Development and characterization of miltefosine-loaded polymeric micelles for cancer treatment

作者：Valenzuela Oses Johanna K; Garcia Monica C; Feitosa Valker A; Pachioni Vasconcelos Juliana A; Gomes Filho Sandro M; Lourenco Felipe R; Cerize Natalia N P; Basseres Daniela S; Rangel Yagui Carlota O^*

来源：Materials Science & Engineering C-Materials for Biological Applications, 2017, 81: 327-333.

DOI：10.1016/j.msec.2017.07.040

• Alkylphosphocholines
• Miltefosine
• Block-copolymer
• Polymeric micelles
• Cancer therapy
• Hemolytic potential

Miltefosine presents antineoplastic activity but high hemolytic potential. Its use in cancer has been limited to treating cutaneous metastasis of breast cancer. To decrease hemolytic potential, we developed a formulation of miltefosine-loaded polymeric micelles (PM) of the copolymer Pluronic-F127. A central composite design was applied and the analysis of variance showed that the optimum level of hydrodynamic diameter and poly-dispersity index predicted by the model and experimentally confirmed were 29 nm and 0.105, respectively. Thermal analyses confirmed that miltefosine was molecularly dispersed within PM. Pluronic-F127 PM with miltefosine 80 mu M presented a significant reduction of hemolytic effect (80%, p < 0.05) in comparison to free drug. In vitro assays against HeLa carcinoma cells demonstrated similar cytotoxicity to free miltefosine and PM. Our results suggest that, by lowering hemolytic potential, miltefosine-loaded Pluronic-F127 PM a promising alternative to broaden this drug use in cancer therapy, as well as of other alkylphosphocholines.

• 出版日期2017-12-1