Nanophytosomes of hesperidin and of hesperetin: Preparation, characterization, and in vivo evaluation.

Hesperidin and hesperetin are two important plant flavanones abundantly found in citrus fruit. They have discovered many biological activities to treat diseases, including cancer, diabetes, and Alzheimer's disease. Despite their various benefits, they have poor solubility, which reduces their bioavailability and absorption. In this study, nanophytosomes have been utilized to improve their payload's solubility and bioavailability. In the current study, hesperetin or hesperidin was complexed with Phospholipon 90G with a 2:1 or 3:1 molar ratio, respectively. The formation of associations between active compounds and phospholipid were confirmed by X-ray diffraction (XRD), Fourier-transform infrared spectroscopy (FTIR), and nuclear magnetic resonance (NMR) techniques. Dynamic light scattering data show that the prepared associations in the presence of body fluids can make nanoparticles in the range of 200-250 nm. In addition, oral administration demonstrated that Cmax of hesperidin and hesperetin was increased (up to four times) after complexation with the lipid. It is concluded that phospholipid association may be used as a suitable and straightforward strategy to improve therapeutic activities of hesperidin and hesperetin by increasing their solubility and bioavailability.

Green synthesis of selenium nanoparticles using Rosmarinus officinalis and investigated their antimicrobial activity.

The interest of many has been attracted by plant-mediated synthesizing procedures for nanoparticles since they provide certain qualities including being cost-effective, quick, and compatible with the environment. In this regard, this work introduces the production of selenium-nanoparticles (Se-NPs) in a biological manner utilizing aqueous extracts of Rosmarinus officinalis (R. officinalis). Production of Se-NPs was confirmed using UV-visible (UV-Vis) spectrophotometry. Also, dynamic light scattering (DLS) analysis was used for determination particle size distribution, while we distinguished the identification of crystalline construction of nanoparticles through the means of X-ray diffraction (XRD) pattern, DLS, and transmission electron microscopy (TEM) examination indicated that Se-NPs are often spherical with a size about 20 to 40 nm. The minimum inhibitory concentration (MIC) of the synthesized Se-NPs by R. officinalis extract against Mycobacterium tuberculosis (M. tuberculosis), Staphylococcus aureus (S. aureus), Streptococcus mutans (S. mutans), Escherichia coli (E. coli), and Pseudomonas aeruginosa (P. aeruginosa) was 256, 16, 32, 128, and 64 µg/mL, respectively. The synthesized Se-NPs had no significant effect on Mycobacterium simiae (M. simiae) and had exhibited a strong antimicrobial functionality towards the gram-positive and gram-negative bacteria and can stand as a potent antibacterial agent.

Anti-mycobacterial Activity of 22 Iranian Endemic or Rare Plant Extracts Against Multi-drug and Extensively Drug-resistant Mycobacterium tuberculosis.

BACKGROUND: Due to side-effects and low efficacy of common drugs on new resistant strains of Mycobacterium tuberculosis (Mtb), investigation on novel drugs and natural compounds from rich sources of endemic plants is required. Thus, in the present study, the anti-mycobacterial effects of 22 Iranian endemic or rare plant extracts on multi-drug resistance (MDR) and extensively-drug resistance (XDR) Mtb isolates were evaluated. METHODS: Twenty-two Iranian endemic and rare plant species from 9 families were collected and extracted by methanol. Their inhibitory-effects were then evaluated against Mtb H37Rv strain, seven clinical MDR-TB, and two XDR-TB isolates using the resazurin microtiter assay (REMA) method. The best of them were then fractionalized by five different polar solvents (Petroleum- Ether, Dichloromethane, Ethyl-Acetate, n-butanol, and water). To find anti-mycobacterial fractions, the inhibitory effect of isolated fractions was tested on Mtb H37Rv. RESULTS: Out of the 22 plants, 14 plant extracts demonstrated anti-mycobacterial activity with minimum inhibitory concentration (MIC) ranging from 4 to 30µg/mL against Mtb H37Rv. Eight plant extracts also exhibited anti-mycobacterial activity against MDR and XDR clinical strains of Mtb by MICs, i.e., 15-60µg/ml. Crinitaria grimmii and Linum album were the best antimycobacterial plants. Among fractions of Crinitaria grimmii, dichloromethane and n-butanol, and for Linum album, dichloromethane and Ethyl-Acetate fractions displayed more anti-mycobacterial effect as compared to crude extract on Mtb. CONCLUSION: The present study confirms the potential role of some plants to treat respiratory diseases as our results have demonstrated that these plants exhibit anti-mycobacterial activity in the acceptable range against Mtb. Thus, these plants could be good sources and alternatives of plant metabolites for anti-TB-drug development.

Implementation of design of experiments for optimization of forced degradation conditions and development of a stability-indicating high-performance liquid chromatography method for sepiwhite.

Sepiwhite is a novel anti-pigmenting agent that is derived from fatty acid and phenylalanine and used for hyperpigmentation induced by light exposure or inflammation. In this study, a simple and validated high-performance liquid chromatography method for the quantitation of sepiwhite was developed. Optimized forced degradation of sepiwhite at thermal, acid/base, photolysis, oxidative, and heavy metal ions conditions were evaluated and the effect of each of them on production of specific 10%-30% degradants was studied by the approach of design of experiments. Sepiwhite accelerated study was conducted and toxicity of sepiwhite at each condition was tested. An optimized high-performance liquid chromatography method was validated by a face-centered central composition design. Ten different degradants were identified from sepiwhite and degradation behavior under different conditions was studied. Sepiwhite and its degradant products show no cytotoxicity. This optimized high-performance liquid chromatography method can be applied for quality control assay and sepiwhite degradation behavior may be considered in the manufacturing of sepiwhite products.

Therapeutic effect of an anti-tuberculosis agent, isoniazid, and its nano-isoform in ulcerative colitis.

BACKGROUND: Isoniazid (INH) is well known as a first-line anti-tuberculosis, while some studies demonstrate that it has anti-inflammatory activity via a different mechanism such as inhibitionthe production of IL-1, ROS, activation of PPARγ expression, inhibition of the transcriptional regulatory activity of NF-κB and AP-1. The aim of this study, investigate the anti-inflammatory effect of INH and INH combined with Sulfasalazine-loaded nanoparticles (NPs) in the ulcerative colitis mouse model. METHODS: To investigate the anti-inflammatory effect of INH and NPs in the ulcerative colitis mice model, we evaluated the effect of INH clinical symptoms and colonic mucosal histology in colitis. RESULT: The present study demonstrates that combination therapy of INH with sulfasalazine as well as NPs reduces the symptom of ulcerative colitis and improved disease activity index include body lose weight, diarrhea, rectal bleeding, colonic length, spleen weight, and colon histopathological score in DSS-induced colitis mice model. CONCLUSION: Our results suggest that the nanoforms of INH with sulfasalazine enhances the therapeutic effect of the drugs in the treatment of ulcerative colitis.