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Polymeric Micelles Based on Amphiphilic Scorpion-like Macromolecules: Novel Carriers for Water-Insoluble Drugs

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Purpose.

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 M12P2 polymeric micelles were <20 nm with a narrow size distribution. In vitro release studies revealed that IMC released from M12P5 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.

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Abbreviations

AScMs:

amphiphilic scorpion-like macromolecules

DLS:

dynamic light scattering

DMF:

N,N-dimethylformamide

ECGS:

endothelial cell growth supplement

FBS:

fetal bovine serum

HUVEC:

human umbilical vein endothelial cells

IMC:

indomethacin

IMC-M12P5:

indomethacin-loaded M12P5 micelles

IMC-M12P2:

indomethacin-loaded M12P2 micelles

M12P5:

poly(ethylene glycol-5000)—mucic acid based amphiphilic scorpion-like macromolecules

M12P2:

poly(ethylene glycol-2000)—mucic acid based amphiphilic scorpion-like macromolecules

MTT:

3-(4,5-dimethyl-thiazol-2-yl)-2,5-diphenyl tetrazolium bromide

PEG:

poly(ethylene glycol)

PTFE:

polytetrafluoroethylene

TEM:

transmission electron microscopy

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Authors and Affiliations

  1. Department of Pharmaceutics, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, Piscataway, New Jersey, 08854, USA

    Jelena Djordjevic & Kathryn E. Uhrich

  2. Department of Chemistry and Chemical Biology, Rutgers, The State University of New Jersey, Piscataway, New Jersey, 08854, USA

    Maryan Barch & Kathryn E. Uhrich

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  1. Jelena Djordjevic
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  3. Kathryn E. Uhrich
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Correspondence to Kathryn E. Uhrich.

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Djordjevic, J., Barch, M. & Uhrich, K. Polymeric Micelles Based on Amphiphilic Scorpion-like Macromolecules: Novel Carriers for Water-Insoluble Drugs. Pharm Res 22, 24–32 (2005). https://doi.org/10.1007/s11095-004-9005-3

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