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.

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.

This study involved the synthesis of bovine serum albumin (BSA) nanoparticles immobilized with the antituberculosis drugs isoniazid (INH) and rifampicin (RIF) by the desolvation method. The primary objective was to explore the impact of varying concentrations of albumin, urea, cysteine, rifampicin, and isoniazid on the average size of nanoparticles, polydispersity, and the encapsulation efficiency of drugs. The study's outcomes affirm that alterations in the concentrations of these components influence nanoparticles’ parameters, highlighting their key role in optimizing the encapsulation process and enhancing the efficacy of tuberculosis drug delivery. The nanoparticles obtaned as a result of optimization demonstrated an optimal size of 231.2±1.2 nm with a polydispersity of 0.061±0.08. Encapsulation efficiency was 89% for rifampicin and 38.5% for isoniazid. The investigation of drug release kinetics from the polymer matrix revealed a gradual release pattern. Evaluation of the obtained nanoparticles by Fourier-transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), and differential scanning calorimetry (DSC) confirmed the successful incorporation of drugs into the polymer matrix. These findings highlight the potential of BSA nanoparticles as effective carriers for tuberculosis treatment, with implications for refining drug delivery strategies.

The aim of this study was to synthesize and optimize polylactide-co-glycolide (PLGA) nanoparticles loaded with rifampicin (RIF), with a given size and high loading rate, using the central composite design (CCD) method. CCD was used to investigate the influence of independent factors such as PLGA:RIF ratio, type of PLGA, type and concentration of surfactants, power and duration of homogenization, and type of organic solvent and its ratio to the aqueous phase on the dependent physicochemical characteristics of the nanoparticles. The optimized nanoparticles were investigated using scanning electron microscope (SEM), Fourier transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC). Comparative evaluation of the drug release kinetics was carried out using different pH and different setups: flow cuvette (USP 4 apparatus) and Franz diffusion cuvette. In addition, the mucoadhesive properties and mycobacterial activity of PLGA-RIF NPs were studied.

Pulmonary delivery of anti-tuberculosis drugs has emerged as a promising alternative for increasing local drug concentrations whilst minimising side effects. Natural polymers—polysaccharides capable of forming polyelectrolyte complexes (PECs) through electrostatic interactions—show great promise in this field. In this study, mucoadhesive chitosan-gellan gum nanoparticles were developed for the controlled release of isoniazid using the polyelectrolyte complex coacervation method. Parameters such as the chitosan-to-gellan gum ratio and the medium pH were investigated to achieve suitable particle size, polydispersity, surface charge, drug loading and encapsulation efficiency. The morphology of the produced nanoparticles was determined using transmission electron microscopy (TEM) and nanoparticle tracking analysis (NTA), which confirmed the formation of nanoscale spherical particles. The mucoadhesive properties were tested on ovine lung tissue using fluorescence retention analysis, whilst in vitro drug release was studied under physiological conditions. Antimycobacterial activity against Mycobacterium tuberculosis H37Rv was assessed using the Mycobacteria Growth Indicator Tube (MGIT) system, followed by subculturing on Löwenstein–Jensen medium. The produced nanoparticles exhibited high mucoadhesion, maintaining prolonged retention on lung tissue. Drug release showed an initial burst followed by sustained release over 24 h. These results demonstrate that CSGG–INH nanoparticles possess sustained drug release, good mucoadhesion to the lungs and high antimycobacterial activity, supporting their further development as potential carriers for pulmonary delivery of anti-tuberculosis drugs.