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

Abstract

Sustained release biodegradable solid lipid microparticles: Formulation, evaluation and statistical optimization by response surface methodologyFor preparing nebivolol loaded solid lipid microparticles (SLMs) by the solvent evaporation microencapsulation process from carnauba wax and glyceryl monostearate, central composite design was used to study the impact of independent variables on yield (Y 1 ), entrapment efficiency (Y 2 ) and drug release (Y 3 ). SLMs having a 10-40 µm size range, with good rheological behavior and spherical smooth surfaces, were produced. Fourier transform infrared spectroscopy, differential scanning calorimetry and X-ray diffractometry pointed to compatibility between formulation components and the zeta-potential study confirmed better stability due to the presence of negative charge (-20 to -40 mV). The obtained outcomes for Y 1 (29-86 %), Y 2 (45-83 %) and Y 3 (49-86 %) were analyzed by polynomial equations and the suggested quadratic model were validated. Nebivolol release from SLMs at pH 1.2 and 6.8 was significantly (p < 0.05) affected by lipid concentration. The release mechanism followed Higuchi and zero order models, while n > 0.85 value (Korsmeyer-Peppas) suggested slow erosion along with diffusion. The optimized SLMs have the potential to improve nebivolol oral bioavailability.

Investigation of the Potential of Nebivolol Hydrochloride-Loaded Chitosomal Systems for Tissue Regeneration: In Vitro Characterization and In Vivo Assessment

“…The XRD study was done to evaluate the physical nature of the drug and the effect of the method of preparation and excipients [ 95 , 96 ]. Figure 5 presents the XRD of NVH, CSL, NVH:CSL physical mixture (2:5) and the lyophilized best-achieved formulation F6.…”

“…Figure 5 presents the XRD of NVH, CSL, NVH:CSL physical mixture (2:5) and the lyophilized best-achieved formulation F6. NVH had sharp intense peaks at 5.9°, 11.9°, 12.2°, 16.3°, 18.4°, 21.4°, 22.4°, and 25.67°, confirming its crystalline form [ 95 , 96 , 97 ]. The X-ray spectra of the physical mixture showed that the NVH peaks intensity decreased, possibly due to the dilution effect, without a qualitative disparity of its diffractogram.…”