scholarly journals In Vitro Bioeffects of Polyelectrolyte Multilayer Microcapsules Post-Loaded with Water-Soluble Cationic Photosensitizer

Pharmaceutics ◽  
2020 ◽  
Vol 12 (7) ◽  
pp. 610 ◽  
Author(s):  
Alexey V. Ermakov ◽  
Roman A. Verkhovskii ◽  
Irina V. Babushkina ◽  
Daria B. Trushina ◽  
Olga A. Inozemtseva ◽  
...  

Microencapsulation and targeted delivery of cytotoxic and antibacterial agents of photodynamic therapy (PDT) improve the treatment outcomes for infectious diseases and cancer. In many cases, the loss of activity, poor encapsulation efficiency, and inadequate drug dosing hamper the success of this strategy. Therefore, the development of novel and reliable microencapsulated drug formulations granting high efficacy is of paramount importance. Here we report the in vitro delivery of a water-soluble cationic PDT drug, zinc phthalocyanine choline derivative (Cholosens), by biodegradable microcapsules assembled from dextran sulfate (DS) and poly-l-arginine (PArg). A photosensitizer was loaded in pre-formed [DS/PArg]4 hollow microcapsules with or without exposure to heat. Loading efficacy and drug release were quantitatively studied depending on the capsule concentration to emphasize the interactions between the DS/PArg multilayer network and Cholosens. The loading data were used to determine the dosage for heated and intact capsules to measure their PDT activity in vitro. The capsules were tested using human cervical adenocarcinoma (HeLa) and normal human dermal fibroblast (NHDF) cell lines, and two bacterial strains, Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli. Our results provide compelling evidence that encapsulated forms of Cholosens are efficient as PDT drugs for both eukaryotic cells and bacteria at specified capsule-to-cell ratios.

2018 ◽  
Vol 2018 ◽  
pp. 1-11 ◽  
Author(s):  
Dominika Wcisło-Dziadecka ◽  
Beniamin Grabarek ◽  
Nikola Zmarzły ◽  
Aleksandra Skubis ◽  
Bartosz Sikora ◽  
...  

Objective. The aim of this study was to evaluate the influence of adalimumab on expression profile of genes associated with the histaminergic system in Normal Human Dermal Fibroblast (NHDF) cells stimulated with 8.00 μg/ml of adalimumab and the identification of miRNAs regulating these genes’ expression. Methods. NHDFs were cultured with or without the presence of adalimumab for 2, 8, and 24 hours. The expression profile of genes and miRNA were determined with the use of microarray technology. Results. Among 22283 ID mRNA, 65 are associated with the histaminergic system. It can be observed that 15 mRNAs differentiate NHDFs cultures with adalimumab form control. The analysis of miRNAs showed that, among 1105 ID miRNA, 20 miRNAs are differentiating in cells treated with adalimumab for 2 hours, 9 miRNA after 8 hours, and only 3 miRNAs after 24 hours. Conclusion. It was also determined that miRNAs play certain role in the regulation of the expression of genes associated with the histaminergic system. The results of this study confirmed the possibility of using both genes associated with this system as well as miRNAs regulating their expression, as complementary molecular markers of sensitivity to the adalimumab treatment.


Pharmaceutics ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 570 ◽  
Author(s):  
Irem Unalan ◽  
Stefan J. Endlein ◽  
Benedikt Slavik ◽  
Andrea Buettner ◽  
Wolfgang H. Goldmann ◽  
...  

The objective of this study was to produce antibacterial poly(ε-caprolactone) (PCL)-gelatin (GEL) electrospun nanofiber mats containing clove essential oil (CLV) using glacial acetic acid (GAA) as a “benign” (non-toxic) solvent. The addition of CLV increased the fiber diameter from 241 ± 96 to 305 ± 82 nm. Aside from this, the wettability of PCL-GEL nanofiber mats was increased by the addition of CLV. Fourier-transform infrared spectroscopy (FTIR) analysis confirmed the presence of CLV, and the actual content of CLV was determined by gas chromatography–mass spectrometry (GC-MS). Our investigations showed that CLV-loaded PCL-GEL nanofiber mats did not have cytotoxic effects on normal human dermal fibroblast (NHDF) cells. On the other hand, the fibers exhibited antibacterial activity against Staphylococcus aureus and Escherichia coli. Consequently, PCL-GEL/CLV nanofiber mats are potential candidates for antibiotic-free wound healing applications.


2018 ◽  
Vol 17 (3) ◽  
pp. 229-235
Author(s):  
Z.A. Mat Yasin ◽  
A.S. Khazali ◽  
F. Ibrahim ◽  
N. Nor Rashid ◽  
R. Yusof

Medicinal plants have been traditionally used for various applications including skin care. In this study, Areca catechu, Boesenbergia rotunda, Piper betle and Orthosiphon aristatus were tested for antioxidant and anti-aging properties. These plant extracts were subjected to 1,1-diphenyl-picrylhydrazyl (DPPH) and 2,2ʹ-azinobis(3-ethylbenzothiazoline)-6-sulphonic acid (ABTS) radical scavenging activity analyses. The extracts were then assessed for collagenase, elastase and hyaluronidase inhibition and subjected to toxicity study in normal human dermal fibroblast cells. Lastly, bioactive compounds in these plant extracts were identified using high performance liquid chromatography. We found that Piper betle and Areca catechu possessed high total flavonoid and phenolic contents. These two extracts showed the best IC50 values for DPPH and ABTS radical scavenging activities and also demonstrated the highest elastase and collagenase inhibition when compared to the other two plant extracts. These crude plants extracts were also non-toxic to normal human dermal fibroblast cells. Our HPLC results identified several potential bioactive compounds in these plant extracts that could be crucial in mediating the observed effects. Based on our results, these plant extracts especially Piper betle and Areca catechu extracts possess significant antioxidant and anti-aging properties and could be utilized in the development of safe and cost-effective anti-aging treatments.


Materials ◽  
2019 ◽  
Vol 12 (23) ◽  
pp. 3907 ◽  
Author(s):  
Sgarbossa ◽  
Śliwińska-Hill ◽  
Guedes da ilva ◽  
Bażanów ◽  
Pawlak ◽  
...  

From the well-known 1,3,5-triaza-phosphaadamantane (PTA, 1a), the novel N-allyl and N-benzyl tetrafuoroborate salts 1-allyl-1-azonia-3,5-diaza-7-phosphaadamantane (APTA(BF4), 1b) and 1-benzyl-1-azonia-3,5-diaza-7-phosphaadamantane (BzPTA(BF4), 1c) were obtained. These phosphines were then allowed to react with (Pt(μ-Cl)(C6F5)(tht))2 (tht = tetrahydrothiophene) affording the water soluble Pt(II) complexes trans-(PtCl(C6F5)(PTA)2) (2a) and its bis-cationic congeners trans-(PtCl(C6F5)(APTA)2)(BF4)2 (2b) and trans-(PtCl(C6F5)(BzPTA)2)(BF4)2 (2c). The compounds were fully characterized by multinuclear NMR, ESI-MS, elemental analysis and (for 2a) also by single crystal X-ray diffraction, which proved the trans configuration of the phosphine ligands. Furthermore, in order to evaluate the cytotoxic activities of all complexes the normal human dermal fibroblast (NHDF) cell culture were used. The antineoplastic activity of the investigated compounds was checked against the human lung carcinoma (A549), epithelioid cervix carcinoma (HeLa) and breast adenocarcinoma (MCF-7) cell cultures. Interactions between the complexes and human serum albumin (HSA) using fluorescence spectroscopy and circular dichroism spectroscopy (CD) were also investigated.


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