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包含去氧胆酸钠的脂质体用于六亚甲基三聚氰胺(HMM)口服递送:开发、表征和体内评价。

Liposomes incorporating sodium deoxycholate for hexamethylmelamine (HMM) oral delivery: development, characterization, and in vivo evaluation.

机构信息

Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, PR China.

出版信息

Drug Deliv. 2010 Apr;17(3):164-70. doi: 10.3109/10717541003667764.

Abstract

Liposomes incorporating sodium deoxycholate (NaDC) were prepared by the method of reverse phase evaporation and used for drug delivery by the oral route. Hexamethylmelamine (HMM), an anti-tumor agent, was chosen as a model drug and encapsulated into liposomes incorporating NaDC (NaDC-Lip). Several properties of NaDC-Lip containing HMM (HMM NaDC-Lip), such as particle size, entrapment efficiency, pinacyanol chloride (PIN) spectral characteristics with various molar ratio of NaDC/PC, as well as the vesicle stability measurements with calcein were evaluated. In vivo, the area under the plasma concentration-time curve obtained from the pharmacokinetics study of HMM NaDC-Lip was found to be approximately 9.76- and 1.21-fold higher than that of HMM solution and HMM Lip, respectively, indicating that NaDC-Lip can be used as a potential carrier for oral drug administration.

摘要

采用逆相蒸发法制备了包含去氧胆酸钠(NaDC)的脂质体,并通过口服途径将其用作药物递送载体。选择六甲蜜胺(HMM)作为模型药物,并将其包封于包含 NaDC 的脂质体(NaDC-Lip)中。评估了包含 HMM 的 NaDC-Lip(HMM NaDC-Lip)的几个性质,例如粒径、包封效率、与不同摩尔比的 NaDC/PC 的芘甲川氯(PIN)光谱特征,以及用钙黄绿素进行的囊泡稳定性测量。在体内,从 HMM NaDC-Lip 的药代动力学研究中获得的血浆浓度-时间曲线下面积分别约为 HMM 溶液和 HMM Lip 的 9.76 倍和 1.21 倍,表明 NaDC-Lip 可用作口服药物给药的潜在载体。

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