Sulforaphane-Loaded Ultradeformable Vesicles as A Potential Natural Nanomedicine for the Treatment of Skin Cancer Diseases

Abstract

Sulforaphane is a multi-action drug and its anticancer activity is the reason for the continuous growth of attention being paid to this drug. Sulforaphane shows an in vitro antiproliferative activity against melanoma and other skin cancer diseases. Unfortunately, this natural compound cannot be applied in free form on the skin due to its poor percutaneous permeation determined by its physico-chemical characteristics. The aim of this investigation was to evaluate ethosomes® and transfersomes® as ultradeformable vesicular carriers for the percutaneous delivery of sulforaphane to be used for the treatment of skin cancer diseases. The physico-chemical features of the ultradeformable vesicles were evaluated. Namely, ethosomes® and transfersomes® had mean sizes <400 nm and a polydispersity index close to 0. The stability studies demonstrated that the most suitable ultradeformable vesicles to be used as topical carriers of sulforaphane were ethosomes® made up of ethanol 40% (w/v) and phospholipon 90G 2% (w/v). In particular, in vitro studies of percutaneous permeation through human stratum corneum and epidermis membranes showed an increase of the percutaneous permeation of sulforaphane. The antiproliferative activity of sulforaphane-loaded ethosomes® was tested on SK-MEL 28 and improved anticancer activity was observed in comparison with the free drug.

<p>Self-Assembled Lecithin/Chitosan Nanoparticles Based on Phospholipid Complex: A Feasible Strategy to Improve Entrapment Efficiency and Transdermal Delivery of Poorly Lipophilic Drug</p>

“…These two vesicular colloidal carriers improve skin permeability significantly compared with other lipid nanocarriers due to the favorable flexibility and deformability conferred by the presence of edge-activator agents (ie, ethanol and sodium cholate), which is different from the mechanism underlying LCNs' enhanced penetration effect. [44][45][46][47][48] As expected, BPC-loaded ethosomes (BPC-ETHs) significantly improved the transdermal permeability of baicalein compared with free baicalein and BPC, as shown by the high values of Q n and Jss. Even more noteworthy is that BPC-LCNs exhibited a trend of enhanced permeability as compared to BPC-ETHs, which may be attributed to the enhanced penetration effect of chitosan which changed the morphology of the stratum corneum and opened the tight conjugation of the corneocyte layers.…”

<p>Potential of Nanoparticles as Permeation Enhancers and Targeted Delivery Options for Skin: Advantages and Disadvantages</p>

“…51 These types of nanocarriers have the advantage of long-term stability and modified drug release kinetics. Although the topical route of administration has many drawbacks in skin drug delivery because of the limitation of skin permeation and stability concerns, 52 a rational selection of suitable nanocarriers according to physicochemical properties of active pharmaceuticals led to preparation of successful delivery system. Paclitaxel-loaded ethosome has been studied as a potential therapy for squamous cell carcinoma.…”

Breast Cancer Prevention-Is there a Future for Sulforaphane and Its Analogs?

“…Hence, some effort are made to improve stability of SFN in body fluids. One approach is to use nanaocarriers based on either natural or the synthetic polymers [83,84]. Soni et al have described preparation of SFN-loaded nanostructured lipid carriers.…”