|
KMID : 0043319930160020129
|
|
Archives of Pharmacal Research
1993 Volume.16 No. 2 p.129 ~ p.133
|
|
|
Preparation and Evaluation of Temperature Sensitive Liposomes Containing Adriamycin and Cytarabine
|
|
Kim Chong-Kook
Lee Suk-Kyeong
Lee Beom-Jin
|
|
|
Abstract
|
|
|
|
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 of TSL was dependent on the lipid compositions of TSL ADM broadened thermogram of TSL but Ara-C did not. However, 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 and observed at for DPPC (Dipalmitoylphosphatidylcholine) only, 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 . However, ADM release from TSL was increased at the near and above . 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.
|
|
|
KEYWORD
|
|
|
Temperature sensitive liposomes, Adriamycin, Cytarabine, Human serum albumin, Encapsulation efficiency, Thermal behavior, Drug release
|
|
|
FullTexts / Linksout information
|
|
|
|
|
|
Listed journal information
|
|
  
|
|