A Full Factorial Design to Optimize Aminexil Nano Lipid Formulation to Improve Skin Permeation and Efficacy Against Alopecia

Abstract

Aminexil (AMX) is considered to be one of the most widely used hair growth promoters. Nanostructured lipid carriers (NLC) are employed to increase the permeation of both lipophilic and hydrophilic drugs. Aminexil nanostructured lipid carrier (NLC) designed by pre-emulsion/ultrasonication method was utilized for alopecia treatment. For selecting optimum excipients, a solubility study was executed in liquid lipids, solid lipids, surfactants, and co-surfactants. A 23 full factorial design was utilized for NLC optimization. Characterization of the developed formulas was performed. The penetration of the optimized formula across cuticle tissues was studied using confocal laser scanning microscopy (CLSM). AMX showed high solubility in glyceryl monostearate (GMS) and stearic acid, 28.87 ± 2.17 and 58.06 ± 2.227mg/g, respectively. The results of physicochemical characterization showed that formula A7 was the optimized one. It is composed of GMS (solid lipid), oleic acid:garlic oil (1:1 v/v) (liquid lipid), and a surfactant/co-surfactant mixture (Cremophor EL/Transcutol HP).The particle size (PS) was 238.0 ± 2.13nm, entrapment efficiency (EE) 100.535 ± 6.73%, and zeta potential (ZP) - 29.3 ± 0.93 mv. Ex vivo permeation study demonstrates the potential of AMX-NLC (formula A7) as a delivery system for AMX. The CLSM highly proved AMX-loaded NLC penetration through the skin. The histological study clearly demonstrated that AMX-loaded NLC promoted hair growth more effectively than the market product in chemotherapy-induced alopecia rats. The acquired findings revealed that targeting of AMX-loaded NLC into hair follicles was improved.