Edge Activator: Effect of Concentration Variation of Tween 80 on Characteristics and Rate of Difusion transfersome sodium diclofenac

Diclofenac sodium is a Transfersom is a transdermal delivery system consisting of phospholipids and edge activators. Transfersom increases the size of the stratum corneum lipid barrier pores, then enters the skin through the drive of the trans-barrier motion and squeezes itself to follow the lipid barrier pore size. The purpose of this study is to determine the effect of the tween-80 concentration as an edge activator on the characteristics and diffusion rate of diclofenac sodium transfersom. Transferom preparation used the vortex-sonication method which was made in five formulae with variations in the concentration ratio of phosphatidylcholine and tween-80 (95:05, 90:10, 85:15, 80:20, and 75:25). The results show that all five formulae have different morphological forms. The results of statistical tests using One-Way ANOVA finds a significant effect (p-value) of the edge activator concentration on the diffusion rate of diclofenac sodium transfersom.

Impact of Alkanediols on Stratum Corneum Lipids and Triamcinolone Acetonide Skin Penetration

Alkanediols are widely used as multifunctional ingredients in dermal formulations. In addition to their preservative effect, considering their possible impact on drug penetration is also essential for their use. In the present study, the influence of 2-methyl-2,4-pentanediol, 1,2-pentanediol, 1,2-hexanediol and 1,2-octanediol on the skin penetration of triamcinolone acetonide from four different semisolid formulations was investigated. Furthermore, confocal Raman spectroscopy measurements were performed to examine the influence of the alkanediols on stratum corneum lipid content and order. Alkanediols were found to increase the penetration of triamcinolone acetonide. However, the extent depends strongly on the formulation used. In certain formulations, 1,2-pentanediol showed the highest effect, while in others the penetration-enhancing effect increased with the alkyl chain length of the alkanediol used. None of the tested alkanediols extracted lipids from the stratum corneum nor reduced its thickness. Notwithstanding the above, the longer-chained alkanediols cause the lipids to be converted to a more disordered state, which favors drug penetration. This behavior could not be detected for the shorter-chained alkanediols. Therefore, their penetration-enhancing effect is supposed to be related to an interaction with the hydrophilic regions of the stratum corneum.

Development of a Self-Emulsifying Drug Delivery System for Optimized Topical Delivery of Clofazimine

A quality-by-design and characterization approach was followed to ensure development of self-emulsifying drug delivery systems (SEDDSs) destined for topical delivery of the highly lipophilic clofazimine. Solubility and water-titration experiments identified spontaneous emulsification capacity of different excipient combinations and clofazimine. After identifying self-emulsification regions, check-point formulations were selected within the self-emulsification region by considering characteristics required to achieve optimized topical drug delivery. Check-point formulations, able to withstand phase separation after 24 h at an ambient temperature, were subjected to characterization studies. Experiments involved droplet size evaluation; size distribution; zeta-potential; self-emulsification time and efficacy; viscosity and pH measurement; cloud point assessment; and thermodynamic stability studies. SEDDSs with favorable properties, i.e., topical drug delivery, were subjected to dermal diffusion studies. Successful in vitro topical clofazimine delivery was observed. Olive oil facilitated the highest topical delivery of clofazimine probably due to increased oleic acid levels that enhanced stratum corneum lipid disruption, followed by improved dermal clofazimine delivery. Finally, isothermal microcalometric experiments studied the compatibility of excipients. Potential interactions were depicted between argan oil and clofazimine as well as between Span®60 and argan-, macadamia- and olive oil, respectively. However, despite some mundane incompatibilities, successful development of topical SEDDSs achieved enhanced topical clofazimine delivery.