Gong (2019) Codelivery of DOX and siRNA by folate-biotinquaternized starch nanoparticles for promoting synergistic suppression of human lung cancer cells,

In this paper, a new oral insulin formulation, insulin-loaded carboxymethyl-b-cyclodextrin-grafted chitosan nanoparticles (insulin/CMCD-g-CS NPs), was fabricated by ionic crosslinking technique. The therapeutic efficacy of new formulation was investigated in detail. Firstly, the CMCD-g-CS was synthesized by EDC-mediated esterification reaction. The prepared CMCD-g-CS exhibited favourable loading capacity and encapsulation efficiency of drug. The release experiment in vitro showed that the nanocarrier could efficiently protect encapsulated insulin at simulated gastric environment and release drug in the simulated colonic fluid. The insulin/CMCD-g-CS NPs effectively promoted drug internalization into Caco-2 cells and could reversibly open the tight junction between cells. The oral administration of insulin/CMCD-g-CS NPs could lastingly decrease blood sugar level in diabetic mice. The liver function study verified that the insulin/CMCD-g-CS NPs had not obvious toxicity to experimental mice. Therefore, the CMCD-g-CS could be an effective and safe oral insulin delivery carrier for future clinical application.A new biocompatible polysaccharide nanoparticle was fabricated as oral insulin delivery carrier for improving diabetic treatment.

The present study aimed to estimate the antiviral activities of Ginkgo biloba (GB) leaves extract and eco-friendly free silver nanoparticles (Ag NPs) against the MERS-CoV (Middle East respiratory syndrome-coronavirus) and HCoV-229E (human coronavirus 229E), as well as isolation and identification of phytochemicals from GB. Different solvents and high-performance liquid chromatography (HPLC) were used to extract and identify flavonoids and phenolic compounds from GB leaves. The green, silver nanoparticle synthesis was synthesized from GB leaves aqueous extract and investigated for their possible effects as anti-coronaviruses MERS-CoV and HCoV-229E using MTT assay protocol. To verify the synthesis of Ag NPs, several techniques were employed, including X-ray diffraction (XRD), scan, transmission electron microscopy, FT-IR, and UV–visible spectroscopy. The highest contents of flavonoids and phenolic compounds were recorded for acetone, methanol, and ethanol as mixtures with water, in addition to pure water. HPLC flavonoids were detected as apegenin, luteolin, myricetin, and catechin, while HPLC phenolic compounds were pyrogallol, caffeic acid, gallic acid, and ellagic acid. In addition, our results revealed that Ag NPs were produced through the shift from yellow to dark brown. TEM examination of Ag NPs revealed spherical nanoparticles with mean sizes ranging from 5.46 to 19.40 nm and an average particle diameter of 11.81 nm. A UV–visible spectrophotometric investigation revealed an absorption peak at λ max of 441.56 nm. MTT protocol signified the use of GB leaves extract as an anti-coronavirus to be best from Ag NPs because GB extract had moderate anti-MERS-CoV with SI = 8.94, while had promising anti-HCov-229E, with an SI of 21.71. On the other hand, Ag NPs had a mild anti-MERS-CoV with SI = 4.23, and a moderate anti-HCoV-229E, with an SI of 7.51.

Recently, the green synthesis of nanomaterials has grown in popularity and has become one of the most used approaches. Plant extracts are safe for the environment and could be cost-effective for nanoparticle preparation. Silver nanoparticles (AgNPs) have been synthesized using aqueous extracts of Nigella sativa (N. sativa) seeds. The formation of AgNPs was confirmed by using an X-ray diffractometer, a UV-visible spectrometer, and a transmission electron microscope. The phytotoxicity and genotoxicity of different AgNP concentrations (12.5, 25, 50, 75, and 100 μg·L−1) were evaluated by wheat (Triticum aestivum L.) seed germination. The results showed that AgNPs did not significantly affect germination, while root and coleoptile lengths decreased considerably. On the contrary, the biomass of seedlings markedly increased in response to AgNP treatments. Moreover, genotoxicity was detected, especially at high concentrations of AgNPs. DNA, RNA, and total soluble proteins of wheat seedlings significantly decreased. In addition, antimicrobial activities of biosynthesized AgNPs were detected.

In this work, folate-phytosterol-carboxymethyl cellulose nanoparticles (FPCMC NPs) derived from plant material were fabricated and investigated as carrier of hydrophobic anticancer drugs. Firstly, hydrophobic phytosterol was grafted onto the framework of water-soluble carboxymethyl cellulose. Then folate, as tumor-targeting ligand, was coupled to the phytosterol-carboxymethyl cellulose to become selfassembled FPCMC NPs. The physicochemical properties of the fabricated FPCMC NPs were characterized. Doxorubicin (DOX) was selected as model anticancer drug that was entrapped in prepared FPCMC NPs with satisfactory loading content (7%) and loading efficiency (71.2%). The in vitro drug release test showed that the release amount of DOX from drug-loaded FPCMC NPs at pH 5.3 was much higher than that at pH 6.5 or pH 7.4. The research results indicated that the fabricated FPCMC NPs had the potential as nanocarrier of hydrophobic anticancer drugs for further experimental study.

