荧光淬灭法研究热敏脂质体的体外释放行为

Establishment of a Method for Evaluating the Release Behavior of Thermo Sensitive Liposome in vitro

目的 建立一种简单且精确评价热敏脂质体（TSL）体外释放行为的方法.方法 采用薄膜分散法制备钙黄绿素热敏脂质体（CTSL）,利用荧光自淬灭法研究热敏脂质体的体外释放,通过差示扫描量热法测定热敏脂质体的相变温度.结果 制备热敏脂质体能成功包裹高浓度荧光素,被包裹的钙黄绿素能屏蔽自身的发射光.钙黄绿素在0.000 1～0.001 mmol·L-1浓度范围内,荧光强度与浓度之间存在良好的线性关系.CTSL在37和41℃下10 min的释放度分别为0.1％和45.4％.CTSL的相转变温度约为41℃.结论 通过荧光淬灭法研究评价热敏脂质体的热敏释药特性,方法准确、简单、可行.

To establish a simple and accurate method to evaluate the release behavior of thermo sensitiveliposome （TSL）. Methods Calcein thermo sensitive liposome （ CTSL） was prepared by film hydration method, and therelease behavior was measured by fluorescence quenching method. Then the transformation temperture was verified by differentialscanning calorimetry. Results Thermo sensitive liposome with different phospholipids could encapsulate the high concentrationof calcein successfully, and trapped calcein could shield its emitted light. Calcein was in a good linearity among the concentrationsof 10-4 ~10-3 mmol·L-1 . The 10-min release rate at 37 and 41 ℃were 0. 1% and 45. 4%, respectively. The transformationtemperature of CTSL was 41 ℃ Conclusion The simple and accurate method to evaluate thermo sensitive liposome releasebehavior is successfully established based on fluorescence quenching method.