4.3 Article

Preparation and in vitro evaluation of a folate-linked liposomal curcumin formulation

期刊

JOURNAL OF LIPOSOME RESEARCH
卷 22, 期 2, 页码 110-119

出版社

INFORMA HEALTHCARE
DOI: 10.3109/08982104.2011.627514

关键词

Liposomes; curcumin; folate receptor; tumor targeting

资金

  1. Natural Science Foundation of China [81072596]
  2. Program for New Century Excellent Talents in University [NCET-08-0226]
  3. Fundamental Research Funds for the Central Universities [HUST: M2009044]

向作者/读者索取更多资源

Curcumin (CUR), a plant-derived compound, exhibits versatile antitumor effects. However, its poor hydrophilic property limits its application. To circumvent these drawbacks, we encapsulated CUR in liposomes modified with folic acid for better solubility and enhanced tumor targeting. This novel formulation was prepared by a film-dispersion method and characterized by size, zeta potential, drug-loading efficiency, and physical-condition stability. In vitro, cellular uptake efficiency, cytotoxicity, and apoptosis analysis by flow cytometry were performed to evaluate tumor targeting and killing ability. Results showed that the folate-receptor (FR)-targeted liposomal CUR (F-CUR-L) performed with improved solubility, sufficient stability, and enhanced antitumor activity. Mean diameter, zeta potential, and drug-loading efficiency were 182 nm, -26 mV, and 68%, respectively, and this formulation exhibited stability in storage at 4 C for 1 month. In vitro, FR-positive cells endocytosed more F-CUR-L than nontargeted liposomal CUR (CUR-L); thus, the former induced more cellular proliferation inhibition and higher apoptosis than the latter, and the enhanced targeting could be hindered by 1 mM of free folic acid. Further, KB cells were more sensitive to F-CUR-L, compared to Hela cells. Finally, the two kinds of tumor cells treated with F-CUR-L also showed dose-and time-dependent apoptosis.

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