Alteration in the Temperature-Dependent Content Release Property of Thermosensitive Liposomes in a Plasma

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The effect of plasma components on the temperature-dependent content release property of thermosensitive liposomes has been described. Temperature-sensitive liposomes containing mitomycin C (MMC) were prepared from dipalmitoylphosphatidylcholine (DPPC liposomes) and a 7:3 mixture of DPPC and dipalmitoylophos-phatidylglycerol (DPPC/DPPG liposomes). We defined in this study the difference in the content release between 38℃ and 44℃ as an index of the temperature-dependent content release efficiency (Δ% release). In the absence of rat plasma, the Δ% release of the DPPC liposomes and the DPPC/DPPG liposomes was 83% and 71%, respectively. However, when the release study was conducted with rat plasma, the Δ% release increased to about 96% for both liposomes. In addition, while the DPPC liposomes were destabilized by rat plasma below the gel-to-liquid crystalline phase transition temperature (T_m), MMC leakage from the DPPC/DPPG liposomes below T_m was suppressed by rat plasma. Moreover, the plasma protein binding onto lipid bilayer was concomitant with the gel-to-liquid crystalline phase transition and then enhanced the temperature-dependent release from the DPPC/DPPG liposomes. The possible mechanism of interaction between liposomes and plasma proteins, especially serum albumin, was discussed based on differential scanning calorimetry and protein binding experiments.
公益社団法人日本薬学会の論文
2003-11-01