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Preparation and Evaluation of Novel Emodin-loaded Stearic Acid-g-chitosan Oligosaccharide Nanomicelles.

ABSTRACT: The purpose of this study was to prepare and characterize emodin-loaded stearic acid-g-chitosan oligosaccharide (CSO-SA/EMO) and to evaluate its antitumor activity in vitro. In this study, stearic acid-g-chitosan oligosaccharide was used as a carrier and its physicochemical properties were determined by different methods. Cell uptake behavior was examined using FITC-labeled stearic acid-g-chitosan oligosaccharide. CSO-SA/EMO was prepared using ultrasonication and dialysis. Particle size, surface potential, entrapment efficiency, and drug release behavior were studied in vitro. The effects of CSO-SA/EMO on gastric cancer cells were investigated using MTT assay and flow cytometry. Results showed CSO-SA/EMO particle size was larger and potential was smaller than that of stearic acid-g-chitosan oligosaccharide. The 12?h micellar uptake by MGC803 and BGC823 cells was sufficient, and the micelles were able to abundantly accumulate at lesion sites in mice thus achieving good passive EPR targeting. MTT and cell cycle arrest assays showed CSO-SA/EMO-enhanced antitumor activity significantly towards MGC803 and BGC823 cells compared with that of free emodine. Tumor volume, hematoxylin and eosin staining, and terminal deoxynucleotide transferase dUTP nick-end labeling assay proved CSO-SA/EMO had a significant antitumor effect on tumor tissues in vivo. In conclusion, the ultrasonication-dialysis method provided a simple and effective method for preparing CSO-SA/EMO. The delivery of emodine using a micelle system improved its antitumor effects effectively.

SUBMITTER: Jiang X

PROVIDER: S-EPMC7183521 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature

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Preparation and Evaluation of Novel Emodin-loaded Stearic Acid-g-chitosan Oligosaccharide Nanomicelles.

Jiang Xiaohong X Ma Mingxing M Li Mingjuan M Shao Shihong S Yuan Hong H Hu Fuqiang F Liu Jianwen J Huang Xuan X

Nanoscale research letters 20200425 1

The purpose of this study was to prepare and characterize emodin-loaded stearic acid-g-chitosan oligosaccharide (CSO-SA/EMO) and to evaluate its antitumor activity in vitro. In this study, stearic acid-g-chitosan oligosaccharide was used as a carrier and its physicochemical properties were determined by different methods. Cell uptake behavior was examined using FITC-labeled stearic acid-g-chitosan oligosaccharide. CSO-SA/EMO was prepared using ultrasonication and dialysis. Particle size, surface ...[more]

PMID: 32335740

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Project description:Background and purposeThe purpose of this study was to investigate the effect of incorporating chitosan (Ch) and chitosan oligosaccharides (ChO) into the commercially premixed antibiotic-loaded bone cement (ALBC). We compare antibiotic release profiles, antibacterial activity, and mechanical properties among different ALBC formulations. The hypothesis was that increasing the amount of Ch and ChO in the cement mixture would increase the antibiotics released and bacterial control. ALBC mixed with Ch or ChO may create a greater effect due to its superior dissolving property.Materials and methodsThe bone cement samples used in this project were made from Copal® G+V composed of vancomycin and gentamicin. To prepare the Ch and the ChO mixed bone cement samples, different amounts of Ch and ChO were added to the polymethylmethacrylate matrix with three concentrations (1%, 5%, and 10%). Drug elution assay, antimicrobial assay, in vitro cytotoxicity, and mechanical properties were conducted.ResultsBone cement samples made from Copal® G+V alone or combined with Ch or ChO can release vancomycin and gentamicin into the phosphate-buffered saline. Mixing ChO into the bone cements can increase the amount of drug released more than Ch. ChO 10% gave the highest amount of antibiotics released. All samples showed good antibacterial properties with good biocompatibility in vitro. The microhardness values of the Ch and ChO groups increased significantly compared to the control group. In all groups tested, the microhardness of bone cements was reduced after the drug eluted out. However, this reduction of the Ch and ChO groups was in line with the control.InterpretationVarious attempts have been made to improve the ALBC efficacy. In our study, the best bone cement formulation was bone cement mixed with ChO (10%), which had the highest drug release profiles, was biocompatible, and contained antibacterial properties with acceptable mechanical properties. This phenomenon could result from the superior water solubility of the ChO. When ChO leaves the bone cement specimens, it generates pores that could act as a path that exposes the bone cement matrix to the surrounding medium, increasing antibiotic elution. From all above, ChO is a promising substance that could be added to ALBC in order to increase the drug elution rate. However, more in vitro and in vivo experiments are needed before being used in the clinic.

Dataset Information

Preparation and Evaluation of Novel Emodin-loaded Stearic Acid-g-chitosan Oligosaccharide Nanomicelles.

Publications

Preparation and Evaluation of Novel Emodin-loaded Stearic Acid-g-chitosan Oligosaccharide Nanomicelles.

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