Characterization of cubosomes as a targeted and sustained transdermal delivery system for capsaicin

Abstract

Phytantriol- and glycerol monooleate-based cubosomes were produced and characterized as a targeted and sustained transdermal delivery system for capsaicin. The cubosomes were prepared by emulsification and homogenization of phytantriol (F1), glycerol monooleate (F2), and poloxamer dispersions, characterized for morphology and particle size distribution by transmission electron microscope and photon correlation spectroscopy. Their Im3m crystallographic space group was confirmed by small-angle X-ray scattering. An in vitro release study showed that the cubosomes provided a sustained release system for capsaicin. An in vitro diffusion study conducted using Franz diffusion cells indicated that the skin retention of capsaicin from cubosomes in the stratum corneum was much higher (2.75±0.22 μg versus 4.32±0.13 μg, respectively) than that of capsaicin cream (0.72±0.13 μg). The stress testing showed that the cubosome formulations were stable under strong light and high temperature for up to 10 days. After multiapplications on mouse skin, the irritation of capsaicin cubosomes and cream was light with the least amount of side effects. Overall, the present study demonstrated that cubosomes may be a suitable skin-targeted and sustained delivery system for the transdermal administration of capsaicin.

Cubosomes: The Next Generation of Smart Lipid Nanoparticles?

“…The samples were then tested in vivo on mice and showed no signs of irritation, indicating that cubosomes may be a viable alternative to currently available commercial creams. [139] The majority of ocular problems and illnesses are treated with eye drops. However, key problems include corneal permeability, retention times and low solubility of some drugs.…”

Formulation and Evaluation of Cubosomes as Skin Retentive System for Topical Delivery of Clotrimazole

“…Recently, it has been envisioned that cubosomes can act as an ideal drug delivery system for drugs with poor loading and permeability for the treatment of topical fungal infections 12 .Moreover,ithas been reported that cubosomes can serve as a potential skin retentive system [13][14] .…”

“…Unique structure of cubosomes can incorporate wide varieties of drugs (hydrophilic, lipophilic and amphiphilic) with high pay load owing to their high internal surface area (400 m 2 /g) 12,[16][17] . Various investigations have also indicated the sustained and prolonged drug delivery properties of cubosomes 14,18 . Moreover, similarities between the bicontinuous structures formed in human skin layers and those comprising cubic phases 19 , offering the promise of better skin retention and transport.…”

Development of a HPLC Method for the Quantitative Determination of Capsaicin in Collagen Sponge

“…Yet capsaicin is actually irritant to human skin producing a burning sensation [2], and because of its high degree of first-pass metabolism in gastric intestinal track and short half-life by intravenous administration (7.06 min) [3, 4], transdermal delivery system seems to be more advantageous for capsaicin. In our previous research, we chose cataplasm [5], cubic phase gel [6, 7], and cubosome [8, 9] as transdermal delivery system providing the sustained release for capsaicin.…”