Polylactide-co-glycolide nanoparticles immobilized with isoniazid: optimization using the experimental Taguchi method

Abstract

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

Central Composite Design for Formulation and Optimization of Rifampicin Loaded Polylactide-Co-Glycolide Nanoparticles

“…Moreover, CCD was successfully used in our previous study to optimize and develop a method for the synthesis of HSA NPs loaded with anti-TB drugs, and the data produced by CCD showed good and reliable predictions [19]. The variables in Table 1 were selected based on our initial studies [11,20].…”

“…Since the percentage of mass loss of the polymer at this point is 77%, this may indicate the onset of significant polymer degradation. The second peak, which appears at 420 °C with slight mass loss, may indicate more complex processes such as the subsequent degradation of residual polymer parts [11,20,25,26]. As for rifampicin-loaded PLGA nanoparticles, no new endothermic peaks are observed in the DSC curve.…”

“…transport of anti-TB drugs is particularly important. PLGA has unique properties such as biocompatibility, biodegradability and the ability to control the rate of drug release [9][10][11]. These characteristics make it an ideal material for the development of drug carriers capable of providing stable and controlled delivery of rifampicin into the body, which is critical for effective treatment of tuberculosis.…”

“…Various factors can affect the average size of PLGA nanoparticles: type of PLGA, polymer to drug ratio, type and concentration of surfactants, type of organic solvent, its ratio to the aqueous phase, as well as the power and duration of the homogenization process [9][10][11]. Determining the optimum conditions for the synthesis of these nanoparticles requires careful investigation and selection of the desired parameters, subsequently studying all the above process parameters.…”

Encapsulation of Isoniazid in Polylactide-Co-Glycolide Nanoparticles by Nanoprecipitation

“…The first phase is caused by the release of the drug substance, which is adsorbed on the surface of the NPs or dispersed near the surface. The second phase is due to the release of the drug substance residing in the core [28][29][30][31]. As shown in Figure 4, "burst release" of the drug is observed at pH 6.86 after 2 hours; at pH 7.4 after 5 hours; and at pH 1.2 was 27 % within an hour.…”