Recent advances in galactose-engineered nanocarriers for the site-specific delivery of siRNA and anticancer drugs

Jain, Ashay; Jain, Atul; Parajuli, Prahlad; Mishra, Vijay; Ghoshal, Gargi; Singh, Bhupinder; Shivhare, U. S.; Katare, Om Prakash; Kesharwani, Prashant

doi:10.1016/j.drudis.2017.11.003

Cited by 41 publications

(27 citation statements)

References 85 publications

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Section: Discussionmentioning

confidence: 99%

“…The glycan galactose is involved in numerous biological processes, hence galactosylation is considered as a useful tool for delivery of therapeutics 86 – 88 . For example, galactosylated nanocarriers have been shown to improve site-specific delivery of siRNA and anticancer drugs 86 . Indeed, galactose has been employed in studies for the treatment and diagnosis of several diseases, as well as vaccine development 89 – 91 .…”

Section: Discussionmentioning

confidence: 99%

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Tryptophan-galactosylamine conjugates inhibit and disaggregate amyloid fibrils of Aβ42 and hIAPP peptides while reducing their toxicity

et al. 2020

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Self-assembly of proteins into amyloid fibrils is a hallmark of various diseases, including Alzheimer's disease (AD) and Type-2 diabetes Mellitus (T2DM). Aggregation of specific peptides, like Aβ42 in AD and hIAPP in T2DM, causes cellular dysfunction resulting in the respective pathology. While these amyloidogenic proteins lack sequence homology, they all contain aromatic amino acids in their hydrophobic core that play a major role in their selfassembly. Targeting these aromatic residues by small molecules may be an attractive approach for inhibiting amyloid aggregation. Here, various biochemical and biophysical techniques revealed that a panel of tryptophan-galactosylamine conjugates significantly inhibit fibril formation of Aβ42 and hIAPP, and disassemble their pre-formed fibrils in a dosedependent manner. They are also not toxic to mammalian cells and can reduce the cytotoxicity induced by Aβ42 and hIAPP aggregates. These tryptophan-galactosylamine conjugates can therefore serve as a scaffold for the development of therapeutics towards AD and T2DM.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Tryptophan-galactosylamine conjugates inhibit and disaggregate amyloid fibrils of Aβ42 and hIAPP peptides while reducing their toxicity

et al. 2020

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“…Such nanogels could avoid the undesirable endocytosis of nanogels in normal cells. Furthermore, to enhance the accumulation of nanogels at the sites of action, the nanogels could be conjugated with peptides and protein, 36 galactose, 37 or coated with cell membranes, 38 leading to specific cell endocytosis. Therefore, chlorophyllin-containing nanogels could enter tumors with minimal damages to the normal tissues.…”

Section: Resultsmentioning

confidence: 99%

Fabrication of Chlorophyll-Incorporated Nanogels for Potential Applications in Photothermal Cancer Therapy

2018

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Nanogels have been widely used in biomedical applications, such as carriers for hyperthermia cancer treatment, drug delivery, and imaging. Owing to the enhanced permeability and retention effect, nanogels have shown a great potential in cancer therapy. In this study, sodium copper chlorophyllin (SCC), a low cytotoxicity and biodegradable photothermal agent, was copolymerized with a nanogel of N-[3-(dimethylamino)propyl]methacrylamide. The nanogels could produce heat under exposure to a green laser with a 532 nm wavelength. The positively charged nature of the nanogels enhanced the endocytosis of the nanogels. The cell mortality was greatly enhanced with the treatment of the SCC-containing nanogels and green light illumination. Our results suggest the potential of SCC-containing nanogels in photothermal cancer therapy.

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“…These results indicate that cytosis plays an important role in the cellular trafficking of RES-GNPs, especially the clathrin-mediated endocytosis by ligand-receptor/transporter interaction. 37 The fluorescent staining of Caco-2 cells treated with coumarin 6-labeled RES-NPs and RES-GNPs is shown in Figure 8. Both RES-NPs and RES-GNPs could be internalized into the cells.…”

Section: Intestinal Permeabilitymentioning

confidence: 99%

Galactosylated PLGA nanoparticles for the oral delivery of resveratrol: enhanced bioavailability and in vitro anti-inflammatory activity

Siu

Lin

et al. 2018

IJN

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BackgroundResveratrol (RES) is a natural anti-inflammatory and antioxidant compound with poor water solubility and oral bioavailability. The present study takes the advantages of nanocarriers combined with a ligand (galactose) anchoring to orally deliver RES in an attempt to improve its bioavailability and pharmacological activity.MethodsRES-loaded galactosylated nanoparticles (RES-GNPs) were prepared by solvent diffusion technique using poly(lactic-co-glycolic acid), synthesized N-oleoyl-d-galactosamine and Tween 80. RES-GNPs were characterized by particle size, morphology, entrapment efficiency (EE) and in vitro release. Oral bioavailability and in vitro anti-inflammatory activity were investigated in rats and lipopolysaccharides-induced RAW 264.7 cells, respectively.ResultsThe resulting RES-GNPs were 108.4 nm around in particle size with a polydispersity index of 0.217. Furthermore, RES-GNPs possessed a high EE and a slow drug release in water. After oral administration, RES-GNPs significantly enhanced the oral bioavailability of RES, up to 335.7% relative to RES suspensions. In situ single-pass intestinal perfusion and cellular uptake experiments showed that GNPs could improve the intestinal permeability and transcellular transport of RES. Moreover, the anti-inflammatory efficacy of RES-GNPs in RAW 264.7 cells model was superior to free RES and RES-GNPs.ConclusionThe results indicate that RES-GNPs can effectively promote the intestinal absorption of RES and strengthen its bioactivity, which may be a promising system for the treatment of inflammatory diseases.

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Recent advances in galactose-engineered nanocarriers for the site-specific delivery of siRNA and anticancer drugs

Cited by 41 publications

References 85 publications

Tryptophan-galactosylamine conjugates inhibit and disaggregate amyloid fibrils of Aβ42 and hIAPP peptides while reducing their toxicity

Tryptophan-galactosylamine conjugates inhibit and disaggregate amyloid fibrils of Aβ42 and hIAPP peptides while reducing their toxicity

Fabrication of Chlorophyll-Incorporated Nanogels for Potential Applications in Photothermal Cancer Therapy

Galactosylated PLGA nanoparticles for the oral delivery of resveratrol: enhanced bioavailability and in vitro anti-inflammatory activity

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