Mixed Edge Activators in Ibuprofen-Loaded Transfersomes: An Innovative Optimization Strategy Using Box–Behnken Factorial Design

Abstract

Transfersomes have been highlighted as an interesting nanotechnology-based approach to facilitate the skin delivery of bioactive compounds. Nevertheless, the properties of these nanosystems still need to be improved to enable knowledge transfer to the pharmaceutical industry and the development of more efficacious topical medicines. Quality-by-design strategies, such as Box–Behnken factorial design (BBD), are in line with the current need to use sustainable processes to develop new formulations. Thus, this work aimed at optimizing the physicochemical properties of transfersomes for cutaneous applications, by applying a BBD strategy to incorporate mixed edge activators with opposing hydrophilic–lipophilic balance (HLB). Tween® 80 and Span® 80 were used as edge activators and ibuprofen sodium salt (IBU) was selected as the model drug. After the initial screening of the IBU solubility in aqueous media, a BBD protocol was implemented, and the optimized formulation displayed appropriate physicochemical properties for skin delivery. By comparing the optimized transfersomes to equivalent liposomes, the incorporation of mixed edge activators was found to be beneficial to upgrade the storage stability of the nanosystems. Furthermore, their cytocompatibility was shown by cell viability studies using 3D HaCaT cultures. Altogether, the data herein bode well for future advances in the use of mixed edge activators in transfersomes for the management of skin conditions.

Insect larvae oil: a high value excipient for lipid-based nanocarriers to tackle atopic dermatitis

“…Our data support that BBD is a powerful tool for nanocarriers optimization, as previously described (12,13). The optimized DEX-loaded SLN had satisfactory physicochemical characteristics, namely PS < 200 nm, a uniform distribution of particle sizes (PDI < 0.3), a promising colloidal stability (ZP lower than -30 mV), and elevated EE and LC values (higher than 85% and 1.2%, respectively).…”

The Optimization Design of Macrophage Membrane Camouflaging Liposomes for Alleviating Ischemic Stroke Injury through Intranasal Delivery

“…Therefore, these three factors were further investigated as experimental response surface factors. The Box Behnken Design was used to optimize the formulation of the liposome by Design Expert.V8.0.6.1 (Stat-Ease, Minneapolis, MN, USA) [54], and a total of 17 experiments were performed to study the effect of three independent variables on the EE% of Rg3 and PNS. The experimental results are summarized in Table 1.…”

“…The experimental results are summarized in Table 1. Design Expert 8.0 software was used to perform regression model equation fitting on the obtained experimental data, and the regression simulation equations between the EE% of PNS (Y1) and the EE% of Rg3 (Y2) on three influencing factors (EPC concentration (A), PNS/EPC ratio (B), and Rg3/EPC ratio (C)) were obtained as follows: The Box Behnken Design was used to optimize the formulation of the liposome by Design Expert.V8.0.6.1 (Stat-Ease, Minneapolis, MN, USA) [54], and a total of 17 experiments were performed to study the effect of three independent variables on the EE% of Rg3 and PNS. The experimental results are summarized in Table 1.…”

The Exploitation of Sodium Deoxycholate-Stabilized Nano-Vesicular Gel for Ameliorating the Antipsychotic Efficiency of Sulpiride

“…Spectrophotometer, Uviline 9100, SCHOTT-EU, Mainz, Germany) at a wavelength of λmax of 293 nm [44]. The entrapment efficiency, expressed as a percentage (% EE), was calculated using the following the following equation [45] The drug loading percentage was determined by measuring the ratio of the amount of drug entrapped to the total amount of lipid utilized in vesicle formation, as illustrated in the following calculation [46]. The DSC technique (DSC-60, Shimadzu, Kyoto, Japan) was utilized to analyze the thermal properties of Sulpiride, soy lecithin, Span 60, SDC, and the optimum bilosomes loaded with Su.…”