TY - JOUR
T1 - Reduced UV-induced degradation of doxorubicin encapsulated in polyethyleneglycol-coated liposomes
AU - Bandak, Suzan
AU - Ramu, Avner
AU - Barenholz, Yechezkel
AU - Gabizon, Alberto
PY - 1999
Y1 - 1999
N2 - Purpose. The aim of this study was to investigate the stability of doxurubicin encapsulated in polyethyleneglycol-coated liposomes (Doxil(TM)) under UV-A light. Methods. High performance liquid chromatography and a fluorimetric method were used to quantify doxorubicin in bulk solution and doxorubicin in Doxil formulation. Results. The photodegradation of Doxil was significantly lower in comparison to the photodegradation of the free drug and showed no concentration dependency at the measured concentration range of 5-50 μg/ml. During and after UV-A irradiation, there was no leakage of the drug from liposomes to the medium. After induced leakage of doxorubicin from the liposomes by the ionophore nigericin, the degradation kinetics of Doxil were identical to that of free doxorubicin. Conclusions. High intraliposomal doxorubicin concentration and intraliposomal acidic pH are the two critical factors that protect DXR in Doxil from UV-A degradation.
AB - Purpose. The aim of this study was to investigate the stability of doxurubicin encapsulated in polyethyleneglycol-coated liposomes (Doxil(TM)) under UV-A light. Methods. High performance liquid chromatography and a fluorimetric method were used to quantify doxorubicin in bulk solution and doxorubicin in Doxil formulation. Results. The photodegradation of Doxil was significantly lower in comparison to the photodegradation of the free drug and showed no concentration dependency at the measured concentration range of 5-50 μg/ml. During and after UV-A irradiation, there was no leakage of the drug from liposomes to the medium. After induced leakage of doxorubicin from the liposomes by the ionophore nigericin, the degradation kinetics of Doxil were identical to that of free doxorubicin. Conclusions. High intraliposomal doxorubicin concentration and intraliposomal acidic pH are the two critical factors that protect DXR in Doxil from UV-A degradation.
KW - Doxorubicin
KW - Liposomes
KW - Photodegradation
KW - UV-A light
UR - http://www.scopus.com/inward/record.url?scp=0032980270&partnerID=8YFLogxK
U2 - 10.1023/A:1018869818282
DO - 10.1023/A:1018869818282
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C2 - 10397603
AN - SCOPUS:0032980270
SN - 0724-8741
VL - 16
SP - 841
EP - 846
JO - Pharmaceutical Research
JF - Pharmaceutical Research
IS - 6
ER -