Formulation and anti-neurotoxic activity of baicalein-incorporating neutral nanoliposome

Despite extensive studies of the effects of herbal-derived small molecules in the biopharmaceutical and biomedical sciences, their low solubility and stability remain a challenge. Here we focus on baicalein, a small molecule showing potential against neurodegenerative diseases such as Parkinson's and Alzheimer's. However, therapeutic usage in vivo is challenged by low solubility and stability. To address this we have applied neutrally-charged nanoliposome (NLP) as carrier for baicalein. Baicalein was incorporated into NLP to form NLP-Ba at molar baicalain:lipid ratios of up to 1:3, giving a drug entrapment efficiency of 96.71%, slow release of approximately 22% after a week and increased baicalein stability up to 27%. Ascorbic acid increased baicalein's stability further, particularly when incorporated in NLP where baicalein stability intensified by 53% in NLP-Ba. Moreover, NLP-Ba did not show significant cytotoxic effects against neurons; rather, showed considerable protective effect against reactive oxygen species. In addition, NLP promoted internalization of baicalein into cells, showing good biocompatibility. We conclude that NLP-Ba can enhance baicalein's therapeutic potential in neurodegenerative diseases. (C) 2017 Elsevier B.V. All rights reserved.