Preparation and Body Distribution of Freeze-Dried Powder of Ursolic Acid Phospholipid Nanoparticles
Preparation and Body Distribution of Freeze-Dried Powder of Ursolic Acid Phospholipid Nanoparticles
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DOI：
10.1080/03639040802302165
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发表时间：
2009-03
影响因子：
3.4
通讯作者：
Xiao Ju Zhou;Xianming Hu;Yi-Mu Yi-Yi-Mu-Yi-29983129;Jing Wan
中科院分区：
文献类型：
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作者：
Xiao Ju Zhou;Xianming Hu;Yi-Mu Yi-Yi-Mu-Yi-29983129;Jing Wan
熊果酸(UA)是一种难溶的天然三萜化合物。它具有广泛的抗肿瘤活性。我们首次从山楂中提取了它。为了达到较高的生物利用度、靶向效应、稳定性和静脉注射。制备了尿酸磷脂纳米粉(UA-PL-NP)，并对其进行了表征和评价。以大豆磷脂为载体，泊洛沙姆188为乳化剂，采用溶剂乳化-蒸发-超声分散法制备了尿酸纳米粒悬浮液。采用冷冻干燥法制备了UA-PL-NP。静脉注射后观察小鼠体内分布情况。UA-PL-NP和UA控制液(UA-SOL)的给药。采用高效液相色谱法测定包封率和体内尿酸浓度。结果表明，UA-PL-NP的平均粒径为273.8 nm，Zeta电位为−23.2 mV。载药率达86.0%，载药量12.8%。静脉注射后。给予低、中、高剂量UA-PL-NP后，小鼠肝脏中UA浓度明显升高，受试器官中UA浓度在4h时最高，肝脏中UA-PL-NP与血浆AUC0-12比值显著高于UA-Sol，肝脏AUC0-12/UA-Sol比值为8.6。这些结果表明，UA-PL-NP具有良好的肝脏靶向性。行政管理。因此，UA-PL-NP被证明可以作为静脉注射使用。以及亲脂性抗肿瘤三萜的肝靶向系统。
Ursolic acid (UA) is a poor soluble natural triterpenoid. It has a wide variety of antitumor activities. We extracted it from Crataegus pinnatifida for the first time. To achieve a high bioavailability, targeting effect, stability, and an intravenous (i.v.) administration, the UA phospholipid nanopowders (UA-PL-NP) were prepared, characterized, and evaluated. With soybean phospholipid as the carrier and poloxamer 188 as emulsifier, the UA nanoparticle suspension was prepared by solvent emulsification–evaporation and ultrasonic dispersion. The UA-PL-NP was obtained by freeze drying. The body distribution in mice was studied after i.v. administration of UA-PL-NP and an UA control solution (UA-Sol). The entrapment efficiency (EE) and UA concentration in vitro and in vivo were analyzed by high-performance liquid chromatography (HPLC). The results showed that the UA-PL-NP had an average diameter of 273.8 nm with a zeta potential of −23.2 mV. The EE was up to 86.0%, and the drug loading (DL) was 12.8%. After i.v. administration of UA-PL-NP with low, middle and high doses, UA concentration in the livers of mice obviously increased during tested period and was highest in tested organs at 4 h. The AUC0–12 ratio of UA-PL-NP in liver to that in plasma was much higher than that of UA-Sol, and the liver AUC0–12 ratio of UA-PL-NP to UA-Sol was 8.6. These results indicate the UA-PL-NP have a good targeting to the liver after i.v. administration. Therefore, the UA-PL-NP is demonstrated to be available as an i.v. and liver targeting system for lipophilic antitumor triterpenoids.