Integration of phospholipid-drug complex into self-nanoemulsifying drug delivery system to facilitate oral delivery of paclitaxel

论文摘要

Self-nanoemulsifying drug delivery system（SNEDDS） has emerged as a promising platform to improve oral absorption of drugs with poor solubility and low permeability. However,large polarity molecules with insufficient lipid solubility,such as paclitaxel（PTX）,would suffer from inferior formulation of SNEDDS due to poor compatibility. Herein,phospholipid-drug complex（PLDC） and SNEDDS were integrated into one system to facilitate oral delivery of PTX. First,PTX was formulated into PLDC in response to its inferior physicochemical properties. Then,the prepared PLDC was further formulated into SNEDDS by integrating these two drug delivery technologies into one system（PLDC-SNEDDS）. After PLDC-SNEDDS dispersed in aqueous medium,nanoemulsion was formed immediately with an average particle size of 30 nm. Furthermore,the nanomulsion of PLDC-SNEDDS showed good colloidal stability in both HCl solution（0.1 mol/l,p H 1.0） and phosphate buffer solution（PBS,p H 6.8）. In vivo,PTX-PLDC-SNEDDS showed distinct advantages in terms of oral absorption efficiency,with a3.42-fold and 2.13-fold higher bioavailability than PTX-PLDC and PTX solution,respectively.Our results suggest that the integration of PLDC into SNEDDS could be utilized to facilitate the oral delivery of hydrophobic drugs with large polarity.

论文目录

• 1. Introduction
• 2. Materials and methods
•   2.1. Materials
•   2.2. Preparation and characterization of PLDC
•   2.3. Preparation and characterization of PLDC-SNEDDS
•   2.4. Colloidal stability of PLDC-SNEDDS colloidal dispersions
•   2.5. Animals
•   2.6. Pharmacokinetics study in rats
•   2.7. Statistical analysis
• 3. Results and discussions
•   3.1. Preparation and characterization of PLDC
•   3.2. Preparation and characterization of PLDC-SNEDDS
•   3.3. Stability of PLDC-SNEDDS colloidal dispersions
•   3.4. Pharmacokinetics study in rats
• 4. Conclusion
• Declaration of interest
• Supplementary materials

文章来源

类型: 期刊论文

作者: Dawei Ding,Bingjun Sun,Weiping Cui,Qin Chen,Xuanbo Zhang,Haotian Zhang,Zhonggui He,Jin Sun,Cong Luo

来源: Asian Journal of Pharmaceutical Sciences 2019年05期

年度: 2019

分类: 医药卫生科技,工程科技Ⅰ辑

专业: 有机化工,药学

单位: Wuya College of Innovation,Shenyang Pharmaceutical University,Cancer Hospital of China Medical University,Liaoning Cancer Hospital & Institute,School of Life Science and Biopharmaceutics,Shenyang Pharmaceutical University

基金: financially supported by the National Nature Science Foundation of China (No. 81703451),the China Postdoctoral Science Foundation (No. 2017M611269 and 2018T110233)

分类号: R943

页码: 552-558

总页数: 7

文件大小: 5161K

下载量: 11