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      • Engineering of multifunctional temperature-sensitive liposomes for synergistic photothermal, photodynamic, and chemotherapeutic effects

        Tran, Tuan Hiep,Nguyen, Hanh Thuy,Le, Nam Van,Tran, Thi Thu Phuong,Lee, Jong Seong,Ku, Sae Kwang,Choi, Han-Gon,Yong, Chul Soon,Kim, Jong Oh Elsevier 2017 International journal of pharmaceutics Vol.528 No.1

        <P><B>Abstract</B></P> <P>Heterogeneity of cancer cells and drug resistance require multiple therapeutic approaches for comprehensive treatment. In this study, temperature-sensitive liposomes containing anti-cancer agent tanespimycin (17-AAG) and photosensitizer IR 820 were developed for combination of phototherapy and chemotherapy. The temperature-sensitive liposomes composed of DPPC, cholesterol, DSPE-PEG, 17-AAG, and IR 820 (LP-AI) at weight ratio of 35/15/3/2/2 were formulated as a thin film using extrusion and evaluated for particle size, morphology and drug release profile. Furthermore, the anticancer effect of combined therapy was examined <I>in vitro</I> and <I>in vivo</I> in SCC-7 and MCF-7 cell lines. As a result, LP-AI was prepared at particle size of 166.7±1.3nm, PDI of 0.153±0.012, and ζ-potential of −32.6±0.8mV. After NIR irradiation (660 and 808nm laser), LP-AI could generate heat and ROS and enhance drug release from nanoparticles which were useful to kill the cancer cells. These were confirmed by <I>in vitro</I> cytotoxicity as well as <I>in vivo</I> effective ablation of tumors. In conclusion, fast drug release and enhanced treatment efficacy of LP-AI indicate the potential of integrating photo- and chemotherapy for synergistic anti-cancer effects.</P> <P><B>Graphical abstract</B></P> <P>Temperature-sensitive liposomes containing anti-cancer agent tanespimycin and photosensitizer IR 820 (LP-AI).</P> <P>[DISPLAY OMISSION]</P>

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        Preparation and Evaluation of Temperature Sensitive Liposomes Containing Adriamycin and Cytarabine

        Kim, Chong-Kook,Lee, Suk-Kyeong,Lee, Beom-Jin The Pharmaceutical Society of Korea 1993 Archives of Pharmacal Research Vol.16 No.2

        Temperature sensitive liposomes(TSL) containing adriamycin (ADM) and cytarabine (Ara-C) were prepared. ADM and Ara-C were selected as model compounds of amphiphilic and hydrophilic drug, respectively. Encapsulation efficiency of ADM entrapped into TSL was about twice greater than that of Ara-C. It might be due to different polarity of the drug, Lipid compositions of TSL had no effect on the encapsulation efficiency of drugs. Thermal behavior of TSL using a differential scanning calorimetry (DSC) was also investigated. Phase transition of TSL using a differential scanning calorimetry (DSC) was also investigated. Phase transition temperature $(T_c)$ of TSL was dependent on the lipid compositions of TSL ADM broadened thermogram of TSL but Ara-C did not. However, $T_c$ of TSL was not changed by any drug. Release rate of drugs was highly dependent on temperature. The release profile of ADM was similar to that of Ara-C. The maximum release rate of drugs from TSL was occurred at the near $T_c$ and observed at $39-41^\circ{C}$ for DPPC (Dipalmitoylphosphatidylcholine) only, $52-54^\circ{C}$ for DPPC and DSPC (1:1), respectively. Effect of human serum alburmin (HAA) on the release rate of ADM was investigated. HSA had no significant effect on the release of ADM below $T_c$. However, ADM release from TSL was increased at the near and above $T_c$. The HSA-induced leakage of drug may result from the interaction of liposomal constituents with HSA structure at the near $4^\circ{C}$. From the fact that the release profiles of ADM from freshly prepared TSL and stored TSL for 1 week at $4^\circ{C}$ was not changed, the TSL was considered to be stable for at least 1 week at $4^\circ{C}$. Based on these findings, TSL may be useful to deliver drugs to preheated target sites due to its thermal behaviors.

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        김진석 숙명여자대학교 약학연구소 2006 약학논문집-숙명여자대학교 Vol.23 No.-

        New temperature-sensitive liposomes, which show a transition temperature around 41°C, were prepared using a differential scanning calorimetry method. Various compositions of phospholipids with or without encapsulated drug were tested and DPPC:DMPC:DSPC (4:1:1 molar ratio) liposome was found to have a transition temperature of 41°C from solid gel state to liquid crystalline state, which might be useful for targeting of anticancer drugs or radio-sensitizers to the tumor or inflammation sites.

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