title: Liposomes assembled from a dual drug-tailed phospholipid for cancer therapy.
abstract: We report a novel dual drug-tailed phospholipid which can form liposomes as a combination of prodrug and drug carrier. An amphiphilic dual chlorambucil-tailed phospholipid (DCTP) was synthesized by a straightforward esterification. With two chlorambucil molecules as hydrophobic tails and one glycerophosphatidylcholine molecule as a hydrophilic head, the DCTP, a phospholipid prodrug, undergoes assembly to form a liposome without any additives by the thin lipid film technique. The DCTP liposomes, as an effective carrier of chlorambucil, exhibited a very high loading capacity and excellent stability. The liposomes had higher cytotoxic effects to cancer cell lines than free DCTP and chlorambucil. The in vivo antitumor activity assessment indicated that the DCTP liposomes could inhibit the tumor growth effectively. This novel strategy of dual drug-tailed phospholipid liposomes may be also applicable to other hydrophobic anticancer drugs which have great potential in cancer therapy.
authors.affiliation: School of Chemistry and Chemical Engineering, Southeast University, Nanjing 210096 (P.R. China).
authors.forename: Shuo
authors.initials: S
authors.lastname: Fang
authors.forename: Yuge
authors.initials: Y
authors.lastname: Niu
authors.forename: Wenjun
authors.initials: W
authors.lastname: Zhu
authors.forename: Yemin
authors.initials: Y
authors.lastname: Zhang
authors.forename: Liangli
authors.initials: L
authors.lastname: Yu
authors.forename: Xinsong
authors.initials: X
authors.lastname: Li
keywords: antitumor activity; cancer; chlorambucil; drug delivery; dual drug-tailed phospholipid; liposomes