Short Term Stability Testing of Efavirenz-Loaded Solid Lipid Nanoparticle (SLN) and Nanostructured Lipid Carrier (NLC) Dispersions

Abstract

The short term stability of efavirenz-loaded solid lipid nanoparticle and nanostructured lipid carrier dispersions was investigated. Hot High Pressure Homogenization with the capability for scale up production was successfully used to manufacture the nanocarriers without the use of toxic organic solvents for the first time. Glyceryl monostearate and Transcutol® HP were used as the solid and liquid lipids. Tween® 80 was used to stabilize the lipid nanocarriers. A Box-Behnken Design was used to identify the optimum operating and production conditions viz., 1100 bar for 3 cycles for the solid lipid nanoparticles and 1500 bar for 5 cycles for nanostructured lipid carriers. The optimized nanocarriers were predicted to exhibit 10% efavirenz loading with 3% and 4% Tween® 80 for solid lipid nanoparticles and nanostructured lipid carriers, respectively. Characterization of the optimized solid lipid nanoparticle and nanostructured lipid carrier formulations in relation to shape, surface morphology, polymorphism, crystallinity and compatibility revealed stable formulations with particle sizes in the nanometer range had been produced. The nanocarriers had excellent efavirenz loading with the encapsulation efficiency >90%. The optimized nanocarriers exhibited biphasic in vitro release patterns with an initial burst release during the initial 0–3 h followed by sustained release over a 24 h period The colloidal systems showed excellent stability in terms of Zeta potential, particle size, polydispersity index and encapsulation efficiency when stored for 8 weeks at 25 °C/60% RH in comparison to when stored at 40 °C/75% RH. The formulations manufactured using the optimized conditions and composition proved to be physically stable as aqueous dispersions.

Comparative study for optimization of folic acid nanoparticles

“…The particle size results are not exceeding 400 nm throughout 9 months storage which implies good physical stability and is very promising for an easy penetration [36,37]. The particle size values of F2 during this study at RT are slightly larger than in Ref T. Results show less stability, in terms of drug retained, for formulations stored at 25 °C, attributed to introduction of energy into the system leading to particle growth and subsequent aggregation and drug expulsion from NLCs [38]. The chemical stability is also evaluated by measuring the drug retained %.…”

Nebulised surface-active hybrid nanoparticles of voriconazole for pulmonary Aspergillosis demonstrate clathrin-mediated cellular uptake, improved antifungal efficacy and lung retention

“…LPH NPs, lyophilized with 5% mannitol and 5% trehalose, get easily dispersed in water, upon reconstitution. The presence of trehalose as cryoprotectant is known to enhance the stability of the NPs during freeze drying [ 86 ]. This could be postulated due to the physical isolation of adjacent NPs in the presence of glassy cryoprotectant to reduce the destabilising stress caused during the freezing process [ 87 ].…”

Nanomaterial Lipid-Based Carrier for Non-Invasive Capsaicin Delivery; Manufacturing Scale-Up and Human Irritation Assessment

“…Many previous studies had confirmed the superior entrapment efficiency of NLCs compared to that of SLN [2,29,30]. Chili-extract-loaded NLCs (NLC_Cs) were prepared from a lipid mixture and surfactant as described in the previous study [29].…”