Development of Oral Sustained Release Rifampicin Loaded Chitosan Nanoparticles by Design of Experiment

Abstract

Objective. The main objective of the present investigation was to develop and optimize oral sustained release Chitosan nanoparticles (CNs) of rifampicin by design of experiment (DOE). Methodology. CNs were prepared by modified emulsion ionic gelation technique. Here, inclusion of hydrophobic drug moiety in the hydrophilic matrix of polymer is applied for rifampicin delivery using CN. The 23 full-factorial design was employed by selecting the independent variables such as Chitosan concentration (X 1), concentration of tripolyphosphate (X 2), and homogenization speed (X 3) in order to achieve desired particle size with maximum percent entrapment efficiency and drug loading. The design was validated by checkpoint analysis, and formulation was optimized using the desirability function. Results. Particle size, drug entrapment efficiency, and drug loading for the optimized batch were found to be 221.9 nm, 44.17 ± 1.98% W/W, and 42.96 ± 2.91% W/W, respectively. In vitro release data of optimized formulation showed an initial burst followed by slow sustained drug release. Kinetic drug release from CNs was best fitted to Higuchi model. Conclusion. Design of Experiment is an important tool for obtaining desired characteristics of rifampicin loaded CNs. In vitro study suggests that oral sustained release CNs might be an effective drug delivery system for tuberculosis.

Nano-engineering chitosan particles to sustain the release of promethazine from orodispersables

“…Despite the weak acidic nature of PEAA which was believed to reduce its dissolution under the 569 acidic conditions of this study (0.1N HCl), PEAA-CS particles exhibited a burst effect, possibly because some 570 of PMZ was attached to the surface of the nanoparticles and released ring the first few hours of the 571 dissolution study as suggested earlier by (Patel, Parikh, & Aboti, 2013). On the other hand, PVP and PEG 572 coated nanoparticles showed the slowest amount of drug release over 24hr.…”

“…The ability of CS to form nano-94 microparticulate systems depends on its ability to form covalent cross-linking between the chitosan chain 95 and the functional cross-linking agent such as polyehtlene glycol (PEG), dicarboxlylic acid or 96 tripolyphosphate. Patel et al (2013) utilised CS to develop a sustained delivery system of Rifampicin. 97…”

“…Increasing CS concentration was associated with an increase in the average 333 particle size of the nanoparticles. Possibly increasing the concentration of CS results in a viscosity 334 increase, which in turn will affect the shear capacity of homogenization leading to the formation of 335 aggregates with larger particle size ( the effect of TPP concentration on particle size, it was demonstrated that the higher the concentration of 338 TPP, the larger the particle size, this is because of the stiffening of the cross-linking bonds between TPP and 339 CS associated with the rise of the tripolyphosphoric ions (Patel, Parikh, & Aboti, 2013). The increase in the 340 drug concentration led to a decrease in the particle size, this could be attributed to the competition between 341 PMZ and CS cations to bind with TPP phosphoric ions which in turn will decrease the intermolecular cross 342 linkage between CS and TPP and hence the formation of larger particles.…”

Application of Box–Behnken design to prepare gentamicin-loaded calcium carbonate nanoparticles

“…Considering a number of reports, this eff ect could be attributed to drug diff usion out of the particles during the size reduction at the high homogenization speeds (Yoncheva et al 2003, Patel et al 2013. Conversely, the drug concentration had a positive eff ect on entrapment effi ciency.…”

Fabrication of PLA-PEG Nanoparticles as Delivery Systems for Improved Stability and Controlled Release of Catechin

“…Dialysis bag diffusion technique with minor modifications was employed for in vitro catechin release studies [13]. The study was performed for six concentrations of CATNP, namely, 1, 2, 5, 10, 12, and 15 mg/ml.…”