Development and optimization of solid lipid nanoparticle formulation for ophthalmic delivery of chloramphenicol using a Box-Behnken design

Abstract

The purpose of the present study was to optimize a solid lipid nanoparticle (SLN) of chloramphenicol by investigating the relationship between design factors and experimental data using response surface methodology. A Box-Behnken design was constructed using solid lipid ( X 1 ), surfactant ( X 2 ), and drug/lipid ratio ( X 3 ) level as independent factors. SLN was successfully prepared by a modified method of melt-emulsion ultrasonication and low temperature-solidification technique using glyceryl monostearate as the solid lipid, and poloxamer 188 as the surfactant. The dependent variables were entrapment efficiency (EE), drug loading (DL), and turbidity. Properties of SLN such as the morphology, particle size, zeta potential, EE, DL, and drug release behavior were investigated, respectively. As a result, the nanoparticle designed showed nearly spherical particles with a mean particle size of 248 nm. The polydispersity index of particle size was 0.277 ± 0.058 and zeta potential was −8.74 mV. The EE (%) and DL (%) could reach up to 83.29% ± 1.23% and 10.11% ± 2.02%, respectively. In vitro release studies showed a burst release at the initial stage followed by a prolonged release of chloramphenicol from SLN up to 48 hours. The release kinetics of the optimized formulation best fitted the Peppas–Korsmeyer model. These results indicated that the chloramphenicol-loaded SLN could potentially be exploited as a delivery system with improved drug entrapment efficiency and controlled drug release.

Sustained release biodegradable solid lipid microparticles: Formulation, evaluation and statistical optimization by response surface methodology

“…release at 12 h. The F-values for Y 2 and Y 3 were found to be 12.36 and 13.65, respectively, indicating that the model was significant (p < 0.0001). It can be concluded from the regression equation that the EE and drug release from prepared SLMs were strongly dependent on the studied variables (19,22). Assessment of EE for every SLM formulation showed great variation, from 45 (F1, F10) to 83 % (F19) ( Table I).…”

“…To get an optimized formulation, help was also sought of the desirability approach, numerical and graphical optimization tools to create optimal settings for SLM formulations. The suggested optimized formulation was not only formulated but also evaluated (21)(22).…”

“…Significance of the quadratic model was analyzed with the aid of analysis of variance (ANOVA) applied at the 5 % significance level and a p-value lower than 0.05 indicated that the model was significant. The selected model was further assessed for the lack of fit (LOF) and for the studied responses; LOF was not found to be significant (21)(22). The values of R 2 , adjusted R 2 , predicted R 2 , SD, % CV (Table II) and the analysis of variance results for each response (ANOVA) in Table II (12.036) were found to be higher than 4, indicating the adequacy and suitability of the model for the studied responses (23)(24).…”

Preparation of Biocompatible Carboxymethyl Chitosan Nanoparticles for Delivery of Antibiotic Drug

“…It provides detailed information to better understand potential interaction between various factors employed in pharmaceutical preparations for yielding the optimal formulation [12, 13]. Experiments were designed according to Box-Behnken response surface method and shown in Table 1.…”

Caracterización Fisicoquímica de Emulsiones Aceite/Agua a partir de Uchuva (Physalis peruviana) como Ingrediente para la Industria Alimenticia

“…Las partículas (gotas) con un potencial Z entre -10 mV y +10 mV se consideran aproximadamente neutras, mientras que las partículas con potenciales Z mayores de +30 mV o menores que -30 mV se consideran fuertemente catiónicas y fuertemente aniónicas, respectivamente. (Rahman et al, 2010;Hao et al, 2011). En el caso de las emulsiones obtenidas a partir de uchuva, se sugiere que la estabilidad conseguida está más relacionada con el aumento de la viscosidad que con la repulsión electrostática, debido a los componentes del sistema.…”