Paclitaxel delivery using carrier made from curcumin derivative: synergism between carrier and the loaded drug for effective cancer treatment.
To fully make use of the synergism between paclitaxel and curcumin (CUR) in cancer treatment, carrier made from CUR derivative was synthesized and used to deliver paclitaxel into cancer cells. The methoxylpolyethylene oxide-linked palmitate-modified curcumin (mPEO-CUR-PA) was synthesized and the obtained amphiphilic mPEO-CUR-PA molecules were allowed to self-assemble into microspheres. In vitro release of free CUR from mPEO-CUR-PA in the presence of lipase was proofed and the ability of cells to endocytose mPEO-CUR-PA microspheres was verified. Cytotoxic activity of the mPEO-CUR-PA microspheres toward cancer cell lines (S102 and A549) was evaluated and compared with that of the unmodified CUR. Paclitaxel was then loaded into the microspheres and the paclitaxel-loaded mPEO-CUR-PA microspheres showed up to fivefold to 44-fold increased in vitro cytotoxicity (in terms of % cell mortality) in susceptible (HCC-S102 and A549) and paclitaxel-resistant (A549RT-eto) cancer cells, respectively, compared with that of free paclitaxel.
Department of Chemistry, Faculty of Science, Chulalongkorn University, Bangkok 10330, Thailand.
Kittima
K
Amornwachirabodee
Khajeelak
K
Chiablaem
Sumrit
S
Wacharasindhu
Kriengsak
K
Lirdprapamongkol
Jisnuson
J
Svasti
Viwat
V
Vchirawongkwin
Supason P
SP
Wanichwecharungruang
D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D045744:Cell Line, Tumor; D003474:Curcumin / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D004357:Drug Synergism; D004705:Endocytosis; D006801:Humans; D008863:Microspheres; D017239:Paclitaxel / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics
D000972:Antineoplastic Agents, Phytogenic; D004337:Drug Carriers; D003474:Curcumin; D017239:Paclitaxel