Research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics: size, surface charge and pro-hydrophobics

Guo, Shiwei; Yu, Lintao; Liu, Lanze; Yin, Miaomiao; Wang, Aiping; Sun, Kaoxiang; Li, Youxin; Shi, Yanan

doi:10.1186/s12951-021-00770-2

Cited by 67 publications

(36 citation statements)

References 62 publications

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“…PDI of the optimized formulation was observed as 0.1, indicating the uniform population size owing to the strong repellent forces between the nanoparticles which in turn is due to high electrostatic charge (Shetta et al, 2019). of the present study (+49.8 mv) may contribute to physical stability of nanoparticles with longer retention in the GI tract due to the presence of higher surface cationic charge (Guo et al, 2021). The nanodrugs with positive ZP have higher cell uptake because of increased permeability and retention value i.e.…”

Section: Size Zeta Potential and Poly Dispersion Indexmentioning

confidence: 53%

Development of nano‐encapsulated green tea catechins: Studies on optimization, characterization, release dynamics, and in‐vitro toxicity

et al. 2021

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Green tea (Camelia sinesis) has been acknowledged for plethora of pharmacological activities attributed by green tea catechins (GTC), however, poor bioavailability, short half-life and stability issues hamper its use as a therapeutic agent. Chitosan and sodium -tripolyphosphate were used to encapsulate GTC, which reduced its degradation in gastro-intestinal tract. The average size, zeta potential, and encapsulation efficiency of nano-encapsulated epigallocatechin-3-gallate (EGCG) rich GTC were observed as 250 nm, +49.8 mV, and 87%, respectively. The morphological and physicochemical characterizations affirmed the size, stability, and encapsulation efficacy of nano-encapsulated green tea catechins. The In-vitro simulated release model showed the release of GTC in the intestinal phase via zero order kinetics. Cell viability studies were conducted on PC12 cell line to validate safety efficacy of nanoencapsulated GTC. Moreover, the study concluded that stability, bioavailability and bioactivity of EGCG was improved by nanoencapsulation of GTC, thereby rendering it a potent nanoceutical for clinical implications. Practical applicationsGreen tea catechin has enormous health endorsing activities. One of the major potentials of GTC is its antioxidant activity that plays a promising role in the prevention of various lethal disorders. In the present study, nanoencapsulation is used as a potential approach to improve the low bioavailability of green tea catechin. The results enlightened that nanoencapsulation of green tea catechin could be useful for improving the stability of green tea catechin in the GI tract as well as its bioaccessibility. Henceforth, this strategy restores the stability and bioavailability of green tea catechin that could be practically implied as a nutraceutical in the food and pharmaceutical industry as it can enhance the biological activity of catechins in catechin rich green tea-related products.

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Section: Size Zeta Potential and Poly Dispersion Indexmentioning

confidence: 53%

Development of nano‐encapsulated green tea catechins: Studies on optimization, characterization, release dynamics, and in‐vitro toxicity

et al. 2021

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“…Analysis of Figure 6(C) reveals that the extent of absorption of H-LNPS and LNPS was greater than the extent of absorption of D-NPS. The results revealed that during in vivo intestinal circulation in the presence of mucus, the extent of absorption of D-NPS was higher than H-LNPS and LNPS, and during in vitro flip-flop intestinal circulation, the extents of absorption of H-LNPS and LNPS were higher than D-NPS (attributable to the removal of the mucus layer) (Guo et al., 2021 ).…”

Section: Resultsmentioning

confidence: 99%

Orally administered intelligent self-ablating nanoparticles: a new approach to improve drug cellular uptake and intestinal absorption

