Nanocrystals for Improving Oral Bioavailability of Drugs: Intestinal Transport Mechanisms and Influencing Factors

2021 ◽  
Vol 22 (5) ◽  
Author(s):  
Zonghua Tian ◽  
Yaping Mai ◽  
Tingting Meng ◽  
Shijie Ma ◽  
Guojing Gou ◽  
...  
Keyword(s):  
Influencing Factors ◽  
Oral Bioavailability ◽  
Intestinal Transport ◽  
Transport Mechanisms

Shale Gas Transport in Nanopores: Contribution of Different Transport Mechanisms and Influencing Factors

2021 ◽  
Vol 35 (3) ◽  
pp. 2033-2047
Author(s):  
Xiangyu Liu ◽  
Liehui Zhang ◽  
Yulong Zhao ◽  
Xiao He ◽  
Jianfa Wu ◽  
...  
Keyword(s):  
Influencing Factors ◽  
Shale Gas ◽  
Gas Transport ◽  
Transport Mechanisms ◽  
Shale Gas Transport

scholarly journals Transport Mechanisms of Polymannuronic Acid and Polyguluronic Acid Across Caco-2 Cell Monolayers

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 167
Author(s):  
Yu Wang ◽  
Xu Bai ◽  
Bo Hu ◽  
Maochen Xing ◽  
Qi Cao ◽  
...  
Keyword(s):  
Epithelial Cells ◽  
Biological Activities ◽  
Intestinal Transport ◽  
Fluorescein Isothiocyanate ◽  
Endocytic Pathway ◽  
Detailed Knowledge ◽  
Intestinal Epithelial ◽  
Transport Mechanisms ◽  
Apparent Permeability ◽  
Cell Monolayers

Detailed knowledge of the intestinal transport of polymannuronic acid (PM) and polyguluronic acid (PG) is critical for understanding their biological activities. To investigate the transport in the gastrointestinal tract, PM and PG were chemically modified with tyramine and conjugated with fluorescein isothiocyanate (FITC) to synthesize FITC-PM (F-PM) and FITC-PG (F-PG) successfully. The transport mechanisms of F-PM and F-PG across the intestinal epithelial cell monolayers (Caco-2 cell monolayers) were then investigated. The results demonstrated that the transport of F-PM and F-PG into epithelial cells was time- and energy-dependent, which was mediated by the macropinocytosis pathway and the clathrin- and caveolae (or lipid raft)-mediated endocytic pathway. The transport process of F-PM and F-PG in Caco-2 cells depended on the acidification of endosomes and involved lysosomes. Tubulin mediated the transport of F-PM, but not of F-PG. Moreover, the absorption enhancer chitosan (CS) promoted the transport of F-PM and F-PG, increasing the apparent permeability coefficient (Papp) by 1.9-fold and 2.6-fold, respectively, by reversibly opening the tight junction (TJ). In summary, this study provided a comprehensive understanding of the transport of PM and PG in the small intestinal epithelial cells, which will provide a theoretical basis for the development of PM and PG with good intestinal absorption.

Effect of Resveratrol Pretreatment on Intestinal Transport and Oral Bioavailability of Carvedilol in Rats by P-gp Inhibition

2020 ◽  
Vol 13 (4) ◽  
pp. 1660
Author(s):  
Mohammed Abdul Aziz Shahid ◽  
Y Shravan Kumar ◽  
Syed Umar Farooq ◽  
Md. Shamim Qureshi
Keyword(s):  
Oral Bioavailability ◽  
Intestinal Transport

scholarly journals Dual-functional Brij-S20-modified nanocrystal formulation enhances the intestinal transport and oral bioavailability of berberine

2018 ◽  
Vol Volume 13 ◽  
pp. 3781-3793 ◽  
Author(s):  
Wei Xiong ◽  
Wei Sang ◽  
Ke Gang Linghu ◽  
Zhang Feng Zhong ◽  
Wai San Cheang ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Intestinal Transport ◽  
Dual Functional

scholarly journals Lipid-based nanocarriers for oral delivery of peptides

OCL ◽  
2022 ◽  
Vol 29 ◽  
pp. 1
Author(s):  
Camille Dumont
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Intestinal Transport ◽  
Intestinal Lumen ◽  
Burst Release ◽  
Solid Lipid ◽  
Lipid Nanocarriers ◽  
Therapeutic Peptides ◽  
Poor Stability ◽  
Platelet Shape

