Transferrin-Functionalized Microemulsions Coloaded with Coix Seed Oil and Tripterine Deeply Penetrate To Improve Cervical Cancer Therapy

• Published in: Molecular pharmaceutics Vol. 16; no. 12; pp. 4826 - 4835
• Main Authors: Guo, Mengfei, Qu, Ding, Qin, Yue, Chen, Yunyan, Liu, Yuping, Huang, Mengmeng, Chen, Yan
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 02.12.2019
• Subjects: Animals; Antineoplastic Agents, Phytogenic - pharmacology; Apoptosis - drug effects; Cell Line, Tumor; Cell Proliferation - drug effects; Coix - chemistry; Drug Delivery Systems - methods; Emulsions - pharmacology; Female; HeLa Cells; Humans; Mice; Mice, Inbred BALB C; Mice, Nude; Plant Oils - pharmacology; Seeds - chemistry; Transferrin - pharmacology; Triterpenes - pharmacology; Uterine Cervical Neoplasms - drug therapy; Xenograft Model Antitumor Assays - methods; microemulsions; deep penetration; transferrin; tripterine; coix seed oil; tumor-targeted; cervical cancer
• ISSN: 1543-8384; 1543-8392
• DOI: 10.1021/acs.molpharmaceut.9b00717

Tumor-targeted ligand modification and nanosized coloaded drug delivery systems are promising for cancer therapy. In this study, we showed that coix seed oil and tripterine coloaded microemulsions with a transferrin modification (Tf-CT-MEs) could improve the treatment of cervical cancer. Tf-CT-MEs exhibited good stability in serum and a notably synergistic antiproliferation effect. In the HeLa xenograft tumor-bearing mouse model, Tf-CT-MEs accumulated at tumor sites and penetrated deeply in tumor tissues. Tf-CT-MEs had superior anticancer efficacy in vivo, which greatly slowed the growth of tumors (***p < 0.001 vs saline). We also found that Tf-CT-MEs inhibited tumor cell proliferation, enhanced antiangiogenesis, and induced apoptosis by regulating bax/bcl-2 and the activating caspase-3 pathway. Tf-CT-MEs decreased by 27.7, 26.9, 61.2, and 42.5% of concentrations of TGF-β1, CCL2, TNF-α, and IL-6 in serum, respectively. In addition, Tf-CT-MEs showed little toxicity in vital organs. These results were due to the improved drug delivery efficiency. Collectively, Tf-CT-MEs enhance tumor-targeting, facilitate deep penetration of drugs, and have promising potential as an efficient treatment for cervical cancer.