Atorvastatin-loaded emulsomes foam as a topical antifungal formulation

Dermal fungal infection faces many challenges, especially for immunocompromised patients. Recently, the repositioning of atorvastatin (ATO) as a promising anti-mycoses therapy is used to overcome some issues of conventional therapeutic agents such as microbial resistance. The goal of this study was to develop a suitable formula for dermal fungal infection. Wherefore, ATO was entrapped into emulsomes and then incorporated in a foam system for topical convenient application. The D-optimal design was used for the optimization of ATO-emulsome and foam to achieve suitable responses. Regarding emulsomes, cholesterol weight and sonication time were independent variables that impact emulsome size, polydispersity index, surface charge, and entrapment efficiency.

The optimum formula showed a size of 359.4 ± 8.97 nm, PDI of 0.4752 ± 0.012, a zeta potential of −21.27 ± 0.53 mV, and a drug entrapment of 95 ± 2.38%. Transmission electron microscope and Fourier-transform infrared spectroscopy (FT-IR) proved the assembly of ATO-emulsome. Foam composition was optimized to achieve good expansion, stability, and viscosity using a surfactant triple mixture and hydroxypropyl methylcellulose. The selected ATO-emulsome foam which consisted of 1% HPMC, 1.249% SDS, and 4% pluronic showed prolonged drug release. Efficient permeation through skin layers was asserted by using a confocal laser scanning microscope. Moreover, the homogenous distribution of the foam bubbles upholds stability and conserves the system from rapid collapse. The antifungal activity was confirmed by an in-vitro and in-vivo microbiology study beside in-vivo biocompatibility. In conclusion, ATO-emulsome and incorporation in foam have demonstrated good antifungal activity which presented a unique aspect for potential clinical applications.

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Materials

Atorvastatin calcium was a kind gift from EIPICO, Egypt. Compritol 888 ATO was kindly gifted from Gatteffose, France. Soya phosphatidylcholine, cholesterol, sodium dodecyl sulfate (SDS), Pluronic f127, hydroxypropyl methylcellulose (HPMC), and cellulose membrane (Molecular weight cut off: 12,000), were purchased from Sigma-Aldrich (St. Loius, MO, U.S.A.). Propylene Glycol, tween 20, and buffer phosphate salts were purchased from El- Nasr Pharmaceutical Co. (Cairo, Egypt). All other used Chemicals were of analytical grade.

Alaa S. Eita, Amna M.A. Makky, Asem Anter, Islam A. Khalil, Atorvastatin-loaded emulsomes foam as a topical antifungal formulation, International Journal of Pharmaceutics: X, 2022, 100140, ISSN 2590-1567, https://doi.org/10.1016/j.ijpx.2022.100140.