c2fd28c8f/41598_2020_62501_Fig7_HTML.jpg

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