Fabrication of galactosylated chitosan–5‐fluorouracil acetic acid based nanoparticles for controlled drug delivery

Abstract

In this study, a novel type of macromolecular prodrug, N-galactosylated chitosan (GC)25-fluorouracil acetic acid (FUA) conjugate based nanoparticles, was designed and synthesized as a carrier for hepatocellular carcinoma drug delivery. The GC-FUA nanoparticles were produced by an ionic crosslinking method based on the modified ionic gelation of tripolyphosphate with GC-FUA. The structure of the as-prepared GC-FUA was characterized by Fourier transform infrared and 1 H-NMR analyses. The average particle size of the GC-FUA nanoparticles was 160.1 nm, and their drug-loading content was 21.22 6 2.7% (n 5 3). In comparison with that of the freshly prepared nanoparticles, this value became larger after 7 days because of the aggregation of the GC-FUA nanoparticles. An in vitro drug-release study showed that the GC-FUA nanoparticles displayed a sustained-release profile compared to 5-fluorouracil-loaded GC nanoparticles. All of the results suggest that the GC-FUA nanoparticles may have great potential for antiliver-cancer applications.

In vitro and in vivo evaluation of macromolecular prodrug GC-FUA based nanoparticle for hepatocellular carcinoma chemotherapy

“…The preparation of the GC-FUA-NPs followed the established procedure, which has been described in detail elsewhere (Yu et al, 2015 ). The compound (GC-FUA) was synthesized by amide condensation reaction of GC and FUA.…”

“…Furthermore, the in vitro cytotoxicity and cellular uptake, in vivo pharmacokinetic (PK) and tissue distribution of GC-FUA nanoparticles also were investigated in this research (our laboratory has been preparing a novel macromolecular prodrug N-galactosylated-chitosan-5-fluorouracil acetic acid (GC-FUA) conjugate based nanoparticle; Yu et al, 2015 ).…”

Development of local anesthetic drug delivery system by administration of organo-silica nanoformulations under ultrasound stimuli: in vitro and in vivo investigations

“…All the prepared specimens demonstrated bands at 1649, 810, and 496 cm −1 due to Si–O bending and stretching, respectively. Contrasted and chitosan (Murali et al., 2018 ), Figure 1(b,c) demonstrates the bands of amides I and II of GC exhibited at the peak ranges of 1626 and 1531 cm −1 , indicating that bathochromic move, which revealed that MONPs was covered by the GCS (Yu et al., 2015 ). Additionally, an extra band displays in the MONPs@RV and GCS-MONPs@RV at 1580 cm −1 because of the amide bowing which is missing in GCS-MONPs.…”

Non-coding RNAs: New therapeutic targets and opportunities for hepatocellular carcinoma

“…It has also been discovered that transfecting miR-122 mimics into HCC mice using cationic lipid nanoparticles as carriers could highly target HCC cells, inhibiting proliferation and angiogenesis. The use of natural macromolecular nanoparticles as vectors to deliver both ncRNAs and antineoplastic agents in HCC therapy has been studied previously [90] . Clinical data have shown that miR-21 in HCC cell lines and clinical HCC samples was a significant modulator of the anti-tumor effect of interferon-alpha (IFN-α) and 5-fluorouracil (5-FU).…”