The aim of this research is to evaluate the intestinal permeation of a new formulation (NF) for the anti-retroviral didanosine (ddI) drug, using the everted gut sac model. The NF is composed by granules containing ddI incorporated in chitosan microspheres, plus free chitosan as an excipient. The permeation was evaluated across the three intestinal segments of adult male Wistar rats. The performance of ddI permeation from the NF was compared to the same granules without free chitosan and to buffered ddI tablets as control. The permeations across duodenum were higher than across jejune and ileum. The ddI from NF presented higher permeation and a crescent-shaped profile in duodenum compared to the other formulations. Such effects are provided by the superior mucoadhesiveness to the intestinal membrane and potentialize sustained release properties for NF. These results lead one to consider the novel formulation to be promising for ddI administration by oral route.
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http://dx.doi.org/10.1080/02652040802466691 | DOI Listing |
J Pharm Sci
December 2024
Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, 5230 Odense, Denmark. Electronic address:
Physiological and artificial solubilizing agents usually enhance apparent solubility of poorly soluble drugs, and in many cases also oral drug exposure. However, exposure may decrease in cases where micellization reduces the molecularly dissolved drug fraction, overriding the solubility advantage. While this information is critical to accurately anticipate the effect of drug micellization on oral absorption, the experimental determination of molecularly dissolved drug concentrations is complex and time consuming.
View Article and Find Full Text PDFBiomater Sci
December 2024
National Engineering Research Center for Nanomedicine, College of Life Science and Technology, Huazhong University of Science and Technology, 430074 Wuhan, P. R. China.
Oral protein drugs' delivery faces challenges due to multiple absorption barriers for macromolecules. Co-administration with permeation enhancers and encapsulation in nano-carriers are two promising strategies to enhance their oral absorption. Herein, the poly(lactic--glycolic acid) nanoparticles (PLGA NPs) are decorated with polyethylene glycol (PEG) and a traditional Chinese medicine-derived permeation enhancer borneol (BO) for oral insulin delivery.
View Article and Find Full Text PDFFood Chem
December 2024
Nano-Biotechnology Key Laboratory of Hebei Province, State Key Laboratory of Metastable Materials Science and Technology, School of Environmental and Chemical Engineering, Yanshan University, Qinhuangdao 066004, PR China. Electronic address:
In order to elucidate the digestion, absorption and metabolism mechanism, Hohenbuehelia serotina polysaccharides were successfully labelled by fluorescein isothiocyanate (FITC-Tyr-HSP), with the fluorescent substitution degree of 0.37 %. FITC-Tyr-HSP with excellent physiological stability possessed the significant fluorescent characteristics, which could be dynamically monitored by in vivo fluorescence imaging and high performance gel permeation chromatography-fluorescence detector (HPGPC-FLD).
View Article and Find Full Text PDFInt J Biol Macromol
December 2024
Department of Pharmaceutics, Faculty of Pharmacy, The Islamia University of Bahawalpur, Bahawalpur, Pakistan.
The present study aims to develop a novel thiolated carboxymethyl cellulose (CMC-SH) by the addition of aldehyde groups via oxidation followed by reductive amination and then develop CMC-SH based pH-responsive hydrogel by free radical polymerization approach while assessing its mucoadhesive and permeation-enhancing capabilities. By in-vitro characterization, the intended compound's chemical composition, thermal stability, and amorphous nature were analyzed for CMC-SH polymer. Ellman's assay was utilized to estimate the thiol content and permeation analysis was performed to evaluate its enhanced permeability characteristics.
View Article and Find Full Text PDFACS Nano
December 2024
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China.
The development of effective oral drug delivery systems for targeted gut-to-liver transport remains a significant challenge due to the multiple biological barriers including the harsh gastrointestinal tract (GIT) environment and the complex protein corona (PC) formation. In this study, we developed ligand-modified nanoparticles (NPs) that enable gut-to-liver drug delivery by crossing the GIT and attenuating PC formation. Specifically, mesoporous silica nanoparticles (MSNs) were functionalized with peptides targeting the neonatal Fc receptor (FcRn), capitalizing on FcRn expression in the small intestine and liver for targeted drug delivery.
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