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Open Access Green as soon as Postprint is submitted to ZB.
Gemcitabine treatment of rat soft tissue sarcoma with phosphatidyldiglycerol-based thermosensitive liposomes.
Pharm. Res. 31, 2276-2286 (2014)
The pyrimidine analogue gemcitabine (dFdC) is frequently used in the treatment of patients with solid tumors. However, after i.v. application dFdC is rapidly inactivated by metabolization. Here, the potential of thermosensitive liposomes based on 1,2-dipalmitoyl-sn-glycero-3-phosphodiglycerol (DPPG(2)-TSL) were investigated as carrier and targeting system for delivery of dFdC in combination with local hyperthermia (HT). DPPG(2)-TSL were prepared by the lipid film hydration and extrusion method and characterized by dynamic light scattering, thin layer chromatography, phosphate assay and HPLC. In vivo experiments were performed in Brown Norway rats with a syngeneic soft tissue sarcoma. Local HT treatment was performed by light exposure. DPPG(2)-TSL were stable at 37A degrees C in serum and showed a temperature dependent dFdC release > 40A degrees C. Plasma half-life of dFdC was strongly increased from 0.07 h (non-liposomal) to 0.53 h (liposomal, vesicle size 105 nm) or 2.59 h (liposomal, 129 nm). Therapy of BN175 tumors with dFdC encapsulated in DPPG(2)-TSL + HT showed significant improvement in tumor growth delay compared to non-liposomal dFdC without HT (p < 0.05), non-liposomal dFdC with HT (p < 0.01), and liposomal dFdC without HT (p < 0.05), respectively. Gemcitabine encapsulated in DPPG(2)-TSL in combination with local HT is a promising tool for the treatment of solid tumors. Therefore, these encouraging results ask for further investigation and evaluation.
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Publication type
Article: Journal article
Document type
Scientific Article
Keywords
Drug Delivery ; Gemcitabine ; Hyperthermia ; Phosphatidyloligoglycerol ; Thermosensitive Liposomes; Randomized Phase-ii; Temperature-sensitive Liposomes; Content Release; Drug-release; 2,2-difluorodeoxycytidine Gemcitabine; Cellular Pharmacology; Pancreatic-cancer; Solid Tumors; Dose-rate; In-vitro
ISSN (print) / ISBN
0724-8741
e-ISSN
1573-904X
Journal
Pharmaceutical Research
Quellenangaben
Volume: 31,
Issue: 9,
Pages: 2276-2286
Publisher
Springer
Publishing Place
New York
Non-patent literature
Publications
Reviewing status
Peer reviewed
Institute(s)
Institute of Molecular Immunology (IMI)