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AKVANO:一种用于局部给药的新型脂质制剂系统——体外研究

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

作者信息

Holmbäck Jan, Rinwa Vibhu, Halthur Tobias, Rinwa Puneet, Carlsson Anders, Herslöf Bengt

机构信息

Lipidor AB, Svärdvägen 13, SE-182 33 Danderyd, Sweden.

Department of Materials and Environmental Chemistry, Stockholm University, Svante Arrhenius väg 16C, SE-106 91 Stockholm, Sweden.

出版信息

Pharmaceutics. 2022 Apr 5;14(4):794. doi: 10.3390/pharmaceutics14040794.

Abstract

A novel formulation technology called AKVANO® 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® membranes have shown that AKVANO formulations can be designed to alter the penetration of active ingredients by changing the lipid composition.

摘要

一种名为AKVANO®的新型制剂技术已经研发出来,旨在为局部给药提供一种可调节且通用的药物递送系统。该载体基于无水脂质制剂,其中选定的脂质(主要是富含磷脂酰胆碱的磷脂)溶解于挥发性溶剂(如乙醇)中。为了描述该系统的基本特性,采用了以下物理化学方法:粘度测定法、动态光散射法、核磁共振扩散法和原子力显微镜法。AKVANO制剂无粘性,几乎不形成或仅形成极微小的聚集体,当通过喷雾等方式应用于皮肤时,会形成由脂质双层结构组成的薄膜。标准化的体外微生物学和刺激性测试表明,AKVANO制剂符合抗菌、抗真菌和抗病毒活性标准,同时正在作为对皮肤和眼睛无刺激性的制剂进行研究。AKVANO中的乙醇含量有助于许多活性药物成分的掺入(已成功测试超过80种),并且磷脂似乎在制剂中起到增溶剂的作用。使用Strat-M®膜进行的体外皮肤渗透实验表明,AKVANO制剂可以通过改变脂质组成来设计,以改变活性成分的渗透。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/8c8e/9030418/618590d18b3e/pharmaceutics-14-00794-g001.jpg

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