Abstract
Objective: Tuberculosis (TB) is an infectious bacterial disease caused by Mycobacterium tuberculosis which most commonly affects the lungs. TB has the highest mortality rate than any other infectious disease occurs worldwide. The main objective of the present investigation was to develop polymeric nanoparticles based drug delivery system to sustain the ethambutol (ETB) release by reducing the dose frequency.
 Methods: The Preformulation studies of drug ETB were done by physical characterization, melting point determination, and UV spectrophotometric analysis. The ETB loaded nanoparticles were prepared by double-emulsion (W/O/W) solvent evaporation/diffusion technique. The prepared polymeric nanoparticles were evaluated for particle size, polydispersity index, zeta potential, drug entrapment efficiency, drug loading, drug-polymer compatibility study, surface morphology, in vitro drug release, and release kinetics.
 Results: Based on the result obtained from the prepared formulations, F11 showed the best result and was selected as the optimized formulation. Optimized batch (F11) showed better entrapment efficiency (73.3%), good drug loading capacity (13.21%), optimum particle size (136.1 nm), and zeta potential (25.2 mV) with % cumulative drug release of 79.08% at the end of 24 h.
 Conclusion: These results attributed that developed polymeric nanoparticles could be effective in sustaining the ETB release over 24 h. Moreover, the developed nanoparticles could be an alternate method for ETB delivery with a prolonged drug release profile and a better therapeutic effect can be achieved for the treatment of tuberculosis.
Highlights
Tuberculosis (TB) is a highly contagious persistent infection caused by Mycobacterium tuberculosis and Mycobacterium Bovis and has the highest mortality rate than any other infectious disease
Treatment of TB involves the administration of a combination of two or more first-line anti-TB drugs namely, Rifampicin, Isoniazid, and Ethambutol in a fixed proportion in a single dosage form for the initial two months followed by Rifampicin and Isoniazid for four months, described as RHZE2/RH4 [2, 3]
Based on the result of these six batches, optimized batch (F11) was prepared using EUDRAGIT RS-100, poloxamer188 (1% w/v) and the optimized has shown better entrapment efficiency (73.3%), drug loading (13.21%) and optimum particle size (136 nm)
Summary
Tuberculosis (TB) is a highly contagious persistent infection caused by Mycobacterium tuberculosis and Mycobacterium Bovis and has the highest mortality rate than any other infectious disease. Nanoparticle-based drug delivery systems form the crux of nanomedicine. They are suitable for targeting chronic diseases such as tuberculosis [4]. Experimental data support the possibility of intermittent chemotherapy with key first-line as well as second-line anti-tuberculosis drugs by employing synthetic or natural carriers, polymers [5]. Besides the sustained release of drugs in plasma and organs, other potential advantages of this system include the possibility of selecting various routes of chemotherapy, reduction in drug dosage, adverse effects, drug interactions, and targeting drug-resistant and latent bacteria [6,7,8]
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