Characterization and pharmacokinetics of a novel pirarubicin liposome powder

Cong, W. , Liu, Q., Chen, X., Gao, R., Lu, J., Wang, Y. and Luo, G. (2010) Characterization and pharmacokinetics of a novel pirarubicin liposome powder. Drug Development and Industrial Pharmacy, 36(10), pp. 1186-1194. (doi: 10.3109/03639041003695097) (PMID:20515395)

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Abstract

Background: Pirarubicin (THP), an analogue of doxorubicin, has exhibited promising activities against acute leukemia, malignant lymphoma, and several solid tumors. However, the cumulative cardiotoxicity limits its wide application in chemotherapy. Method: To provide an alternative strategy for reducing the cardiotoxicity, a novel THP liposome powder (L-THP), comprising distearoylphosphatidylcholine, distearoylphosphatidylglycerol, cholesterol, and lactose was appropriately prepared based on the physicochemical properties of THP. And L-THP was characterized and evaluated. Comparative studies on pharmacokinetic and biodistribution behaviors between L-THP and commercialized THP injection were performed in normal mice through intravenous administration. Results: When L-THP was reconstituted in a proper amount of normal saline for injection, it had a mean diameter of around 220.0 nm, a zeta potential of about −33.0 mV, and a high THP entrapment efficiency of more than 93.1%. Pharmacokinetics study showed that heart accumulation of THP could be reduced by 81.2% for L-THP. Conclusion: These results suggest that our L-THP might greatly reduce the cardiotoxicity, thus improving the therapeutic index of THP. Meanwhile, further preclinical studies are warranted to define the cardiotoxicity and the therapeutic efficacy of L-THP.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Cong, Dr Wenjuan
Authors: Cong, W., Liu, Q., Chen, X., Gao, R., Lu, J., Wang, Y., and Luo, G.
College/School:College of Medical Veterinary and Life Sciences > School of Medicine, Dentistry & Nursing
Journal Name:Drug Development and Industrial Pharmacy
Publisher:Taylor & Francis
ISSN:0363-9045
ISSN (Online):1520-5762
Published Online:01 June 2010

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