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Preparation and Evaluation of Temperature Sensitive Liposomes Containing Adriamycin and Cytarabine

Kim, Chong-Kook    (College of Pharmacy, Seoul National University   ); Lee, Suk-Kyeong    (College of Pharmacy, Seoul National University   ); Lee, Beom-Jin    (College of Pharmacy, Seoul National University  );
  • 초록

    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 TEX>$4^\circ{C}$ . From the fact that the release profiles of ADM from freshly prepared TSL and stored TSL for 1 week at TEX>$4^\circ{C}$ was not changed, the TSL was considered to be stable for at least 1 week at TEX>$4^\circ{C}$ . Based on these findings, TSL may be useful to deliver drugs to preheated target sites due to its thermal behaviors.


  • 주제어

    Temperature sensitive liposomes .   Adriamycin .   Cytarabine .   Human serum albumin .   Encapsulation efficiency .   Thermal behavior .   Drug release.  

 저자의 다른 논문

  • Kim, Chong-Kook (109)

    1. 1979 "Riboflavin과 Orotic Acid Derivative와의 분자간 상호작용" 약학회지 = Yakhak hoeji 23 (2): 63~68    
    2. 1980 "Mathematical Description of the Volume of Distribution in the Isolated Organ" 藥劑學會誌 = Journal of Korean pharmaceutical sciences 10 (1): 1~3    
    3. 1980 "Mathematical description of drug distribution in the isolated organ" Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 3 (1): 13~16    
    4. 1981 "Ibuprofenlysine binding to human and bovine serum albumin using a fluorescence probe technique" Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 4 (1): 19~24    
    5. 1981 "Interaction of flavins and some alcohols on the molecular level" Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 4 (1): 43~51    
    6. 1981 "Drug-biomacromolecule interaction 1" Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 4 (2): 99~107    
    7. 1981 "고체상태에서 Ampicillin Trihydrate의 안정성에 관한 연구" 약학회지 = Yakhak hoeji 25 (1): 37~42    
    8. 1981 "약물과 생체고분자간의 상호작용(II) Difference Spectra에 의한 Cephalothin 및 Cefazoline과 Human Serum Albumin의 결합에 관한 연구" 약학회지 = Yakhak hoeji 25 (4): 161~165    
    9. 1982 "오메가 아미노산(酸) 유도체(誘導體)의 분자구조(分子構造)에 관(關)한 연구(硏究)" 藥劑學會誌 = Journal of Korean pharmaceutical sciences 12 (3): 64~73    
    10. 1982 "약물과 생체 고분자간의 상호작용(III) 형광측정법에 의한 1-Anilinonaphthalene-8-sulfonate와 Bovine Serum Albumin간의 결합에 관한 연구" 약학회지 = Yakhak hoeji 26 (2): 85~90    

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