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Preparation and Characterization of SDF-1α-Chitosan-Dextran Sulfate Nanoparticles
Published on: January 22, 2015
Preparation and characterization of novel chitosan-protamine nanoparticles for nucleus-targeted anticancer drug
Xiwei Yu1, Jiahui Hou1, Yijie Shi1
1School of Pharmacy.
Abstract:
It is well known that most anticancer drugs commonly show high toxicity to the DNA of tumor cells and exert effects by combining with the DNA or associated enzymes in the nucleus. Most developed drugs are first delivered into the cytoplasm and then transferred to the nucleus through the membrane pores. Sometimes, the transportation of drugs from cytoplasm to nucleus is not efficient and often results in poor therapeutic effects. In this study, we developed special and novel nanoparticles (NPs) made of chitosan and protamine for targeted nuclear capture of drugs to enhance anticancer effects. The anticancer effects of nuclear targeted-delivery of drugs in NPs were also evaluated by investigating cytotoxicity, cellular uptake mechanism, and cell apoptosis on cells. Chitosan-protamine NPs were characterized by good drug entrapment, sustained release, small average particle size, low polydispersity index, and high encapsulation efficiency; and accomplished the efficient nuclear delivery of fluorouracil (5-Fu). Compared with free 5-Fu and 5-Fu-loaded chitosan NPs, treatment of A549 cells and HeLa cells with 5-Fu-loaded chitosan-protamine NPs showed the highest cytotoxicity and further induced the significant apoptosis of cells. In addition, 5-Fu-loaded chitosan-protamine NPs exhibited the best efficiency in inhibiting tumor growth than the other three formulations. 5-Fu-loaded chitosan-protamine NPs enhanced antitumor efficacy through the targeted nuclear capture of drugs and showed promising potential as a nanodelivery system for quickly locating drugs in the nucleus of cells.
Insights
Novel chitosan-protamine nanoparticles efficiently deliver anticancer drugs directly to the cell nucleus, enhancing therapeutic effects and reducing tumor growth. This targeted nuclear delivery system shows significant potential for improved cancer treatment.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Pharmacology
Background:
- Anticancer drugs target tumor cell DNA within the nucleus, but inefficient cytoplasmic-to-nuclear transport limits therapeutic efficacy.
- Developing advanced drug delivery systems is crucial for overcoming these transport barriers and improving cancer treatment outcomes.
Purpose of the Study:
- To develop novel chitosan-protamine nanoparticles (NPs) for targeted nuclear delivery of anticancer drugs.
- To evaluate the enhanced anticancer effects of nuclear-targeted drug delivery using these NPs.
Main Methods:
- Chitosan-protamine nanoparticles were synthesized and characterized for drug entrapment, release kinetics, particle size, and encapsulation efficiency.
- The nuclear delivery of fluorouracil (5-Fu) using these NPs was confirmed.
- Cytotoxicity, cellular uptake mechanisms, and apoptosis induction were assessed in A549 and HeLa cancer cell lines.
Main Results:
- Chitosan-protamine NPs demonstrated excellent drug entrapment, sustained release, and efficient nuclear delivery of 5-Fu.
- 5-Fu-loaded chitosan-protamine NPs exhibited significantly higher cytotoxicity and induced greater apoptosis in cancer cells compared to free 5-Fu or 5-Fu in chitosan NPs.
- These NPs showed superior inhibition of tumor growth in vivo.
Conclusions:
- Chitosan-protamine nanoparticles effectively achieve targeted nuclear drug delivery, enhancing anticancer efficacy.
- This nanodelivery system holds significant promise for improving cancer therapy by concentrating drugs within the cell nucleus.
