Development of Metronidazole Loaded Chitosan Nanoparticles Using QbD Approach—A Novel and Potential Antibacterial Formulation

Abstract

The aim of this study was to design, optimize, and develop metronidazole (Met) loaded nanoparticles (MetNp) by employing quality-based design (QbD) as well as a risk assessment methodology. A fractional factorial design was used by selecting five independent variables viz., chitosan concentration, tripolyphosphate concentration, and acetic acid concentration as material attributes, stirring speed, and stirring time as process parameters, whereby their influence on two dependent variables such as particle size (PS) and %entrapment efficiency (%EE) was studied. MetNp were synthesized by employing an ionic-gelation technique and optimized formula obtained from the QbD design study. PS and %EE studies revealed the formation of MetNp with 558.06 ± 2.52 nm and 59.07 ± 2.15%, respectively. Furthermore, a Met release study in various simulated gastro-intestinal media suggested pH-triggered (pH > 7.0) and sustained release profile of Met from Eudragit S100 enteric-coated MetNp capsule (MetNp cap). Moreover, the stability investigation of formulations confirmed good stability with respect to their PS and residual drug content (RDC) at different temperature conditions. In conclusion, the QbD method was effectively utilized in the development of MetNp and enteric-coated MetNp cap depicting their potential to release Met through MetNp cap only in the colon region and can be utilized for the treatment of amoebiasis in the colon.

An Engineered Specificity of Anti-Neoplastic Agent Loaded Magnetic Nanoparticles for the Treatment of Breast Cancer

“…Additionally, CS was found to be a promising nanocarrier of anti-neoplastic drugs in many reports [22]. Furthermore, the principal amino groups of CS can be utilized for designing controlled release, mucoadhesion, in situ gelling, transfection delivery, penetration enhancement, and hampering efflux pumps [23][24][25]. CS can effortlessly affix to the magnetic nanoparticle surface and also render the amine and hydroxyl groups for coupling with the therapeutic drug molecules [26].…”

Encapsulation of Metronidazole in Biocompatible Macrocycles and Structural Characterization of Its Nano Spray-Dried Nanostructured Composite

“…As the amount of SCX4–MetH + came close to the particle charge neutralization, the zeta potential gradually vanished. Our approach to inducing the nanoparticle formation of protonated chitosan by SCX4–MetH + complexation has the advantage of providing smaller particle diameters (d = 168–302 nm) than the previously published optimised method (d = 558 nm) that employed a tripolyphosphate supramolecular crosslinker for metronidazole embedment [ 15 ]. The smaller carrier particles usually improve the bioavailability of the drugs.…”

“…Cyclodextrins and mesoporous silica particles were combined as a composite to reduce the rate of drug liberation [ 14 ]. An ionic gelation technique was employed to create Met-loaded chitosan nanoparticles capable of pH-triggered sustained release [ 15 , 16 ]. Met was also incorporated in nanofibrous webs by electrospinning [ 17 , 18 , 19 ], whereas crystalline–amorphous nanostructured micronized solid dispersions were prepared by the spray drying of solutions containing polymers [ 20 ].…”

Itraconazole loaded nano-structured lipid carrier for topical ocular delivery: Optimization and evaluation

“…The size of particles in the prepared NLCs was determined by laser diffraction technique using a Malvern Zetasizer (S90 series, Worcestershire, UK) ( Morsy et al, 2019 ). The size of the particles was checked at 25 °C after diluting the drug concentration with deionized purified water and filtered using a syringe filter (pore size 0.45 µm, Millipore Co., USA) ( Sreeharsha et al, 2020 ). For each formulation, the particle size was measured six times and the results are represented as means ± SD.…”