THERMOSENSITIVE LIPOSOMES CONTAINING DOXORUBICIN. PREPARATION AND IN VITRO EVALUATION.
MARCELA ACHIM^1*, CĂLIN PRECUP², DANIEL GONGANĂUNIŢU
², LUCIAN BARBU-TUDORAN³, ALINA SILVIA PORFIRE¹,
RĂZVAN SCURTU², CONSTANTIN CIUCE²
1Department of Pharmaceutical Technology and Biopharmaceutics,
Faculty of Pharmacy
2No.I Surgery Department, Faculty of Medicine, "Iuliu Hatieganu"
University, 8 V.Babes, 400012Cluj-Napoca, Romania
3Electron Microscopy Center, Faculty of Biology & Geology, "Babes-Bolyai"
University of Cluj-Napoca, 5-7 Clinicilor, 400006 Cluj-Napoca, Romania
*corresponding author: machim@umfcluj.ro
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Abstract:

This work describes doxorubicin (DOX)-loaded thermosensitive liposomes (TSL) preparation and in vitro evaluation.
TSL were based on dipalmitoylphosphatidylcholine (DPPC): distearoylphosphatidylcholine (DSPC): cholesterol (CHOL) molar ratio 26:4:6; lyso-thermosensitive liposomes (LTSL) based on 1-palmitoyl-2-hydroxy-3-glicerophosphatidylcholine:DPPC:DSPC:CHOL 2:24:4:6 and non-thermosensitive liposomes (NTSL) based on L-α-phosphatidylcholine: CHOL, 30:6. Liposomes were prepared by lipid film hydration and extrusion method and characterized with respect to DOX loading, entrapment efficiency, size, morphology and in vitro DOX release. DOX entrapment efficiency was low, especially for TSL and LTSL (5.6 – 5.6%) and higher for NTSL. Examined using transmission electron microscopy liposomes have a mean diameter of 246 nm (44.3% polydispersity index). Drug release from liposomes was performed at a temperature above the phase transition temperature, possible in conditions of a local controlled hyperthermia (41-42^oC). In vitro DOX release study showed that TSL and LTSL in 15 min at 42^oC released more DOX (36%, 54% diffused in 5h), compared with NTSL (2% diffused in 5h)..

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