Fabrication and Characterization of Pluronic F68 and Phospholipon 90g Embedded Nanoformulation for Sertraline Delivery: An Optimized Factorial Design Approach and In Vivo Study

Abstract

Objective: The objective of present work was to utilize the potential of nanostructured lipid carriers (NLCs) form improvement in bioavailability of Sertraline as antidepressant drug formulated by emulsification- solvent evaporation technique with some modification. NLC is the blend of solid lipid, liquid lipid and surfactant for encapsulation of poor water soluble actives. Design: A full 32 factorial design was utilized to study the effect of two independent parameters namely solid lipid to liquid lipid concentration and stabilizer concentration on the entrapment efficiency of the prepared NLCs. The sertraline NLC formulation was characterized with respect to particle size, polydispersity index (PDI), zeta-potential, encapsulation efficiency and physical morphology. Result: The NLC formulation had an average diameter of 96.59 nm, PDI of 0.192, zeta-potential of -39.88 mV, and encapsulation efficiency of 97%, respectively. Conclusion: The NLC formulation for sertraline encapsulation has been successfully developed and is suitable for nose to brain delivery system due to their nano-size and sta

Double Optimization of Rivastigmine-Loaded Nanostructured Lipid Carriers (NLC) for Nose-to-Brain Delivery Using the Quality by Design (QbD) Approach: Formulation Variables and Instrumental Parameters

“…The PDI is an indicative of the particle size distribution. According to the literature, a monodisperse sample has PDI values close to 0, while values between 0.1 and 0.3 indicate a narrow size distribution, between 0.1 and 0.4 indicate a moderate size distribution, and greater than 0.4 represent a wide size distribution [ 32 , 63 ]. From the analysis of the Pareto chart ( Supplementary Data, Section 3.1, Figure S4D ), the surfactants ratio (Tw/Ph) and lipids ratio (SL/LL) were not statistically significant for PDI, although the ratio of lipids showed a more significant effect than the surfactants ratio through the length of the bar.…”

“…ZP reflects the electric potential and the surface charge of nanoparticles in a suspension and is a predicting factor of the long-term stability. When ZP values are higher than │30│ mV, the electrostatic repulsion of the attractive Van der Waals forces stops nanoparticle aggregation from occurring [ 63 , 92 , 93 , 94 ]. Lipids arrangements on the surface of the nanoparticle, surfactant surface absorption, and the charge of the encapsulated drug interfere with ZP [ 32 , 92 ].…”

“…This can be explained by the lipophilic nature of rivastigmine, which becomes more solubilized as the lipid concentration increases. In addition, this can also be related to the surfactants, which create more available space between lipids to accommodate rivastigmine molecules [ 32 , 63 ].…”

“…These results suggest that both optimized rivastigmine-loaded NLC formulations are stable during storage and fulfil the QTPP for nasal administration. This high stability is related to the presence of Tween ® 80 and Phospholipon ® 90 G, which stabilize NLC via distinct mechanisms (steric and electrostatic, respectively) and also to the presence of vitamin E, which has antioxidant activity that provides chemical stability to rivastigmine and prevents oxidation of the lipid matrix [ 31 , 34 , 56 , 57 , 63 ]. Besides, it has been described that NLC formulations with ZP values close to |30| mV show high long-term stability [ 105 ].…”

“…Surfactants should be selected according to their charge, molecular weight, and adequacy for the desired route of administration for the formulation [ 22 , 50 , 60 , 61 ]. Smaller particle sizes have been observed when a higher surfactant/lipid ratio was used [ 31 , 62 , 63 ]. Accordingly, polysorbate 80 (Tween ® 80), a non-ionic surfactant containing a polyoxyethylene chain tetrahydrofuran ring that provides steric stabilization and a hydrophobic tail that prevents particle aggregation, was selected based on previous works that showed its compatibility with the lipids used [ 46 , 52 , 53 , 59 , 60 , 64 ].…”