Shiqi Guo1, Yanzi Liang1, Lanze Liu2, Miaomiao Yin3, Aiping Wang1, Kaoxiang Sun1,4, Youxin Li5,6, Yanan Shi7. 1. School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai, 264005, People's Republic of China. 2. College of Life Science, Yantai University, Yantai, 264005, People's Republic of China. 3. China Resources Double-crane Pharmaceutical Co., Ltd., Beijing, China. 4. State Key Laboratory of Long-acting and Targeting Drug Delivery System, Luye Pharmaceutical Co., Ltd., Yantai, China. 5. School of Pharmacy, Key Laboratory of Molecular Pharmacology and Drug Evaluation (Yantai University), Ministry of Education, Collaborative Innovation Center of Advanced Drug Delivery System and Biotech Drugs in Universities of Shandong, Yantai University, Yantai, 264005, People's Republic of China. youxinli@luye.com. 6. State Key Laboratory of Long-acting and Targeting Drug Delivery System, Luye Pharmaceutical Co., Ltd., Yantai, China. youxinli@luye.com. 7. College of Life Science, Yantai University, Yantai, 264005, People's Republic of China. shiyanan001@163.com.
Abstract
BACKGROUND: The use of drug nanocarriers to encapsulate drugs for oral administration may become an important strategy in addressing the challenging oral absorption of some drugs. In this study-with the premise of controlling single variables-we prepared model nanoparticles with different particle sizes, surface charges, and surface hydrophobicity/hydrophilicity. The two key stages of intestinal nanoparticles (NPs) absorption-the intestinal mucus layer penetration stage and the trans-intestinal epithelial cell stage-were decoupled and analyzed. The intestinal absorption of each group of model NPs was then investigated. RESULTS: Differences in the behavioral trends of NPs in each stage of intestinal absorption were found to result from differences in particle properties. Small size, low-magnitude negative charge, and moderate hydrophilicity helped NPs pass through the small intestinal mucus layer more easily. Once through the mucus layer, an appropriate size, positive surface charge, and hydrophobic properties helped NPs complete the process of transintestinal epithelial cell transport. CONCLUSIONS: To achieve high drug bioavailability, the basic properties of the delivery system must be suitable for overcoming the physiological barrier of the gastrointestinal tract.
BACKGROUND: The use of drug nanocarriers to encapsulate drugs for oral administration may become an important strategy in addressing the challenging oral absorption of some drugs. In this study-with the premise of controlling single variables-we prepared model nanoparticles with different particle sizes, surface charges, and surface hydrophobicity/hydrophilicity. The two key stages of intestinal nanoparticles (NPs) absorption-the intestinal mucus layer penetration stage and the trans-intestinal epithelial cell stage-were decoupled and analyzed. The intestinal absorption of each group of model NPs was then investigated. RESULTS: Differences in the behavioral trends of NPs in each stage of intestinal absorption were found to result from differences in particle properties. Small size, low-magnitude negative charge, and moderate hydrophilicity helped NPs pass through the small intestinal mucus layer more easily. Once through the mucus layer, an appropriate size, positive surface charge, and hydrophobic properties helped NPs complete the process of transintestinal epithelial cell transport. CONCLUSIONS: To achieve high drug bioavailability, the basic properties of the delivery system must be suitable for overcoming the physiological barrier of the gastrointestinal tract.
Authors: Nabeel Ahmad; Sharad Bhatnagar; Ritika Saxena; Danish Iqbal; A K Ghosh; Rajiv Dutta Journal: Mater Sci Eng C Mater Biol Appl Date: 2017-04-05 Impact factor: 7.328
Authors: Carlos Fernandes; Cláudia Martins; André Fonseca; Rute Nunes; Maria João Matos; Renata Silva; Jorge Garrido; Bruno Sarmento; Fernando Remião; Francisco J Otero-Espinar; Eugenio Uriarte; Fernanda Borges Journal: ACS Appl Mater Interfaces Date: 2018-11-09 Impact factor: 9.229
Authors: Agata P Walczak; Peter J M Hendriksen; Ruud A Woutersen; Meike van der Zande; Anna K Undas; Richard Helsdingen; Hans H J van den Berg; Ivonne M C M Rietjens; Hans Bouwmeester Journal: J Nanopart Res Date: 2015-05-22 Impact factor: 2.253