title: Encapsulation of curcumin within poly(amidoamine) dendrimers for delivery to cancer cells.
abstract: Curcumin has anti-proliferative and pro-apototic properties against a variety of cancer cells in vitro. Unfortunately, the water-insolubility and instability leads to its low bioavailability in vivo tests. Here, we report a general approach to using poly(amidoamine) dendrimer with acetyl terminal groups to encapsulate curcumin(G₅-Ac/Cur) for drug delivery to cancer cells. The solubility, release kinetics, anticancer activity, and apoptotic-related protein expression (Bax and Bcl-2) were investigated in detail. Comparing with curcumin, the water-solubility value of G₅-Ac/Cur increased 200-fold, and the release of curcumin from the complexes was in a sustained manner. G₅-Ac/Cur showed higher anti-proliferative activity against A549 cell lines and had the better effect on the generation of intracellular reactive oxygen species, the mitochondrial membrane potential and cell apoptosis. Furthermore, the ratio of Bax/Bcl-2 was higher in samples treated with G₅-Ac/Cur. The results indicated that the G₅-Ac drug delivery system could improve the solubility and anti-cancer effect of curcumin.
authors.affiliation: Laboratory of Physical Biology, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, 2019 BaoJia Road, Shanghai 201800, China.
authors.forename: Lu
authors.initials: L
authors.lastname: Wang
authors.forename: Xiaoping
authors.initials: X
authors.lastname: Xu
authors.forename: Yi
authors.initials: Y
authors.lastname: Zhang
authors.forename: Yuanqing
authors.initials: Y
authors.lastname: Zhang
authors.forename: Ying
authors.initials: Y
authors.lastname: Zhu
authors.forename: Jiye
authors.initials: J
authors.lastname: Shi
authors.forename: Yanhong
authors.initials: Y
authors.lastname: Sun
authors.forename: Qing
authors.initials: Q
authors.lastname: Huang
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000627:therapeutic use; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical; D003474:Curcumin / Q000008:administration & dosage / Q000737:chemistry* / Q000627:therapeutic use; D050091:Dendrimers / Q000737:chemistry*; D004337:Drug Carriers; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy*
chemical_list: D000970:Antineoplastic Agents; D050091:Dendrimers; D004337:Drug Carriers; C104700:PAMAM Starburst; D003474:Curcumin