title: Development of a liposome-based formulation for vitamin K1 nebulization on the skin.
abstract: Vitamin K1 (VK1) is a very lipophilic and photosensitive molecule contained in some vegetables. Recently, the use of VK1 on the skin has been proposed for different pharmaceutical or cosmeceutical applications. In this study, an innovative strategy for the administration of VK1 on the skin was proposed. In particular, to overcome the drawbacks associated with a VK1-containing fatty ointment available on the market, an aqueous formulation suitable to be administered by nebulization was developed. The use of liposomes encapsulating VK1 enabled issues due to the lipophilicity of VK1 to be overcome. Thus, different liposomal formulations, with different VK1 concentrations, were prepared and characterized in terms of size, zeta potential, VK1 encapsulation into liposomes, and stability of the formulations during storage. After a first phase of screening, the selected formulation was tested by a portable device for nebulization. No alteration of the vesicle characteristics following the liposome supply through the nebulizer was found. Finally, permeation studies were carried out on pig-excised skin in Franz cells and the newly developed formulation was compared to a marketed VK1-containing ointment. In this test, an enhanced VK1 accumulation into the skin was found when using nebulized liposomes. In conclusion, in order to administer VK1 on the skin, the newly developed formulation could be a valid alternative to the products available on the market today. In particular, the use of liposomes could facilitate the multiple administrations per day by aerosol, but also increase, compared to a semi-solid preparation, the accumulation of VK1 into the epidermis and dermis.
authors.affiliation: Department of Pharmacy, Università degli Studi di Napoli Federico II, Naples, Italy ; Xenus Srl, Rome, Italy.
authors.forename: Virginia
authors.initials: V
authors.lastname: Campani
authors.affiliation: Department of Pharmacy, Università degli Studi di Napoli Federico II, Naples, Italy.
authors.forename: Dario
authors.initials: D
authors.lastname: Marchese
authors.affiliation: Xenus Srl, Rome, Italy.
authors.forename: Maria Teresa
authors.initials: MT
authors.lastname: Pitaro
authors.affiliation: Xenus Srl, Rome, Italy.
authors.forename: Michele
authors.initials: M
authors.lastname: Pitaro
authors.affiliation: Department of Pharmacy, Università degli Studi di Napoli Federico II, Naples, Italy.
authors.forename: Paolo
authors.initials: P
authors.lastname: Grieco
authors.affiliation: Department of Pharmacy, Università degli Studi di Napoli Federico II, Naples, Italy.
authors.forename: Giuseppe
authors.initials: G
authors.lastname: De Rosa
mesh_terms: D000336:Aerosols / Q000008:administration & dosage / Q000138:chemical synthesis / Q000493:pharmacokinetics; D000818:Animals; D004339:Drug Compounding / Q000379:methods; D066298:In Vitro Techniques; D008081:Liposomes / Q000138:chemical synthesis*; D053769:Nanocapsules / Q000008:administration & dosage* / Q000737:chemistry*; D009330:Nebulizers and Vaporizers; D012869:Skin Absorption / Q000502:physiology*; D013552:Swine; D010837:Vitamin K 1 / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*
chemical_list: D000336:Aerosols; D008081:Liposomes; D053769:Nanocapsules; D010837:Vitamin K 1
keywords: Franz cells; liposome nebulization; liposome stability; liposomes
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