The physicochemical compatibility between amphiphilic polymers and hydrophobic drugs has been recognized as an important issue for improving the drug solubilisation in polymeric micelle formulations. In this work, poly-L-lysine (PLL) grafted by cholate pendants as the only hydrophobic moiety were synthesized in order to facilitate the solubilisation of sterol drugs. Results showed that micelles formed by cholate grafted PLL encapsulated significantly higher level of prednisolone and estradiol than palmitoylated PLL micelles, whereas the solubilisation capacity of non-sterol drug (griseofulvin) is inefficient for both polymers. This suggests that higher drug-polymer incorporation can be achieved by the inclusion of hydrophobic moieties with similar architecture as the drugs, i.e. 'drug-like' functional groups, which will be useful for the future design of colloidal systems for the encapsulation of specific drug.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.3109/02652048.2011.615951 | DOI Listing |
Am J Physiol Gastrointest Liver Physiol
April 2024
Departamento de Bioquímica y Biología Molecular y Celular, Facultad de Veterinaria, Instituto de Investigación Sanitaria de Aragón-Universidad de Zaragoza, Zaragoza, Spain.
Molecules
January 2024
Food Science College, Shanxi Normal University, Taiyuan 030619, China.
Jujube residue is an abundant and low-cost dietary fiber resource, but its relatively lower hydration and functional properties limit its utilization as an ingredient of functional food. Thus, cellulase and hemicellulase hydrolysis, enzymatic hydrolysis assisted by phosphate grafting (EPG), and enzymatic hydrolysis assisted by acrylate grafting (EAG) were used to improve the functional properties of jujube residue dietary fiber (JRDF) in this study. The results evidenced that these modifications all increased the porosity of the microstructure of JRDF and increased the soluble fiber content, surface area, and hydration properties, but reduced its brightness ( < 0.
View Article and Find Full Text PDFHepatol Commun
February 2023
Guangdong Pharmaceutical University, Guangzhou, Guangdong, China.
Non-alcoholic steatohepatitis (NASH) has become a major cause of liver transplantation and liver-associated death. The gut-liver axis is a potential therapy for NASH. Sodium cholate (SC) is a choleretic drug whose main component is bile acids and has anti-inflammatory, antifibrotic, and hepatoprotective effects.
View Article and Find Full Text PDFFood Res Int
September 2021
College of Food Science, Shanxi Normal University, Linfen 041004, China.
To improve the adsorption capacities and hypoglycemic properties of millet bran dietary fibre (MBDF), four methods including acrylate-grafting, carboxymethylation, heat assisted with cellulase hydrolysis, and enzymatic hydrolysis combined with acrylate-grafting were used. The results demonstrated that all carboxymethylation, acrylate-grafting, and enzymatic hydrolysis combined with acrylate-grafting improved soluble dietary fibre content, water swelling ability and α-amylase-inhibition activity of MBDF. They also increased oil, cholesterol, sodium cholate, copper ion and nitrite ion adsorption capacities of MBDF.
View Article and Find Full Text PDFCarbohydr Polym
September 2020
Department of Chemical Engineering, Waterloo Institute for Nanotechnology, University of Waterloo, 200 University Avenue West, Waterloo, ON, N2L 3G1, Canada. Electronic address:
Grafting beta-cyclodextrin (β-CD) onto cellulose nanocrystals (CNC) with the formation of well-dispersed nanoparticles (CNC-CD) and understanding their physicochemical properties are appealing but still challenging in controlled-release applications. Two immobilization methods were proposed and examined in this study; (i) copper (I) catalyzed click chemistry (CuACC) and (ii) carbodiimide coupling. Fourier-transform infrared spectroscopy (FTIR), UV-vis, elementary analysis, contact angle measurements, and thermogravimetric analysis (TGA) were conducted to elucidate the surface modifications.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!