Research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics: size, surface charge and pro-hydrophobics

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 pa...

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Main Authors: Shiqi Guo, Yanzi Liang, Lanze Liu, Miaomiao Yin, Aiping Wang, Kaoxiang Sun, Youxin Li, Yanan Shi
Format: Article
Language:English
Published: BMC 2021-01-01
Series:Journal of Nanobiotechnology
Subjects:
Online Access:https://doi.org/10.1186/s12951-021-00770-2
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author Shiqi Guo
Yanzi Liang
Lanze Liu
Miaomiao Yin
Aiping Wang
Kaoxiang Sun
Youxin Li
Yanan Shi
author_facet Shiqi Guo
Yanzi Liang
Lanze Liu
Miaomiao Yin
Aiping Wang
Kaoxiang Sun
Youxin Li
Yanan Shi
author_sort Shiqi Guo
collection DOAJ
description 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.
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spelling doaj.art-b5a946972c9e43faa174ded4098096ab2022-12-22T04:20:58ZengBMCJournal of Nanobiotechnology1477-31552021-01-0119112110.1186/s12951-021-00770-2Research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics: size, surface charge and pro-hydrophobicsShiqi Guo0Yanzi Liang1Lanze Liu2Miaomiao Yin3Aiping Wang4Kaoxiang Sun5Youxin Li6Yanan Shi7School 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 UniversitySchool 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 UniversityCollege of Life Science, Yantai UniversityChina Resources Double-crane Pharmaceutical Co., Ltd.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 UniversitySchool 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 UniversitySchool 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 UniversityCollege of Life Science, Yantai UniversityAbstract 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.https://doi.org/10.1186/s12951-021-00770-2Polymeric nanoparticlesBasic propertiesMucus layerIntestinal epitheliumPhysiological barrier
spellingShingle Shiqi Guo
Yanzi Liang
Lanze Liu
Miaomiao Yin
Aiping Wang
Kaoxiang Sun
Youxin Li
Yanan Shi
Research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics: size, surface charge and pro-hydrophobics
Journal of Nanobiotechnology
Polymeric nanoparticles
Basic properties
Mucus layer
Intestinal epithelium
Physiological barrier
title Research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics: size, surface charge and pro-hydrophobics
title_full Research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics: size, surface charge and pro-hydrophobics
title_fullStr Research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics: size, surface charge and pro-hydrophobics
title_full_unstemmed Research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics: size, surface charge and pro-hydrophobics
title_short Research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics: size, surface charge and pro-hydrophobics
title_sort research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics size surface charge and pro hydrophobics
topic Polymeric nanoparticles
Basic properties
Mucus layer
Intestinal epithelium
Physiological barrier
url https://doi.org/10.1186/s12951-021-00770-2
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