Abstract

Chitosan nanoparticles have been considered as potential candidates for drug loading/release in drug delivery systems. In this paper, nanoparticles (HACAFNP) loading adriamycin based on 2-hydroxypropyltrimethyl ammonium chloride chitosan grafting folic acid (HACF) were synthesized. The surface morphology of the novel nanoparticles was spherical or oval, and the nanoparticles exhibited a relatively small hydrodynamic diameter (85.6 ± 2.04 nm) and positive zeta potential (+21.06 ± 0.96 mV). The drug release of nanoparticles was assayed and represented a burst effect followed by a long-term steady release. Afterward, the antioxidant efficiencies of nanoparticles were assayed. In particular, the target nanoparticles exhibited significant enhancement in radical scavenging activities. Cytotoxicities against cancer cells (MCF-7, BGC-823, and HEPG-2) were estimated in vitro, and results showed nanoparticles inhibited the growth of cancer cells. It’s worth noting that the inhibition index of HACAFNP against BGC-823 cells was 71.19% with the sample concentration of 25 μg/mL, which was much higher than the inhibitory effect of ADM. It was demonstrated that the novel nanoparticles with dramatically enhanced biological activity, reduced cytotoxicity, and steady release could be used as the practical candidates for drug loading/release in a delivery system.

Highlights

  • Despite the rapid development of technology and medicine in the 21st century, cancer is still one of the major diseases that can threaten the safety and health of human life all over the world [1,2]

  • In this paper, nanoparticles (HACAFNP) loading ADM based on hydroxypropyltrimethyl ammonium chloride chitosan grafting folic acid (HACF) were synthesized via ionic gelation with the aid of TPP

  • Nanoparticles (HACAFNP) loading ADM based on HACF were synthesized via ionic gelation with the aid of TPP

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Summary

Introduction

Despite the rapid development of technology and medicine in the 21st century, cancer is still one of the major diseases that can threaten the safety and health of human life all over the world [1,2]. It has been reported that chitosan nanoparticles can be served as practical drug carriers with the advantage of a controlled and slow drug release, which can reduce toxic and adverse effects and enhance the efficacy of chemotherapy [9,17]. We hypothesize that nanoparticles loading ADM based on HACC grafting folic acid could be a practical drug carrier with the advantages of slow and controlled drug release, enhanced antioxidant activity, antitumor activity, and reduced toxicity. In this present work, the objective was to develop novel nanoparticles loading ADM based on HACC grafting folic acid through ionic gelation with the aid of sodium tripolyphosphate (TPP), and to evaluate the morphology, properties, and activities of nanoparticles. After 48 h of dialyzing, the residual solution was dried in vacuo to obtain HACC grafting folic acid (HACF)

Preparation of Nanoparticles via HACC and HACF
Fourier-Transform Infrared Spectroscopy
H Nuclear Magnetic Resonance Spectroscopy of Chitosan Derivatives
Morphology
Entrapped Efficiency and Drug Loading of Nanoparticles
Swelling Degree
Evaluation of Sustained Release Performance
Superoxide-Radical Scavenging Activity Assay
DPPH Radical Scavenging Ability Assay
Cytotoxicity Assay
Statistical Analysis
FTIR Spectra
H NMR Spectra and DS of Chitosan Derivatives
MMoorrpphhoollooggyy AAnnaallyyssiiss
Entrapped Efficiency and Drug Loading Analysis
In Vitro Release of Chitosan Nanoparticles
Conclusions
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