Ding

Liu

et al. 2022

Drug Delivery

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Oral drug delivery to treat diabetes is being increasingly researched. The mucus and the epithelial cell layers hinder drug delivery. We designed a self-ablating nanoparticle to achieve smart oral delivery to overcome the gastrointestinal barrier. We used the zwitterionic dilauroyl phosphatidylcholine, which exhibits a high affinity toward Oligopeptide transporter 1, to modify poly(lactic-co-glycolic acid) nanoparticles and load hemagglutinin-2 peptide to facilitate its escape from lysosomes. Nanoparticles exhibit a core–shell structure, the lipid layer is degraded by the lysosomes when the nanoparticles are captured by lysosomes, then the inner core of the nanoparticles gets exposed. The results revealed that the self-ablating nanoparticles exhibited higher encapsulation ability than the self-assembled nanoparticles (77% vs 64%) and with better stability. Quantitative cellular uptake, cellular uptake mechanisms, and trans-monolayer cellular were studied, and the results revealed that the cellular uptake achieved using the self-ablating nanoparticles was higher than self-assembling nanoparticles, and the number of uptake pathways via which the self-ablating nanoparticles functioned were higher than the self-assembling nanoparticles. Intestinal mucus permeation, in vivo intestinal circulation, was studied, and the results revealed that the small self-assembling nanoparticles exhibit a good extent of intestinal uptake in the presence of mucus. In vitro flip-flop, intestinal circulation revealed that the uptake of the self-ablating nanoparticles was 1.20 times higher than the self-assembled nanoparticles. Pharmacokinetic study and the pharmacodynamic study showed that the bioavailability and hypoglycemic effect of self-ablating nanoparticles were better than self-assembled nanoparticles.

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“…Since the surface charges and sizes of the complexes would affect cell uptake to the complexes, the zeta potentials and particle sizes of CBSF/pDNA complexes at different mass ratios were tested [ 38 ], as shown in Figure 4 B. The zeta potential of naked pDNA was −20.9 ± 0.4 mV.…”

Section: Resultsmentioning

confidence: 99%

Polyethylenimine-Modified Bombyx mori Silk Fibroin as a Delivery Carrier of the ING4-IL-24 Coexpression Plasmid

et al. 2021

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One of the major challenges for lung cancer gene therapy is to find a gene delivery vector with high efficiency and low toxicity. In this study, low-molecular-weight polyethyleneimine (PEI, 1.8 kDa) was grafted onto the side chains of Bombyx mori silk fibroin (BSF) to prepare cationized BSF (CBSF), which was used to package the plasmid DNA (pDNA) encoded by the inhibitor of growth 4 (ING4) and interleukin-24 (IL-24). FTIR and 1H-NMR spectra demonstrated that PEI was effectively coupled to the side chains of BSF by amino bonds. The results of the trinitrobenzene sulfonic acid method and zeta potential showed that the free amino group content on BSF increased from 125.1 ± 1.2 µmol/mL to 153.5 ± 2.2 µmol/mL, the isoelectric point increased from 3.68 to 8.82, and the zeta potential reversed from − 11.8 ± 0.1 mV to + 12.4 ± 0.3 mV after PEI grafting. Positively charged CBSF could package pDNA to form spherical CBSF/pDNA complexes. In vitro, human lung adenocarcinoma A549 cells and human embryonic lung fibroblast WI-38 cells were transfected with CBSF/pDNA complexes. Confocal laser scanning microscopy analysis and flow cytometry tests showed that CBSF/pDNA complexes can effectively transfect A549 cells, and the transfection efficiency was higher than that of 25 kDa PEI/pDNA complexes. CCK-8 assay results showed that CBSF/pDNA complexes significantly inhibited the proliferation of A549 cells but had no significant effect on WI-38 cells and exhibited lower cytotoxicity to WI-38 cells than 25 kDa PEI. Therefore, a gene delivery system, constructed with the low-molecular-weight PEI-modified silk fibroin protein and the ING4-IL-24 double gene coexpression plasmid has potential applications in gene therapy for lung cancer.

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Research on the fate of polymeric nanoparticles in the process of the intestinal absorption based on model nanoparticles with various characteristics: size, surface charge and pro-hydrophobics

Cited by 67 publications

References 62 publications

Development of nano‐encapsulated green tea catechins: Studies on optimization, characterization, release dynamics, and in‐vitro toxicity

Development of nano‐encapsulated green tea catechins: Studies on optimization, characterization, release dynamics, and in‐vitro toxicity

Orally administered intelligent self-ablating nanoparticles: a new approach to improve drug cellular uptake and intestinal absorption

Polyethylenimine-Modified Bombyx mori Silk Fibroin as a Delivery Carrier of the ING4-IL-24 Coexpression Plasmid

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