4.4 Article

Spray-Dried Proliposomes: an Innovative Method for Encapsulation of Rosmarinus officinalis L. Polyphenols

Journal

AAPS PHARMSCITECH
Volume 21, Issue 5, Pages -

Publisher

SPRINGER
DOI: 10.1208/s12249-020-01668-2

Keywords

rosemary polyphenols; proliposomes; spray drying; design of experiment; antioxidant activity; antifungal activity

Funding

  1. State of Sao Paulo Research Foundation (FAPESP) [2011/10333-1, 2014/15905-1, 2018/26069-0]
  2. Nigerian Tertiary Education Trust Fund (TETFUND)
  3. Coordination for the Improvement of Higher Education Personnel (CAPES) [001]

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This work aims to improve the functionality of Rosmarinus officinalis L. (rosemary) polyphenols by encapsulation in an optimized proliposome formulation. A 2(3) Box-Wilson central composite design (CCD) was employed to determine lone and interaction effects of composition variables on moisture content (X-p); water activity (A(w)); concentration and retention of rosemary polyphenols-rosmarinic acid (ROA), carnosol (CAR), and carnosic acid (CNA); and recovery of spray-dried proliposomes (SDP). Processing conditions which generate proliposomes with optimum physicochemical properties were determined by multi-response analysis (desirability approach). Antioxidant and antifungal activities were evaluated by 1,1-diphenyl-2-picrylhydrazyl (DPPH center dot) sequestering and minimum inhibitory concentration (MIC)/minimum fungicidal concentration (MFC) assays, respectively. SDP exhibited high polyphenol retention, ranging from 62.0 to 100.0% w/w, showing dependence on composition variables and polyphenol lipophilicity. SDP recovery ranged from 20.1 to 45.8%, with X-p and A(w) of 1.7 +/- 0.14-2.5 +/- 0.23% w/w and 0.30 +/- 0.004-0.47 +/- 0.003, respectively, evidencing product with good chemical and microbiological stability. Optimum liposomal composition was determined, namely, lipid concentration (4.26% w/w), lyophilized extract (LE) concentration (4.48% w/w), and drying aid:(lipid+extract) ratio (7.55% w/w) on wet basis. Relative errors between experimental and predicted values for SDP properties showed concurrence for all responses except CAR retention, being 22% lower. SDP showed high antioxidant activity with IC50 of 9.2 +/- 0.2 mu g/mL, superior to results obtained for LE (10.8 mu g/mL) and butylated hydroxytoluene (BHT), a synthetic antioxidant (12.5 mu g/mL). MIC and MFC against Candida albicans (ATCC1023) were 312.5 mu g/mL and 1250 mu g/mL, respectively, a moderate antimicrobial activity for phytochemical-based products. SDP is shown as a veritable tool to encapsulate hydrophilic and lipophilic rosemary polyphenols generating a product with optimal physicochemical and biological properties.

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