载有顺铂的固体脂质纳米颗粒的制备，表征和体内分布。,Die Pharmazie

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载有顺铂的固体脂质纳米颗粒的制备，表征和体内分布。
Die Pharmazie Pub Date : 2008-09-06
Jie Tian ₁ , Xiujuan Pang , Kefu Yu , Linjie Liu , Jun Zhou

Affiliation

采用乳化分散-超声法制备载有顺铂的固体脂质纳米粒（SLN）。将传统的抗肿瘤药物顺铂（CDDP）掺入SLN中，以获得靶向性和毒性较小的药物递送系统。CDDP-SLN在透射电子显微镜（TEM）摄影中呈球形且均匀。平均粒径和ζ电位分别为121 +/- 15nm和-46.4 +/- 10.3mV。此外，采用了一种新型的阳离子交换树脂方法来研究SLN的封装效率（EE％）。该方法基于药物与树脂之间阳离子交换的原理，最佳配方的EE％为82.3％。体外释放曲线表明，与其他释放介质相比，CDDP在生理盐水（NS）中有效而完全地从SLN释放。建立了柱前衍生HPLC方法用于体内顺铂测定。静脉给药8 mg mL（-1）CDDP-SLN和顺铂NS后，在雄性大鼠中进行了组织分布研究，结果发现CDDP-SLN对肝脏具有靶向作用，并且在肝脏中浓度较低。大鼠肾脏。这些结果表明，乳化分散-超声是制备CDDP-SLN的简单，简便，有效的方法，而阳离子交换树脂法是评价CDDP-SLN EE％的可行且合适的方法。通过这种方法制备的CDDP-SLN被证明是一种靶向且毒性较小的药物递送系统。建立了柱前衍生HPLC方法用于体内顺铂测定。静脉给药8 mg mL（-1）CDDP-SLN和顺铂NS后，在雄性大鼠中进行了组织分布研究，结果发现CDDP-SLN对肝脏具有靶向作用，并且在肝脏中浓度较低。大鼠肾脏。这些结果表明，乳化分散-超声是制备CDDP-SLN的简单，简便，有效的方法，而阳离子交换树脂法是评价CDDP-SLN EE％的可行且合适的方法。通过这种方法制备的CDDP-SLN被证明是一种靶向且毒性较小的药物递送系统。建立了柱前衍生HPLC方法用于体内顺铂测定。静脉给药8 mg mL（-1）CDDP-SLN和顺铂NS后，在雄性大鼠中进行了组织分布研究，结果发现CDDP-SLN对肝脏具有靶向作用，并且在肝脏中浓度较低。大鼠肾脏。这些结果表明，乳化分散-超声是制备CDDP-SLN的简单，简便，有效的方法，而阳离子交换树脂法是评价CDDP-SLN EE％的可行且合适的方法。通过这种方法制备的CDDP-SLN被证明是一种靶向且毒性较小的药物递送系统。并且发现CDDP-SLN对大鼠具有靶向作用，并且对肾脏具有低浓度。这些结果表明，乳化分散-超声是制备CDDP-SLN的简单，简便，有效的方法，而阳离子交换树脂法是评价CDDP-SLN EE％的可行且合适的方法。通过这种方法制备的CDDP-SLN被证明是一种靶向且毒性较小的药物递送系统。并且发现CDDP-SLN对大鼠具有靶向作用，并且对肾脏具有低浓度。这些结果表明，乳化分散-超声是制备CDDP-SLN的简单，简便，有效的方法，而阳离子交换树脂法是评价CDDP-SLN EE％的可行且合适的方法。通过这种方法制备的CDDP-SLN被证明是一种靶向且毒性较小的药物递送系统。

"点击查看英文标题和摘要"

Preparation, characterization and in vivo distribution of solid lipid nanoparticles loaded with cisplatin.

An emulsification dispersion-ultrasonication method was employed to prepare solid lipid nanoparticles (SLN) loaded with cisplatin. The conventional antitumor drug cisplatin (CDDP) was incorporated into SLN to obtain a targeted and less toxic drug delivery system. The CDDP-SLNs were spherical and uniform in transmission electron microscopy (TEM) photography. The mean particle size and zeta potential were 121 +/- 15 nm, and -46.4 +/- 10.3 mV, respectively. Also, a novel cation exchange resin method was adopted to investigate the encapsulation efficiency (EE%) of the SLN. This method is based on the principle of cation exchange between drugs and resins, and the EE% of the optimal formulation was 82.3%. The in vitro release profile revealed that CDDP was released from SLN efficiently and completely in normal saline (NS) compared with other release media. A pre-column derivatization HPLC method was established for in vivo assay of cisplatin. A tissue distribution study was conducted in male rats after iv administration of 8 mg mL(-1) CDDP-SLN and cisplatin NS, and it was found that CDDP-SLN has a targeted effect to the liver as well as a low concentration in the kidney in rats. These results indicated that emulsification dispersion-ultrasonication is a simple, easy, available and effective method for preparing CDDP-SLN, and the cation exchange resin method is a feasible and suitable method to evaluate the EE% of CDDP-SLN. CDDP-SLN prepared by this method was proved to be a targeted and less toxic drug delivery system.

更新日期：2019-11-01

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