Publications by authors named "L Ebralidze"

26 Publications

FORMULATION THERMORESPONSIVE NANOCOMPOSITE HYDROGELWITH EMBEDDED PLGA NANOPARTICLES CONTAINING CYTOTOXIC AGENT.

Georgian Med News 2021 Mar(312):133-138

Tbilisi State Medical University, Faculty of Pharmacy, 1Department of Pharmaceutical Technology; Georgia.

The aim of the study was to develop and characterize the nanocomposite in-situ hydrogel as local drug delivery system of cytotoxic agent. In-situ hydrogel consisting of 15% thermosensitive (Poloxamer 407) and 1% mucoadhesive (sodium alginate) polymers was selected as the optimal formulation by the conducted studies. The influence of nanoparticle concentration on gelation time and temperature has been experimentally established. As a result, the optimum concentration of nanoparticles (5%) is selected, which does not alter the gel forming process. The resulting nanocomposite hydrogel was characterized through Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), rotational viscometer (LVDV-1T). FT-IR spectra confirmed the PLGA nanoparticles presence within the hydrogel matrix through the absorption peak located at 1750 cm-1. SEM images allowed observing the nanoparticles to be homogenously dispersed. The release pattern of the active substance from the nanocomposite hydrogel is following: at 72 h, 64% and 78% of the active substance were released into the phosphate buffer and cell culture area, respectively. Irritation test on hen's egg model revealed that formulated nanocomposite hydrogel did not show damage of vascular system.
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March 2021

BIOPHARMACEUTICAL UNDERSTANDING OF FORMULATION PREPARATION VARIABILITY OF PLGA NANOPARTICLES LOADED WITH ERYSIMUM EXTRACT.

Georgian Med News 2021 Feb(311):173-177

Tbilisi State Medical University, Faculty of Pharmacy, 1Department of Pharmaceutical Technology; Faculty of Pharmacy, 2Direction of Pharmacognosy and pharmaceutical botany, Georgia.

The purpose of this study was to evaluate effect of process and formulation variables on the preparation of Erysimum extract loaded PLGA nanoparticles. The influence of the various biopharmaceutical factors such as type of organic solvent, type and concentration of surfactant, polymer concentration in the organic phase, ratio of organic phase and water phase were studied. Modified emulsification solvent evaporation method was used for preparation of nanoparticles. Based on the performed experiments optimal formulation of nanocomposite is suggested. Nanoparticle size, size distribution and entrapment efficiency were determined. Among five non-ionic surfactants polyvinyl alcohol provided more stable nanocomposite. Influence mechanisms of different surfactants on nanoparticle formation are provided. Water miscible organic solvent, acetone obtained 232 nm nanoparticles with improved size distribution. Entrapment efficiency was increased to 73% by reducing ratio of organic and water phases. Based on experiments nanoparticles with stable, reproducible properties are fabricated.
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February 2021

The Comparative Analysis of Antiviral Activity of Native and Modified Fucoidans from Brown Algae In Vitro and In Vivo.

Mar Drugs 2020 Apr 22;18(4). Epub 2020 Apr 22.

G.P. Somov Institute of Epidemiology and Microbiology, 690087 Vladivostok, Russia.

The enzymatic depolymerization of fucoidans from brown algae allowed the production of their standardized derivatives with different biological activities. This work aimed to compare the antiviral activities of native (FeF) and modified with enzyme (FeHMP) fucoidans from . The cytotoxicity and antiviral activities of the FeF and FeHMP against herpes viruses (HSV-1, HSV-2), enterovirus (ECHO-1), and human immunodeficiency virus (HIV-1) in Vero and human MT-4 cell lines were examined by methylthiazolyltetrazolium bromide (MTT) and cytopathic effect (CPE) reduction assays, respectively. The efficacy of fucoidans in vivo was evaluated in the outbred mice model of vaginitis caused by HSV-2. We have shown that both FeF and FeHMP significantly inhibited virus-induced CPE in vitro and were more effective against HSV. FeF exhibited antiviral activity against HSV-2 with a selective index (SI) > 40, and FeHMP with SI ˃ 20, when they were added before virus infection or at the early stages of the HSV-2 lifecycle. Furthermore, in vivo studies showed that after intraperitoneal administration (10 mg/kg), both FeF and FeHMP protected mice from lethal intravaginal HSV-2 infection to approximately the same degree (44-56%). Thus, FeF and FeHMP have comparable potency against several DNA and RNA viruses, allowing us to consider the studied fucoidans as promising broad-spectrum antivirals.
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http://dx.doi.org/10.3390/md18040224DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7230360PMC
April 2020

FORMULATION OF BIODEGRADABLE POLYMERIC NANOPARTICLES CONTAINING CYTOTOXIC SUBSTANCE OF PLANT ORIGIN.

Georgian Med News 2020 Feb(299):137-142

Tbilisi State Medical University, 1Department of Pharmaceutical Technology, Georgia.

Formulation of novel drug delivery system is one of the approaches for improvement of pharmacological activity of drugs. This implies encapsulation of the API into the biocompatible polymeric material. Objective of the research was formulation of biodegradable amino acid based polyesteramide nanoparticles composing cytotoxic substance of plant origin. Research materials and methods: biodegradable polyesteramide (PEA), alkaloids from Vinca Minor, surfactants (Tween 80, polyvinyl pirolidone, polyvinyl alcohol, Poloxamer 188). NPs size (mean particle diameter) and size distribution (polydispersity index, PDI), and zeta-potential (ZP) were measured by dynamic light scattering (DLS) using a Zetasizer Nano ZS (Malvern Instruments, U.K.) at 25°C, UV spectrophotometer was used for %EE study. Amino acid based PEA particles were fabricated by the modified emulsification method. Based on the studies optimal composition and fabrication condition of PEA NPs was determined. The conditions of the NPs fabrication were as follows: the O/W ratio: 1:10; the solvent: DMSO; polymer concentration in the organic phase: 50.0 mg/mL; surfactants (PVA) concentration in aqueous phase 0.5%,the stirring rate: 1000 rpm. The influence of the various factors such as organic solvents, surfactants, as well as a polymer concentration in the organic phase,surfactant concentration in the aqueous phase,the organic/water phase ratio on the NPs fabrication was studied.The NPs were characterized by size (mean particle diameter & size distribution (polydispersity index, PDI), and zeta-potential (ZP). Increase concentration of the surfactant (polyvinyl alcohol) from 0.1% to 0.5% decrease average particle size from 568±63 to 169±1.66 respectively. EE% was obtained to be around 50%.
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February 2020

Antiviral and Antioxidant Properties of Echinochrome A.

Mar Drugs 2018 Dec 15;16(12). Epub 2018 Dec 15.

G.P. Somov Institute of Epidemiology and Microbiology, FEB RAS, Vladivostok 690087, Russia.

The aim of this study was to examine the in vitro antioxidant and antiviral activities of echinochrome A and echinochrome-based antioxidant composition against tick-borne encephalitis virus (TBEV) and herpes simplex virus type 1 (HSV-1). The antioxidant composition, which is a mixture of echinochrome A, ascorbic acid, and α-tocopherol (5:5:1), showed higher antioxidant and antiviral effects than echinochrome A. We suppose that echinochrome A and its composition can both directly affect virus particles and indirectly enhance antioxidant defense mechanisms in the hosting cell. The obtained results allow considering the echinochrome A and the composition of antioxidants on its basis as the promising agents with the both antioxidant and antiviral activities.
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http://dx.doi.org/10.3390/md16120509DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6315383PMC
December 2018