Wound Healing Efficacy of Rosuvastatin Transethosomal Gel, I Optimal Optimization, Histological and In Vivo Evaluation

Abstract

This study aimed to make a formulation and statistical optimization of transethosomal formulations of rosuvastatin (ROS) to enhance its topical wound healing efficiency. Design-Expert® software was used to employ I optimal design. The formulation variables in the study were surfactant concentration (%w/v), ethanol concentration (%w/v) and surfactant type (span 60 or tween 80), while the dependent responses were entrapment efficiency percent (EE%), vesicle size (VS) and zeta potential (ZP). The numerical optimization process employed by the design expert software resulted in an optimum formula composed of 0.819439 (%w/v) span 60, 40 (%w/v) ethanol and 100 mg lecithin with a desirability of 0.745. It showed a predicted EE% value of 66.5517 vs. 277.703 nm and a ZP of −33. When it was prepared and validated, it showed less than a 5% deviation from the predicted values. The optimum formula was subjected to further characterizations, such as DSC, XRD, TEM, in vitro release, the effect of aging and wound healing efficiency. The DSC thermogram made a confirmation of the compatibility of ROS with the ingredients used in the formulation. XRD showed the encapsulation of ROS in the transethosomal vesicles. The TEM image pointed out the spherical nature of the nanovesicles with the absence of aggregation. Additionally, the optimum formula revealed an enhancement of drug release in comparison with the drug suspension. It also showed good stability for one month. Furthermore, it revealed good wound healing efficiency when compared with the standard silver sulphadiazine (1% w/w) ointment or the drug-loaded gel, which could be related to the enhanced penetration of the nanosized vesicles of TESMs into the skin, which enhances the wound healing process. So, it could be regarded as a promising carrier of ROS for the treatment of chronic wounds.

Formulation Development, Optimization by Box–Behnken Design, and In Vitro and Ex Vivo Characterization of Hexatriacontane-Loaded Transethosomal Gel for Antimicrobial Treatment for Skin Infections

“…The drop in vesical size with increasing surfactant concentration may be attributable to the membrane’s greater elasticity and softness, which in turn enhances its reduction capacity. The findings we obtained were in agreement with those of Zaki et al [ 28 ].…”

Numerical Optimization of Prednisolone–Tacrolimus Loaded Ultraflexible Transethosomes for Transdermal Delivery Enhancement; Box–Behnken Design, Evaluation, Optimization, and Pharmacokinetic Study

“…The predicted responses of EE%, vesicle size and zeta potential were 79.308%, 298.929 nm, and −35.047 mV, respectively, with a desirability of 0.704 as represented in Table 4 and Figure 3. Validation of the optimum formula resulted in a % relative error less than 5% for all predicted responses, confirming the fitness of the model [36].…”

“…Briefly, the accurate weight of HPMC (0.25 g) was dispersed in 10 mL distilled water while stirring at 1000 rpm to obtain homogenous dispersion. Then the optimum TETSMs formula was dispersed into the gel base with continuous stirring to obtain a final gel formulation with 5 mg PRED per 1 g gel [36].…”

Box Behnken optimization of cubosomes for enhancing the anticancer activity of metformin: Design, characterization, and in-vitro cell proliferation assay on MDA-MB-231 breast and LOVO colon cancer cell lines

“…MTF-loaded CUBs were isolated from the free drug by centrifugation at 17000 rpm for 1 h at 4 °C by the use of a cooling centrifuge (SIGMA 3–30 K, Sigma, Steinheim, Germany) ( Zaki et al, 2022c ; Zaki et al, 2022d ). Then quantification of MTF in the supernatant was performed using a UV spectrophotometer (Shimadzu UV-1800, Kyoto 604–8511, Japan) after diluting it suitably.…”

“…After each sample the MTF concentration was determined at 232 nm with a UV spectrophotometer ( Mali et al, 2015 ). The percentage of MTF released at each time point was calculated using the following equation ( Zaki et al, 2022d ): where,…”