Key result
A pH-sensitive pullulan-doxorubicin conjugate caused 0% hemolysis at 250 mg/L compared to 8.38% with free doxorubicin, while demonstrating lower cardiotoxicity and comparable antitumor efficacy.
Why the study?
Does a pH-sensitive pullulan-doxorubicin conjugate reduce cardiotoxicity and improve biosafety compared to free doxorubicin in an in vivo tumor model?
Does a pH-sensitive pullulan-doxorubicin conjugate reduce cardiotoxicity and improve biosafety compared to free doxorubicin in an in vivo tumor model?
A novel pH-sensitive pullulan-doxorubicin conjugate maintains antitumor efficacy while significantly reducing the cardiotoxicity associated with free doxorubicin in vivo.
Answers are grounded in this paper and cite their sources.
Supports development of pH-sensitive doxorubicin conjugates to lower cardiotoxicity; leaves open translation from animal models to patients.
A pH‐sensitive pullulan–doxorubicin conjugate is evaluated in vivo by comparison with doxorubicin with respect to hemolytic activity, biodistribution, biosafety, cardiotoxicity and antitumor effects. Hemolytic studies show that doxorubicin caused 8.38% hemolysis at 250 mg L−1, while no hemolysis is observed with pullulan–doxorubicin conjugate at the same drug concentration. The circulation time of pullulan–doxorubicin conjugate is relatively longer than that of doxorubicin, and the concentration in tumors for pullulan–doxorubicin conjugate increases to about double that of doxorubicin within 240 min after injection of drugs via the lateral vein. In vivo safety research shows that pullulan–doxorubicin conjugate shows better biosafety than free doxorubicin, confirmed by acute toxicity, systemic toxicity and histopathological observations. The cardiotoxicity of pullulan–doxorubicin conjugate is much lower than that of free doxorubicin, as confirmed by TEM and ECG. In vivo antitumor activity assays show that the pullulan–doxorubicin conjugate has an antitumor efficacy comparable to that of doxorubicin.
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Lu et al. (2010) studied Tumors. pH-sensitive pullulan-doxorubicin conjugate vs. doxorubicin was evaluated on Hemolysis at 250 mg L-1. A pH-sensitive pullulan-doxorubicin conjugate caused 0% hemolysis at 250 mg/L compared to 8.38% with free doxorubicin, while demonstrating lower cardiotoxicity and comparable antitumor efficacy.
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