Fabrication and optimization of raloxifene loaded spanlastics vesicle for transdermal delivery

This research work is envisioned for the development and optimization of Raloxifene HCL loaded spanlastics. Raloxifene HCL, a selective estrogen receptor modulator (SERM), is active for the deterrence and management of postmenopausal osteoporosis. Spanlastics nanocarrier was prepared by ethanol injection method and optimized for independent variables by using Box Behnken design. The independent variables used in the experiment were concentration of Span 60, Tween 80 as an edge activator, and sonication time. The individual and joined impacts of independent variables were assessed on vesicle size, polydispersity index (PDI), and encapsulation efficiency (EE). Raloxifene HCL and formulation were analyzed by FT-IR, DSC and XRD. Raloxifene HCL loaded spanlastics were characterized for particle size, PDI, EE, and in-vitro drug release. Ex vivo skin permeation and stability studies were performed for the optimized formulation. The optimized spanlastics vesicle showed a particle size of 275.4 nm with PDI, 0.267 which was suitable for permeation through skin layers. TEM image illustrated well dispersed nanocarrier with spherical shape. The % cumulative drug release and transdermal flux for the optimized spanlastics formulation were found to be 85% (Approx. after 24 h) and 4.24 mu g/cm2/hr respectively. The enhanced permeation across the skin layers was proposed to be due to the presence of ethanol which will increase the lipid fluidity of the stratum corneum and will help to penetrate the drug. Later the skin penetration ability was determined by confocal laser scanning microscopy (CLSM) and showed that rhodamine loaded spanlastics formulation penetrated to the depth of 54.9 mu m while rhodamine suspension limited to 20 mu m in the skin. We can conclude that raloxifene HCL loaded spanlastics could serve as a better approach to deliver drug in deeper layers of the skin.

Automated summary

This research aims to develop and optimize Raloxifene HCL loaded spanlastics. A nanocarrier was prepared using ethanol injection method and optimized using Box Behnken design. The effects of independent variables on vesicle size, polydispersity index, and encapsulation efficiency were evaluated. The optimized spanlastics formulation showed suitable particle size for skin permeation. Various characterization and release studies were performed. The result indicated that Raloxifene HCL loaded spanlastics could be a better approach for delivering drugs in deeper layers of the skin.