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Major polyphenols in Rosmarinus officinalis L. primarily consist of phenolic acids, phenolic diterpenes, and flavonoids, all of which have pharmacological properties including anti-inflammatory and antibacterial characteristics. Numerous in vitro and animal studies have found that rosemary polyphenols have the potential to decrease the severity of intestinal inflammation. The beneficial effects of rosemary polyphenols were associated with anti-inflammatory properties, including improved gut barrier (increased mucus secretion and tight junction), increased antioxidant enzymes, inhibiting inflammatory pathways and cytokines (downregulation of NF-κB, NLRP3 inflammasomes, STAT3 and activation of Nrf2), and modulating gut microbiota community (increased core probiotics and SCFA-producing bacteria, and decreased potential pathogens) and metabolism (changes in SCFA and bile acid metabolites). This paper provides a better understanding of the anti-inflammatory properties of rosemary polyphenols and suggests that rosemary polyphenols might be employed as strong anti-inflammatory agents to prevent intestinal inflammation and lower the risk of inflammatory bowel disease and related diseases.

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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 23 Box-Wilson central composite design (CCD) was employed to determine lone and interaction effects of composition variables on moisture content (Xp); water activity (Aw); 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 Xp and Aw 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 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.

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BACKGROUND: Rosmarinus officinalis is an aromatic plant used in folk medicine as a result of the therapeutic properties associated with its phenolic composition, being rich in rosmarinic acid (RA) and caffeic acid (CA). To better understand the bioactivity of these compounds, their absorption and metabolism were assessed in human Caco-2 and HepG2 cells, as small intestine and liver models, respectively, using RA and CA standards, as well as a rosemary infusion and ferulic acid (FA). RESULTS: Test compounds were partially up-taken and metabolized by Caco-2 and HepG2 cells, although a higher metabolization rate was observed after hepatic incubation compared to intestinal incubation. CA was the compound best absorbed followed by RA and FA, showing metabolites percentages of 30.4%, 11.8% and 4.4% in Caco-2 and 34.3%, 10.3% and 3.2% in HepG2 cells, respectively. RA in the rosemary infusion showed improved bioavailability compared to pure RA. Methyl derivatives were the main metabolites detected for CA and RA after intestinal and hepatic metabolism, followed by methyl-glucuronidates and glucuronidates. RA was also minimally hydrolyzed into CA, whereas FA only was glucuronidated. Rosemary polyphenols followed the same biotransformation pathways as the standards. In addition, phase II derivatives of luteolin were observed. CONCLUSION: Rosemary polyphenols are partially metabolized in both the intestine and liver. © 2018 Society of Chemical Industry.

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The present study evaluates the potential of encapsulation of polyphenolic antioxidants from rosemary (Rosmarinus officinalis L.) leaves by combining emulsification and spray drying techniques. To stabilize the emulsions and prepare samples suitable for use in dry products, double emulsions encapsulating rosemary polyphenolic extract and containing polyglycerol polyricinoleate (4%), whey protein isolates (2 and 4%) as emulsifiers, and maltodextrins (MDE 10 and 21) as enhancing coatings were subjected to spray drying. The obtained results show insignificant (p>0.05) effect of used maltodextrin type and protein content on mean particle size of double emulsions containing rosemary polyphenols. Morphology analyses showed that double emulsions were successfully prepared, spherical microcapsules were obtained after spray drying of double emulsions and double emulsion form was still preserved after rehydration of spray-dried microcapsules. Regardless of used maltodextrins, significantly (p>0.05) higher encapsulation efficiencies (EE) of total polyphenols (39.57 and 42.83%) in rehydrated samples were achieved when higher protein content (4% whey protein isolate) was used, indicating the major impact of protein content on EE of rosemary polyphenols. Also, using HPLC analysis, rosmarinic and caffeic acids, apigenin and luteolin derivatives were detected among specific polyphenols, where rosmarinic acid had notable encapsulation efficiency ranging from 62.15 to 67.43%. In this way, the obtained microcapsules encapsulating rosemary polyphenols could be easily blended with various dry mixtures, and serve for delivery in different functional products.