Therapeutic peptides can treat a wide variety of diseases with selective and potent action. Their oral bioavailability is strongly limited by an important proteolytic activity in the intestinal lumen and poor permeation across the intestinal border. We have evaluated the capacity of solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) to overcome both oral bioavailability limiting aspects, using leuprolide (LEU) as model peptide. Lipidization of LEU by formation of a hydrophobic ion pair (HIP) with sodium docusate enables a significant increase of peptide encapsulation efficiency in both SLN and NLC. The nanocarriers, obtained by high-pressure homogenization, measured 120 nm and were platelet shaped. Regarding the protective effect towards proteolytic degradation, only NLC maintained LEU integrity in presence of trypsin. Intestinal transport, evaluated on Caco-2 (enterocyte-like model) and Caco-2/HT29-MTX (mucin-secreting model) monolayers, showed nanocarriers internalization by enterocytes but no improvement of LEU permeability. Indeed, the combination of nanoparticles platelet-shape with the poor stability of the HIP in the transport medium induces a high burst release of the peptide, limiting nanoparticles capacity to transport LEU across the intestinal border. Stability of peptide lipidization needs to be improved to withstand biorelevant medium to benefit from the advantages of encapsulation in solid lipid nanocarriers and consequently improve their oral bioavailability.

Enhanced oral bioavailability of metoprolol with gallic acid and ellagic acid in male Wistar rats: involvement of CYP2D6 inhibition

2016 ◽  
Vol 31 (4) ◽  
Author(s):  
Bhargavi Latha Athukuri ◽  
Prasad Neerati
Keyword(s):  
Drug Interactions ◽  
Gallic Acid ◽  
Ellagic Acid ◽  
Oral Bioavailability ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Intestinal Transport ◽  
Herbal Drug ◽  
Male Wistar Rats ◽  
Mixed Function Oxidase System

Abstract Background: Cytochrome P450-2D6 (CYP2D6), a member of the CYP450 mixed function oxidase system, is an important CYP isoform with regard to herbal-drug interactions and is responsible for the metabolism of nearly 25% of drugs. Until now, studies on the effects of various phytochemicals on CYP2D6 activity Methods: The intestinal transport of metoprolol was assessed by conducting an Results: After pretreatment with gallic acid and ellagic acid, no significant change in effective permeability of metoprolol was observed at the ileum part of rat intestine. A significant improvement in the peak plasma concentration (C Conclusions: Gallic acid and ellagic acid significantly enhanced the oral bioavailability of metoprolol by inhibiting CYP2D6-mediated metabolism in the rat liver. Hence, adverse herbal-drug interactions may result with concomitant ingestion of gallic acid and ellagic acid supplements and drugs that are CYP2D6 substrates. The clinical assessment of these interactions should be further investigated in human volunteers.

Improved oral bioavailability of docetaxel by nanostructured lipid carriers: in vitro characteristics, in vivo evaluation and intestinal transport studies

RSC Advances ◽  
2015 ◽  
Vol 5 (117) ◽  
pp. 96437-96447 ◽  
Author(s):  
Guihua Fang ◽  
Bo Tang ◽  
Yanhui Chao ◽  
Yu Zhang ◽  
Hui Xu ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Intestinal Transport ◽  
Nanostructured Lipid Carriers ◽  
Absorption Mechanism ◽  
In Vivo Evaluation ◽  
Transport Studies

The objective of the current study was to explore the potential of nanostructured lipid carriers (NLC) for oral delivery of docetaxel (DTX) and investigate the absorption mechanismin vivo.

Developmental patterns of intestinal transport mechanisms in the chick

1976 ◽  
Vol 54 (1) ◽  
pp. 109-111 ◽  
Author(s):  
Joseph Lerner ◽  
Peter H. Burrill ◽  
Peggy A. Sattelmeyer ◽  
Caryle F. Janicki
Keyword(s):  
Intestinal Transport ◽  
Transport Mechanisms ◽  
Developmental Patterns
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