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AKVANO?: A Novel Lipid Formulation System for Topical Drug Delivery-In Vitro Studies

Pharmaceutics(2022)

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摘要
A novel formulation technology called AKVANO (R) has been developed with the aim to provide a tuneable and versatile drug delivery system for topical administration. The vehicle is based on a water-free lipid formulation where selected lipids, mainly phospholipids rich in phosphatidylcholine, are dissolved in a volatile solvent, such as ethanol. With the aim of describing the basic properties of the system, the following physicochemical methods were used: viscometry, dynamic light scattering, NMR diffusometry, and atomic force microscopy. AKVANO formulations are non-viscous, with virtually no or very minute aggregates formed, and when applied to the skin, e.g., by spraying, a thin film consisting of lipid bilayer structures is formed. Standardized in vitro microbiological and irritation tests show that AKVANO formulations meet criteria for antibacterial, antifungal, and antiviral activities and, at the same time, are being investigated as a non-irritant to the skin and eye. The ethanol content in AKVANO facilitates incorporation of many active pharmaceutical ingredients (>80 successfully tested) and the phospholipids seem to act as a solubilizer in the formulation. In vitro skin permeation experiments using Strat-M (R) membranes have shown that AKVANO formulations can be designed to alter the penetration of active ingredients by changing the lipid composition.
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关键词
topical drug delivery,phospholipids,physicochemical methods,atomic force microscopy,antibacterial,antiviral,antifungal,in vitro skin irritation,in vitro eye irritation,in vitro skin permeation
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