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

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 •) 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 IC 50 of 9.2 ± 0.2 μg/ mL, superior to results obtained for LE (10.8 μg/mL) and butylated hydroxytoluene (BHT), a synthetic antioxidant (12.5 μg/mL). MIC and MFC against Candida albicans (ATCC1023) were 312.5 μg/mL and 1250 μg/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.

Spouted Bed Dried Rosmarinus officinalis Extract: A Novel Approach for Physicochemical Properties and Antioxidant Activity

“…The results of AA of the rosemary extracts assessed by DPPH • * and LPO assays evidenced a slight to moderate decrease in the AA of the rosemary extracts caused by the SB drying operation, apparently due to degradation of bioactive compounds on exposure to the processing conditions used in this study; mainly heated air. It is known that polyphenolic compounds are thermolabile and their efficacy may be compromised on exposure to heat [61]. However, the SB dried rosemary extracts here produced are near 13.5 times more concentrated than the concentrated extract (in dry weight); and have high concentration of bioactive compounds by extract mass (in wet basis).…”

Liposomal Encapsulation of Phenolic Compounds for Augmentation of Bio‐Efficacy: A Review

“…In this case, proliposome contained 9.73 % (w/w) silymarin. Bankole et al [68] . and Hızır‐Kadı et al [69] .…”

Spray-Dried Structured Lipid Carriers for the Loading of Rosmarinus officinalis: New Nutraceutical and Food Preservative

“…Recently, the use of standardized dried extracts is a trend of the industry. Encapsulation of phytochemicals in drug delivery systems is a suitable way to improve their physical-chemical properties, prevent their degradation, and also to improve their bioavailability in biological settings [34,35]. The highly lipophilic nature of rosemary antioxidants makes encapsulation in lipid systems the most suitable.…”

“…The spray-drying, one of the most used drying techniques, is widely used to standardize phytopharmaceutical ingredients, ensuring product efficacy, safety, and quality [37]. It is also a widely used approach for the microencapsulation of compounds of different chemical nature, producing microspheres or microcapsules, according to the initial feed material [34,38,39].…”

“…The highly lipophilic nature of rosemary antioxidants makes encapsulation in lipid systems the most suitable. The solid form has clear advantages over the conventional liquid form, namely: higher physicochemical and microbiological stability; ease of standardization; a higher bioactive content; ease in logistics processes; and the possibility to be used under distinct dosage forms [ 34 , 36 ]. The spray-drying, one of the most used drying techniques, is widely used to standardize phytopharmaceutical ingredients, ensuring product efficacy, safety, and quality [ 37 ].…”