release behavior
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2022 ◽  
Vol 15 (1) ◽  
pp. 85
Author(s):  
Xia Niu ◽  
Xiaomei Wang ◽  
Bingyu Niu ◽  
Yucheng Wang ◽  
Hongwei He ◽  
...  

Liver fibrosis is challenging to treat because of the lack of effective agents worldwide. Recently, we have developed a novel compound, N-(3,4,5-trichlorophenyl)-2(3-nitrobenzenesulfonamido) benzamide referred to as IMB16-4. However, its poor aqueous solubility and poor oral bioavailability obstruct the drug discovery programs. To increase the dissolution, improve the oral bioavailability and enhance the antifibrotic activity of IMB16-4, PVPK30 was selected to establish the IMB16-4 nanoparticles. Drug release behavior, oral bioavailability, and anti-hepatic fibrosis effects of IMB16-4 nanoparticles were evaluated. The results showed that IMB16-4 nanoparticles greatly increased the dissolution rate of IMB16-4. The oral bioavailability of IMB16-4 nanoparticles was improved 26-fold compared with that of pure IMB16-4. In bile duct ligation rats, IMB16-4 nanoparticles significantly repressed hepatic fibrogenesis and improved the liver function. These findings indicate that IMB16-4 nanoparticles will provide information to expand a novel anti-hepatic fibrosis agent.


2022 ◽  
Vol 8 ◽  
Author(s):  
Xiaotong Yang ◽  
Haomin Sui ◽  
Hongshan Liang ◽  
Jing Li ◽  
Bin Li

The gel properties of sodium alginate (SA) have been revealed to be strongly correlated with its ratio of D-mannuronate to L-guluronate (M/G ratio). Herein, we focused on SA with different M/G ratios to conduct an in-depth study on the effect of the M/G ratio difference on physicochemical stability and calcium release behavior of the Pickering emulsion stabilized by calcium carbonate (CaCO3). The oil phase was added to the aqueous phase, prepared by SA with different M/G ratios (2.23, 0.89, and 0.56) and CaCO3, for one-step shearing to obtain the E1, E2, and E3 emulsions, respectively. The results of the particle size, microstructure, long-term stability, rheological, and microrheological properties of the emulsions showed that the E3 emulsion, prepared by SA with a smaller M/G ratio, had a smaller particle size and has remained in a flow condition during the long-term storage, while the E1 and E2 emulsions had a gelation behavior and a stronger viscoelasticity. Moreover, the emulsion, as a liquid calcium supplement, is not only convenient for oral intake while meeting the calcium needs of the body, but also controls the release of Ca2+. The calcium release of the emulsions in a simulated gastric environment demonstrated that the calcium release ratio increased with the decrease of SA concentration, with the increase of M/G ratio, and with the decrease of oil phase volume.


2022 ◽  
pp. 52118
Author(s):  
Wen Shen ◽  
Yuanlan Ning ◽  
Xuemei Ge ◽  
Guodong Fan ◽  
Fen Ao ◽  
...  

2021 ◽  
Vol 26 (4) ◽  
pp. 193-199
Author(s):  
dongil choi ◽  
hojoon shin ◽  
soon young kwon

Polymers ◽  
2021 ◽  
Vol 14 (1) ◽  
pp. 41
Author(s):  
Ravinder Kumar ◽  
Agnieszka Najda ◽  
Joginder Singh Duhan ◽  
Balvinder Kumar ◽  
Prince Chawla ◽  
...  

Biopolymeric Chitosan-Carrageenan nanocomposites 66.6–231.82 nm in size containing the chemical fungicide mancozeb (nano CSCRG-M) were synthesized following a green chemistry approach. The physicochemical study of nanoparticles (NPs) was accomplished using a particle size analyzer, SEM and FTIR. TEM exhibited clover leaf-shaped nanoparticles (248.23 nm) with mancozeb on the inside and entrapped outside. Differential scanning calorimetry and TGA thermogravimetry exhibited the thermal behaviour of the nanoform. Nano CSCRG-1.5 at 1.5 ppm exhibited 83.1% inhibition against Alternaria solani in an in vitro study and performed as well as mancozeb (84.6%). Complete inhibition was exhibited in Sclerotinia sclerotiorum at 1.0 and 1.5 ppm with the nanoformulation. The in vivo disease control efficacy of mancozeb-loaded nanoparticles against A. solani in pathogenized plants was found to be relatively higher (79.4 ± 1.7) than that of commercial fungicide (76 ± 1.1%) in pot conditions. Nanomancozeb showed superior efficacy for plant growth parameters, such as germination percentage, root–shoot ratio and dry biomass. The nanoformulation showed higher cell viability compared to mancozeb in Vero cell cultures at 0.25 and 0.50 mg/mL in the resazurin assay. CSCRG-0.5 showed slow-release behavior up to 10 h. Thus, these green nano-based approaches may help combat soil and water pollution caused by harmful chemical pesticides.


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