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

Author(s)

Bankole, Victor Oloruntoba ^{[1, 2]} ; Osungunna, Michael Oluwole ^{[1, 2]} ; Fernandes Souza, Claudia Regina ^[1] ; Salvador, Sergio Luiz ^[1] ; Oliveira, Wanderley Pereira ^[1]

Affiliation

^[1] Univ Sao Paulo, Fac Pharmaceut Sci Ribeirao Preto, Av Cafe S-N, Ribeirao Preto 14040903, SP - Brazil

^[2] Obafemi Awolowo Univ, Fac Pharm, Dept Pharmaceut, Ife 220005 - Nigeria

• Document type: Journal article
• Source: AAPS PHARMSCITECH; v. 21, n. 5 MAY 18 2020.
• Web of Science Citations: 0

Abstract

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. (AU)

• FAPESP's process: 14/15905-1 - Encapsulation of essential oils in solid lipid carriers: technological development and applications
• Grantee: Wanderley Pereira Oliveira
• Support Opportunities: Regular Research Grants
• FAPESP's process: 18/26069-0 - Encapsulation of essential oils for use in pharmaceutical compositions with antimicrobial activity
• Grantee: Wanderley Pereira Oliveira
• Support Opportunities: Regular Research Grants
• FAPESP's process: 11/10333-1 - Microencapsulation and nanoencapsulation of natural compounds by drying technologies
• Grantee: Cláudia Regina Fernandes de Souza
• Support Opportunities: Research Grants - Young Investigators Grants