Polymeric micelles based on amphiphilic scorpion-like macromolecules: novel carriers for water-insoluble drugs.
OBJECTIVE
The objective was to evaluate amphiphilic scorpion-like macromolecules (AScMs) as drug carriers for hydrophobic drugs.


METHODS
Indomethacin (IMC) was incorporated into two AScM micelles (M12P5 and M12P2) by the O/W emulsion technique. The influences of IMC:polymer feed ratio and molecular weight of the hydrophilic block of AScMs on the micelle size, IMC entrapment efficiency and release behavior were investigated. Furthermore, cytotoxicity of the AScMs was evaluated with human umbilical vein endothelial cells (HUVEC).


RESULTS
The maximal IMC entrapment efficiency in M12P5 and M12P2 micelles (72.3 and 20.2%, respectively) was obtained at ratios of 0.1 to 1 for indomethacin:polymer. The sizes of IMC-loaded M12P5 and Mi2P2 polymeric micelles were <20 nm with a narrow size distribution. In vitro release studies revealed that IMC released from MI2P5 and M12P2 polymeric micelles showed sustained release behavior during the 24 h of experiment. Additionally, M12P5 and M12P2 polymeric micelles did not induce remarkable cytotoxicity against HUVEC cells at concentrations up to 1 and 0.5 mM, respectively.


CONCLUSIONS
The amphiphilic scorpion-like macromolecules may be useful as novel drug carriers because of their small size, ability to encapsulate hydrophobic drugs and release them in a sustained manner as well as low cytotoxicity.
Djordjevic
Jelena
J
Department of Pharmaceutics, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, New Jersey 08854, USA.
Barch
Maryan
M
Uhrich
Kathryn E
KE
D002460:Cell Line; D004337:Drug Carriers / Q000008:administration & dosage / Q000378:metabolism*; D042783:Endothelial Cells / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D046911:Macromolecular Substances / Q000008:administration & dosage / Q000378:metabolism; D008823:Micelles; D004364:Pharmaceutical Preparations / Q000008:administration & dosage / Q000378:metabolism; D011108:Polymers / Q000008:administration & dosage / Q000378:metabolism*; D012995:Solubility / Q000187:drug effects; D013501:Surface-Active Agents / Q000008:administration & dosage / Q000378:metabolism*
D004337:Drug Carriers; D046911:Macromolecular Substances; D008823:Micelles; D004364:Pharmaceutical Preparations; D011108:Polymers; D013501:Surface-Active Agents