Intestinal oligopeptide transporter PepT1-targeted polymeric micelles for further enhancing the oral absorption of water-insoluble agents

Nanoscale ◽  
2019 ◽  
Vol 11 (44) ◽  
pp. 21433-21448 ◽  
Author(s):  
Yao Jin ◽  
Qi Liu ◽  
Chuhang Zhou ◽  
Xinping Hu ◽  
Leqi Wang ◽  
...  
Keyword(s):  
Oral Absorption ◽  
Polymeric Micelles ◽  
Oligopeptide Transporter ◽  
Intestinal Transporter

Intestinal transporter PepT1-targeted polymeric micelles were fabricated as nanocarriers for further enhancing the oral absorption of water-insoluble agents via PepT1-mediated transcytosis.

Formulation and Evaluation of Solubility Enhanced Ciprofloxacin

2013 ◽  
Vol 6 (3) ◽  
pp. 2131-2136
Author(s):  
R S Thakur ◽  
A Nayaz ◽  
Y Koushik
Keyword(s):  
Oral Absorption ◽  
Polymeric Micelles ◽  
In Vitro Release ◽  
Microemulsion System ◽  
Salt Form ◽  
Solubility Study ◽  
Ternary Phase Diagrams ◽  
Blood Ph ◽  
Vitro Release

In the case of solubility limited absorption, creating supersaturation in the GI fluid is very critical as supersaturation may provide great improvement of oral absorption. The techniques to create the so-called supersaturation in the GI fluid include microemulsions, emulsions, liposomes, complexations, polymeric micelles, and conventional micelles. Ciprofloxacin was chosen because it is practically insoluble in water; hence its salt form is used commercially, which is soluble in water. The objective of the present investigation was to enhance the solubility of Ciprofloxacin by formulating it into microemulsion system. For this purpose, initially, surfactant and cosurfactant were selected based on their HLB value, followed by pseudo-ternary phase diagrams to identify the microemulsion existing zone. Different formulations were developed and evaluated for pH, conductivity, in vitro release and stability. Solubility study was performed for optimized formulation. The pH of the designed formulations varied from 6.02-7.04. This was ideal and near blood pH 7.4. Conductivity data indicated that the microemulsion was of the o/w type. In vitro release of optimized formulation(FM3) was 95.2% as compared to pure drug 46.61% after 90 min and marketed product(salt form) 93.9%. Hence, by formulating into microemulsion, the solubility of ciprofloxacin is significantly enhanced.    

scholarly journals Polymeric micelles for oral drug delivery: Why and how

2004 ◽  
Vol 76 (7-8) ◽  
pp. 1321-1335 ◽  
Author(s):  
M. F. Francis ◽  
Mariana Cristea ◽  
F. M. Winnik
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Oral Absorption ◽  
Polymeric Micelles ◽  
Oral Drug Delivery ◽  
Polymeric Micelle ◽  
Water Soluble ◽  
Oral Drug ◽  
Therapeutic Effects ◽  
The Impact

The oral delivery of drugs is regarded as the optimal means for achieving therapeutic effects owing to increased patient compliance. Unfortunately, the oral delivery route is beset with problems such as gastrointestinal (GI) destruction of labile molecules, low levels of macromolecular absorption, etc. To reduce the impact of digestive enzymes and to ensure the absorption of bioactive agents in an unaltered form, molecules may be incorporated into microparticulate carriers. Many approaches to achieve the oral absorption of a wide variety of drugs are currently under investigation. Among the different polymer-based drug delivery systems, polymeric micelles represent a promising delivery vehicle especially intended for poorly water-soluble pharmaceutical active ingredients in order to improve their oral bioavailability. Recent findings of a dextran-based polymeric micelle study for solubilization of a highly lipophilic drug, cyclosporin A (CsA), will be discussed.

Enhancing Oral Bioavailability by Paclitaxel Polymeric Micelles: Role of Transmembrane Pathways in the Oral Absorption

2020 ◽  
Vol 16 (7) ◽  
pp. 1160-1168
Author(s):  
Qiaoming Liu ◽  
Meng Cheng ◽  
Jianqin Liang ◽  
Yi Jin ◽  
Jianfang Feng ◽  
...  
Keyword(s):  
Oral Bioavailability ◽  
Transport Process ◽  
Oral Absorption ◽  
Polymeric Micelles ◽  
Bioavailability Enhancement ◽  
Perfusion Model ◽  
Intestinal Membrane ◽  
Endocytosis Pathway

The oral administration of paclitaxel suffering obstacles like poorly solubility and low permeability, causing extremely low oral bioavailability. In this study, we aim to study the role of transmembrane pathway on the absorption mechanisms of PTX-Micelles. In addition, we will further study the permeability of PTX-Micelles by employing in situ perfusion model. The results showed the PTX-Micelles could be up taken by caco-2 intact. In addition, we found that the endocytosis pathway and M cells pathway attended, while paracellular pathway absented in the transport process of PTX-Micelles. The study on in situ perfusion showed the absorption rate constant (Ka) of PTX was enhanced from 6.3, 6.1, 10.6 and 13.6 × 10–2/min to 15.1, 18.4, 45.6 and 42.9 × 10–2/min by micelles in duodenum, jejunum, ileum and colon, respectively, indicating the PTX-Micelles could enhance the permeability of PTX in intestinal membrane. This study indicating that transmembrane pathway-mediated transport is an important part in the transport process of polymeric micelles, and designing formulation based on transmembrane pathways may be a promising route for oral bioavailability enhancement of poor-soluble drugs.

Preparation of scutellarin loaded TPGS polymeric micelles and evaluation of its pharmacokinetics and pharmacodynamics effects in rats

2018 ◽  
Vol 75 (6) ◽  
pp. 1305-1312
Author(s):  
Liu Zou ◽  
Shujuan Xiong ◽  
Xiangping Deng ◽  
Juan Liu ◽  
Runde Xiong ◽  
...  
Keyword(s):  
Polymeric Micelles ◽  
Pharmacokinetics And Pharmacodynamics
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