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Sustained-release drugs against tuberculosis are a promising approach to therapy since they positively affect patient compliance with long regimens, especially when it comes to the multidrug-resistant form of the disease. Conventional UV-visible spectroscopy does not work well with multicomponential culture media used for growing M. tuberculosis. The aim of this study was to develop a method for evaluating the kinetics of anti-tuberculosis drug released from bioresorbable polymeric carriers suitable for screening a wide range of encapsulated prolonged-release drugs and identifying the best performing candidate. While studying the growth dynamics of the laboratory susceptible strain M. tuberculosis H37Rv in the presence of different levofloxacin concentrations (from 0.03 to 0.4 μg/ml), we developed a model, which is essentially a set of 2 parallel experiments evaluating the kinetics of drug release into the culture medium. The results of these 2 experiments conducted on 3 encapsulated forms of levofloxacin loaded onto bioresorbable polymeric PLGA carriers (particles sized 50 μm and 100 μm and the matrix) revealed that release kinetics of the drug largely depended on the type of polymeric carrier. The best encapsulation of the antibiotic and its gradual release into the culture medium was observed for the matrix. All experiments were run in 3 replicates. The obtained data were analyzed using descriptive statistics.
Sustained-release drugs against tuberculosis are a promising approach to therapy since they positively affect patient compliance with long regimens, especially when it comes to the multidrug-resistant form of the disease. Conventional UV-visible spectroscopy does not work well with multicomponential culture media used for growing M. tuberculosis. The aim of this study was to develop a method for evaluating the kinetics of anti-tuberculosis drug released from bioresorbable polymeric carriers suitable for screening a wide range of encapsulated prolonged-release drugs and identifying the best performing candidate. While studying the growth dynamics of the laboratory susceptible strain M. tuberculosis H37Rv in the presence of different levofloxacin concentrations (from 0.03 to 0.4 μg/ml), we developed a model, which is essentially a set of 2 parallel experiments evaluating the kinetics of drug release into the culture medium. The results of these 2 experiments conducted on 3 encapsulated forms of levofloxacin loaded onto bioresorbable polymeric PLGA carriers (particles sized 50 μm and 100 μm and the matrix) revealed that release kinetics of the drug largely depended on the type of polymeric carrier. The best encapsulation of the antibiotic and its gradual release into the culture medium was observed for the matrix. All experiments were run in 3 replicates. The obtained data were analyzed using descriptive statistics.
Antioxidant drugs are actively used in medical practice for the treatment of inflammatory processes in various cardiac, ophthalmic, autoimmune, cancer and other diseases. The use of nanobiotechnological methods is a promising area of modern pharmacy, as it allows for creation of drugs of a qualitatively new level. Encapsulation of active pharmaceutical ingredients in liposomal nanoparticles makes it possible to increase the bioavailability and efficacy of natural antioxidants, to create water-soluble injectable forms of hydrophobic compounds. Biotesting is a simple, informative and rapid method to evaluate the toxicity and antioxidant activity of drugs, which can be a valid alternative to the use of laboratory animals at the screening stage. Paramecium caudatum is an unicellular infusoria widely used as test-object due to high sensitivity to environmental changes; big cell size, which makes it possible to monitor changes in morphology and mobility of the cells; easy cultivation. The aim of the study is to evaluate the toxicity and antioxidant activity of liposomal forms of antioxidants: quercetin, curcumin, coenzyme Q10 and cytochrome C by biotesting method using Paramecium caudatum. The toxicity of liposomal forms of quercetin, curcumin, coenzyme Q10 and cytochrome C at doses of 25–100 μg/ml using Paramecium caudatum was studied. Incubation of Paramecium caudatum with liposomal forms of quercetin, curcumin and coenzyme Q10 led to growth of the cell culture, whereas liposomal cytochrome C caused cell lysis within 24 hours. It is established that toxicity of liposomal preparation is influenced by its lipid composition. Incorporation of anionic phospholipid (dipalmitoylphosphatidylglycerol) in lipid membrane significantly reduces the survival of the test culture compared with liposomes containing only phosphatidylcholine. In the model of oxidative stress induced in Paramecium caudatum by hydrogen peroxide, liposomal forms of quercetin, curcumin and coenzyme Q10 demonstrated dose-dependent antioxidant effects, which resulted in tolerance increasing of the test culture to the toxicant.
The effect of anionic phospholipids, namely, cardiolipin, phosphatidylglycerol and phosphatidic acid, on the growth of gram-negative bacteria E. coli BL21(DE3), as well as gram-positive bacteria M. tuberculosis H37Rv was investigated in this study. The influence of all anionic phospholipids tested on the bacteria growth was shown to be dose-dependent. Lipids at concentrations below 335 μM didn’t affect, while at 335 μM and above they repressed bacteria growth and caused cellular death of both type of microorganisms. SOS response induction was observed by using strain E. coli CSH50 sfiA::lacZ during cultivation E. coli with cardiolipin, phosphatidylglycerol and phosphatidic acid. This indicates DNA damage through double-strand breaks. One reason of the DNA damage could be stabilization of transient complexes of DNA topoisomerase (types I and II) with DNA temporary broken by anionic phospholipids. However, neither phosphatidylglycerol nor phosphatidic acid affect the activity of types I and II DNA topoisomerases from E. coli in vitro. In contrast, cardiolipin inhibited DNA topoisomerase I and DNA gyrase (type II topoisomerase), but didn’t stabilize transient complexes of the enzyme with DNA. It indicates that DNA damage due to anionic phospholipids exposure didn’t result from inhibition of DNA topoisomerase activity through stabilization of the transient complex of the enzyme with DNA. The obtained results of cardiolipin, phosphatidylglycerol and phosphatidic acid bactericidal activity against grampositive M. tuberculosis and gram-negative E. coli make it possible to use anionic phospholipids as individual antimicrobial agents or as a matrix of effective and non-toxic liposomal drugs for tuberculosis treatment.
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