As a result of the emergence of new virus strains and the synthetics, virus infections pose significant global health challenges, so the need for new therapeutic drugs rises as new vi and bacterial infectious diseases emerge. This study aimed to synth extract and investigate their possible antiviral and antibacterial properties. X microscopy, and UV-Visible spectroscopy were used to validate the synthesis of Ag-NPs production through the shift from yellow color to dark brown color. TEM examination of Ag nanoparticles with mean sizes ranging from 2 to 9 nm and an average particle diameter of 2.5 spectrophotometric investigation revealed an absorption peak at action against the four studied bacteria, with the inhibition zones for Bacillus subtilis ranging from 6 to 25 mm, Staphylococcus aureus from 8 to 25 mm, and Escherichia coli from 10 to 19 mm, whereas Pseudomonas aeruginosa has shown resistance to the AgNPs solution. The MBC varied from 22.3 to 36.8 nanoparticles against the chosen bacterial strains ranged from 5.7 to 10.2 concentration (MNTC) of Ag-NPs, 10.56 µg/mL, the greenly generated Ag antiviral efficacy against HSV-1, HAV, and adenovirus Finally, The novelty in this study is the application of silver nanoparticles as an antiviral against HSV adenovirus because of the high mutation of viruses.

In this paper, the β-cyclodextrin (β-CD) and biotin (Bi) were successfully grafted onto carboxymethyl chitosan (CMCS). And then the β-CD-Bi-CMCS nanoparticles (NPs) were prepared as oral nano-delivery carrier of protein drugs by ionic gelation method. The morphological feature of fabricated drug carrier was determined by dynamic light scattering and transmission electron microscopy. The result showed that the prepared NPs presented spherical structure with an average diameter of 138 nm. Bovine serum albumin (BSA) was selected as model protein drug that was entrapped in prepared drug carrier with satisfactory entrapment efficiency (79.18%) and loading content (3.96%). The drug release profiles of BSA/β-CD-Bi-CMCS NPs were studied at different pH environment for simulated gastric fluid (SGF), simulated intestinal fluid (SIF) and simulated colonic fluid (SCF). It was found that the BSA/β-CD-Bi-CMCS NPs displayed a pH dependent drug release profiles. After 72 h, the cumulative release amount of BSA in SGF, SIF, and SCF was about 20.57, 74.46, and 91%, respectively. Furthermore, the enzymatic degradation and cytotoxicity studies showed the synthesized β-CD-Bi-CMCS NPs had high chemical stability and biocompatibility. This work indicated that the β-CD-Bi-CMCS NPs had the potentiality as promising nanocarriers for oral delivery of protein drugs.

Purpose: To study the in vitro anticancer effect of doxorubicin-loaded folate-phytosterol-carboxymethyl cellulose nanoparticles (DOX/FPCMC NPs), alone and in combination with the antimalarial drug hydroxychloroquine (HCQ) on human lung cancer cells (A549 cells). Methods: Human lung adenocarcinoma A549 cell line was treated with blank FPCMC NPs, HCQ, free DOX, DOX/FPCMC NPs, free DOX + HCQ or DOX/FPCMC NPs + HCQ. The concentrations of HCQ, DOX and FPCMC NPs varied within the ranges of 20-120 μmol/L, 2-12 mg/L and 50-500 mg/L, respectively. Cell viability and free folate competitive inhibition were determined using MTT assay. Cell proliferation and migration were investigated with wound healing assay, while confocal laser scanning microscopy (CLSM) was used to determine cellular uptake of drugs. Results: In all formulations, the DOX/FPCMC NPs + HCQ produced the highest cytotoxicity in A549 cells due to high cytotoxicity arising from folate-receptor-mediated endocytosis and HCQ-induced inhibition of autophagy. Free folate competitively inhibited the cytotoxicity of DOX/FPCMC NPs on A549 cells. Wound healing assay showed that A549 cells treated with DOX/FPCMC NPs + HCQ had the lowest cell levels of proliferation and migration capacity. The cellular uptake of DOX/FPCMC NPs by A549 cells was higher than that of free DOX. Conclusion: The combination of DOX/FPCMC NPs and HCQ produced the best antitumor effect and had a promising potential for reversal of MDR Keywords: Folate-phytosterol-carboxymethyl cellulose, Doxorubicin, Hydroxychloroquine, Anticancer, Lung cancer