Free amino groups on the surface of chitosan nanoparticles and its characteristics
Guangdong Provincial Hospital of Traditional Chinese Medicine, Guangzhou University of Traditional Chinese Medicine, Guangzhou 510120, China.Yao xue xue bao = Acta pharmaceutica Sinica 04/2007; 42(3):323-8.
The relationship of free amino groups on the surface and the characteristics of chitosan nanoparticles (CS-NPs) prepared by ionic gelation method was investigated. Free amino groups on the surface of CS-NPs were determined by colloidal titration, and the effects of the amount of free amino groups and its ionizable level on the particle size, zeta potential, appearance, drug entrapment efficiency and drug release profile in vitro of CS-NPs were investigated. The result showed that the surface free amino groups reduced, the average size, zeta potential, stability of nanoparticles, and the drug release rate and degree all decreased while the drug entrapment efficiency was not affected with the increase of tripolyphosphate (TPP) concentration. With the increase of pH, the free amino groups could be deprotonated and the ionizable level was stepped down, correspondingly the particle size and zeta potential of CS-NPs decreased. Additionally, the drug release rate and degree were elevated in acid medium while descended in neutral or base medium. The amount and ionizable level of free amino groups on the surface are affected by the gelation degree and pH, which further affected the volume phase transitions (swelling/shrinking processes) of CS-NPs. The properties of CS-NPs have correlation with the surface free amino groups.
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ABSTRACT: The aim of the present work was to investigate the potential utility of chitosan nanoparticles surface modified with glycyrrhizin (CS-NPs-GL) as new hepatocyte-targeted delivery vehicles. For this purpose, chitosan nanoparticles (CS-NPs) were prepared previously by ionic gelation process and glycyrrhizin was oxidized by sodium periodate to be conjugated to the surface of CS-NPs. The CS-NPs-GL obtained were first characterized for their morphology, particle size, zeta potential, association efficiency and in vitro release of adriamycin (ADR), using as a model drug. The nanoparticles were also labeled with rhodamine B isothiocyanate and their interaction with rat hepatocytes was examined by flow cytometry (FCM) and confocal laser microscopy (CLSM). The spherical nanoparticles prepared with oxidized GL/CS ratio of 0.14:1 (w/w) were in the 147.2nm size range, and exhibited a positive electrical charge (+9.3mV), and associated ADR quite efficiently (association efficiency: 91.7%) and showed lower extent of release (28% over 72h) in vitro. FCM and CLSM studies showed that CS-NPs-GL were preferentially accumulated in hepatocytes and the cellular uptake amount were 4.9 times more than that in hepatic nonparenchymal cells, and the uptake process was dependent on incubation time and dose of nanoparticles, which indicated that the internalization of these nanoparticles into hepatocytes was mostly mediated by a ligand-receptor interaction. In conclusion, CS-NPs-GL as a promising hepatocyte-targeted delivery carrier holds promise for further effective studies.International Journal of Pharmaceutics 08/2008; 359(1-2):247-53. DOI:10.1016/j.ijpharm.2008.03.039 · 3.65 Impact Factor
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ABSTRACT: Encapsulation and immobilization technology is important for the food processing and bioengineering industries. Chitosan is a natural polysaccharide prepared by the N-deacetylation of chitin. It has been widely used in food and bioengineering industries, including the encapsulation of active food ingredients, in enzyme immobilization, and as a carrier for controlled drug delivery, due to its significant biological and chemical properties such as biodegradability, biocompatibility, bioactivity, and polycationicity. In this work, chitosan nanoparticles and nanofibers used to encapsulate bioactive substances and immobilize enzymes were reviewed. Preparation of chitosan nanoparticles and nanofibers, including the work achieved in our group on chitosan nanoparticles for enzyme immobilization, were also introduced. Some problems encountered with nano-structured chitosan carriers for bioactive substance encapsulation and enzyme immobilization were discussed, together with the future prospects of such systems.Brazilian Journal of Chemical Engineering 09/2011; 28(3):353-362. DOI:10.1590/S0104-66322011000300001 · 1.04 Impact Factor
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