The aim of this study was to create nanoparticles of human serum albumin immobilized with anti-TB drugs (rifampicin, isoniazid) using the desolvation method. Central Composite Design (CCD) was applied to study the effect of albumin, urea, L-cysteine, rifampicin and isoniazid concentration on particle size, polydispersity and loading degree of the drugs. The optimized nanoparticles were spherical in shape with an average particle size of 216.7 ± 3.7 nm and polydispersity of 0.286 ± 4.9. The loading degree of rifampicin and isoniazid in the optimized nanoparticles were 44% and 27%, respectively. The obtained nanoparticles were examined by Fourier-transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC); the results showed the absence of drug–polymer interactions. The drug release from the polymer matrix was studied using dialysis membranes.

Tuberculosis is one of the dangerous infectious diseases, killing over a million people worldwide each year. The search for new dosage forms for the treatment of drug-resistant tuberculosis is an actual task. Biocompatible polymer nanoparticles, in particular bovine serum albumin (BSA), are promising drug carriers. Nanoparticle (NP) parameters such as diameter, polydispersity, bioactive substance loading, and NP yield are very important when it comes to drug transport through the bloodstream. The most well-known and widely used first-line anti-tuberculosis drug, isoniazid (INH), is being used as a drug. BSA-INH NPs were obtained by an ethanol desolvation of an aqueous protein solution in the drug presence. The peculiarity of the method is that natural components, namely urea and cysteine, are used for the stabilization of BSA-INH NPs after desolvation. The characteristics of the obtained BSA-INH NPs are significantly affected by the concentration of protein, isoniazid, urea, and cysteine in the solution. The aim of the present study is to investigate the concentration effect of the system reacting components on the parameters of the NPs that are obtained. We have chosen the concentrations of four reacting components, i.e., BSA, isoniazid, urea, and cysteine, as controlling factors and applied the Taguchi method to analyze which concentration of each component has an important effect on BSA-INH NPs characteristics.

Despite the large number of works on the synthesis of polylactide-co-glycolide (PLGA) nanoparticles (NP) loaded with antituberculosis drugs, the data on the influence of various factors on the final characteristics of the complexes are quite contradictory. In the present study, a comprehensive analysis of the effect of multiple factors, including the molecular weight of PLGA, on the size and stability of nanoparticles, as well as the loading efficiency and release of the antituberculosis drug rifampicin (RIF), was carried out. Emulsification was carried out using different surfactants (polyvinyl alcohol, Tween 80 and Pluronic F127), different aqueous-to-organic phase ratios, and different solvents (dichloromethane, dimethyl sulfoxide, ethyl acetate). In this research, the PLGA nanoemulsion formation process was accompanied by ultrasonic dispersion, at different frequencies and durations of homogenization. The use of the central composite design method made it possible to select optimal conditions for the preparation of PLGA-RIF NPs (particle size 223 ± 2 nm, loading efficiency 67 ± 1%, nanoparticles yield 47 ± 2%). The release of rifampicin from PLGA NPs was studied for the first time using the flow cell method and vertical diffusion method on Franz cells at different pH levels, simulating the gastrointestinal tract. For the purpose of the possible inhalation administration of rifampicin immobilized in PLGA NPs, their mucoadhesion to mucin was studied, and a high degree of adhesion of polymeric nanoparticles to the mucosa was shown (more than 40% within 4 h). In the example of strain H37Rv in vitro, the sensitivity of Mycobacterium tuberculosis to PLGA-RIF NPs was proven by the complete inhibition of their growth.

The research aims to optimize and minimize the number of experiments to obtain polylactide-co-glycolide (PLGA) nanoparticles (NPs) immobilized with antituberculosis (anti-TB) drug — isoniazid (INH) by applying the Taguchi method and Design Expert statistical software. Several experiments were performed with varying parameters, namely polymer/drug ratio, polyvinyl alcohol (PVA) concentration, the ratio of organic solvent to the aqueous phase, and solvent type. Three different levels and a fractional factorial design were derived for each parameter, particularly the standard orthogonal array (OA) L9. Drug-loaded nanoparticles were prepared by the double emulsion method. The results were obtained from 9 runs indicated particle sizes ranging from 152.2±6.4 nm to 496.4±9.5 nm. These results were used to predict the optimum conditions for synthesizing INH-PLGA particles. The calculated data correlate well with the experimental data. INH-PLGA NPs were obtained with a mean size and polydispersity of nanoparticles of 152.2±2.25 nm and 0.279±0.03, respectively. Scanning electron microscopy, thermogravimetric analysis, and differential scanning calorimetry were carried out to characterize the obtained nanoparticles. The degree of drug release from PLGA NPs was studied, and the results showed that PLGA prolonged the release of INH from the polymer matrix

This article considers someaspects of synthesis and characterizationof polylactide-co-glycolide nanoparticles immobilized withthe antituberculous drug isoniazid. The influence of some synthesis parameters of nanoparticles (the ratio of drug substance:polymer and surfactant concentration) onproperties of the obtained nanosomal drug form of isoniazid has been studied. Optimal conditions for obtainingthenanoparticles with the best physicochemical parameters such as: particle size, polydispersity, conversion, etc. have been found. These nanoparticlescan be used asdrug carriers.The results revealed thata polymer: drug ratio of 1:1 and the use of 3% Twin 80 are necessaryto obtain stable emulsions of nanoparticles of polylactide-co-glycolide with satisfactory characteristics. Average size of the obtained particles was 196.4 nm,and the polydispersity value was 0.323. The aggregation stability of nanoparticles during 4 hours at temperatures of 4ºC and 20ºC has been evaluated. The morphology of the obtained nanoparticles has been studied.Analysis of nanoparticles was characterized by various instrumental methods includinggas chromatography and thermogravimetrytechniques. The resulting nanoparticles of polylactide-co-glycolide immobilized with isoniazid are stable in time andcanprolong the action of the drug. In vitrorelease of isoniazid from polylactide-co-glycolide nanoparticles hasbeen studied.