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目的:表征叶酸受体介导pH敏感型分子靶向阿霉素脂质体,建立RP-HPLC法进行含量测定。方法:采用动态光散射法测定脂质体的粒径;采用液相色谱法开展含量测定的方法学研究与验证。选用Agilent HC-C18色谱柱(250 mm×4.6 mm,5μm),流动相为1.23%醋酸钠水溶液(用冰醋酸调pH至3.3)-甲醇(55∶45),等度洗脱,流速为1.0 mL.min-1,检测波长233 nm,柱温30℃。结果:自制的新型脂质体粒径(120±20)nm(PDI<0.200),包封率不小于91.0%。建立的RP-HPLC法中,自制脂质体的辅料对主峰无干扰,且各杂质峰与主成分峰均能达到基线分离,检测限为0.2 ng(S/N=3),定量限为1.0 ng(S/N=10),主成分的浓度在1.0～40.0μg.mL-1范围内线性良好(r=0.9991)。结论:本文所建方法简便易行,专属性强,灵敏,耐用性好,适于本脂质体中阿霉素的含量测定。
OBJECTIVE: To characterize the folate receptor-mediated pH-sensitive molecule targeting doxorubicin liposomes and establish RP-HPLC method. Methods: The particle size of liposomes was determined by dynamic light scattering method. The methodological study and verification of determination by HPLC were carried out. The mobile phase consisted of 1.23% sodium acetate solution (adjusted to pH 3.3 with glacial acetic acid) -methanol (55:45) using an Agilent HC-C18 column (250 mm × 4.6 mm, 5 μm) mL.min-1, detection wavelength 233 nm, column temperature 30 ℃. Results: The self-made liposomes had a diameter of (120 ± 20) nm (PDI <0.200) and encapsulation efficiency of no less than 91.0%. The established RP-HPLC method, the self-made liposomes excipients on the main peak without interference, and the impurity peak and the main component peak can be baseline separation, the detection limit of 0.2 ng (S / N = 3), the limit of quantification of 1.0 ng (S / N = 10). The linearity was good (r = 0.9991) in the range of 1.0 ~ 40.0μg.mL-1. Conclusion: The method proposed in this paper is simple and easy to use, with special specificity, sensitivity and durability, and is suitable for the determination of doxorubicin in this liposome.