Development and Efficacy Evaluation of Innovative Cosmetic Formulations with Caryocar brasiliense Fruit Pulp Oil Encapsulated in Freeze-Dried Liposomes.

Encapsulation and drying technologies allow the engineering of innovative raw materials from plant biodiversity, with potential applications in pharmaceutical and cosmetic fields. Lipid-based nanoencapsulation stands out for its efficiency, ease of production, and versatility in encapsulating substances, whether hydrophilic or lipophilic. This work aimed at encapsulating pequi oil in liposomes and freeze-dried liposomes to enhance its stability and functional benefits, such as skin hydration and anti-aging effects, for use in innovative cosmetic formulations. Pequi oil-extracted from the Caryocar brasiliense fruit pulp, a plant species from Brazilian plant biodiversity-is rich in secondary metabolites and fatty acids. Liposomes and dried liposomes offer controlled production processes and seamless integration into cosmetic formulations. The physicochemical analysis of the developed liposomes confirmed that the formulations are homogeneous and electrokinetically stable, as evidenced by consistent particle size distribution and zeta potential values, respectively. The gel-type formulations loaded with the dried liposomes exhibit enhanced skin hydration, improved barrier function, and refined microrelief, indicating improvements in skin conditions. These results highlight the potential of dried liposomes containing pequi oil for the development of innovative cosmeceutical products. This research contributes to the valorization of Brazilian biodiversity by presenting an innovative approach to leveraging the dermatological benefits of pequi oil in cosmetic applications.

Characterization, Antimicrobial Activity, and Antioxidant Efficacy of a Pomegranate Peel Solution Against Persistent Root Canal Pathogens.

BACKGROUND: The limitations of dental irrigation solutions reinforce the need to explore novel bioactive compounds that are safer and biodegradable. This study aimed to prepare a 10% pomegranate peel solution (Punica granatum extract - PGE) and evaluate its antimicrobial and antioxidant effects for root canal treatment. METHODS: Lyophilized extracts (1g/10 mL) from pomegranate peels were prepared, and the punicalagin content was assessed by ultra-performance liquid chromatography using pure punicalagin (standard). The antimicrobial activity was tested against common persistent root canal pathogens by the agar diffusion method, minimum inhibitory concentration (MIC), and minimum bactericidal/fungicide concentration (MCB/MFC). The antioxidant activity (%AA) was assessed by the DPPH radical scavenging method. Data were analyzed by ANOVA and Tukey's test (α = 0.05). RESULTS: The total phenolic content of the PGEextract was 6.55 µg/mL. Differences were found among the inhibition zone of PGE (23.32 ± 3.65), 1% NaOCl (30.76 ± 4.73), and 50% ethanol (without inhibition) (p < 0.05). The MIC values of PGE ranged between 6.25 and 75 mg/ml, and PGE was effective against the tested pathogens. PGE had antioxidant potential (IC50 = 3.52 µg/mL); however, the mean values were inferior to that of the quercetin (positive control) (IC50 = 0.95 µg/mL). The DPPH scavenging effect (%AA) of PGE (70.98 ± 2.3) had no difference from the positive control (72.94 ± 2.1) (p = 0.253). CONCLUSION: The PGE extract was successfully biosynthesized and exhibited antimicrobial and antioxidant activity, suggesting its potential use as an adjuvant therapy during root canal treatment.

Process Development for the Spray-Drying of Probiotic Bacteria and Evaluation of the Product Quality.

Probiotics and prebiotics are of great interest to the food and pharmaceutical industries due to their health benefits. Probiotics are live bacteria that can confer beneficial effects on human and animal wellbeing, while prebiotics are types of nutrients that feed the beneficial gut bacteria. Powder probiotics have gained popularity due to the ease and practicality of their ingestion and incorporation into the diet as a food supplement. However, the drying process interferes with cell viability since high temperatures inactivate probiotic bacteria. In this context, this study aimed to present all the steps involved in the production and physicochemical characterization of a spray-dried probiotic and evaluate the influence of the protectants (simulated skim milk and inulin:maltodextrin association) and drying temperatures in increasing the powder yield and cell viability. The results showed that the simulated skim milk promoted higher probiotic viability at 80 °C. With this protectant, the probiotic viability, moisture content, and water activity (Aw) reduce as long as the inlet temperature increases. The probiotics' viability decreases conversely with the drying temperature. At temperatures close to 120 °C, the dried probiotic showed viability around 90%, a moisture content of 4.6% w/w, and an Aw of 0.26; values adequate to guarantee product stability. In this context, spray-drying temperatures above 120 °C are required to ensure the microbial cells' viability and shelf-life in the powdered preparation and survival during food processing and storage.

Electrospun Poly (Vinyl Alcohol) Nanofibrous Mat Loaded with Green Propolis Extract, Chitosan and Nystatin as an Innovative Wound Dressing Material.

Purposes: The objective of this work was to produce and characterise biodegradable poly (vinyl alcohol) (PVA) nanofibre loaded with green propolis extract (GPE), chitosan (CS) and nystatin (NYS) alone and in mixtures as a potential wound dressing material. Methods: The GPE, NYS and CS1% were loaded in electrospinning compositions based on PVA 7%, 8% and 12% solubilised in milli-Q water or a mixture of water and glacial acetic acid. The electrospinning compositions without actives (blank) and those loaded with actives were characterised by determining the pH, electrical conductivity and rheological properties. An image analysis procedure applied to photomicrographs obtained by scanning electronic microscopy (SEM) allowed the determination of the nanofibres' diameter distribution and average surface porosity. The disintegration time and swelling ratio of the nanofibre mats were also determined. Results: The physicochemical parameters of the electrospinning compositions (pH, electrical conductivity and rheology) and the incorporated active ingredients (GPE, CS and NYS) affected the electrospun nanofibre mats properties. The electrospun nanofibres' mean diameters and surface porosity ranged from 151.5 to 684.5 nm and from 0.29 ± 0.04 to 0.50 ± 0.05. The PVA/CS electrospun nanofibres fibres exhibited the smallest diameters, high surface porosity, water absorption capacity and disintegration time. The characteristics of the PVA/CS nanofibres mat associated with the biodegradability of the polymers make them a novel material with the potential to be applied as wound and burn dressings.

Cyclodextrins-in-Liposomes: A Promising Delivery System for Lippia sidoides and Syzygium aromaticum Essential Oils.

Biological activity of essential oils (EOs) has been extensively reported; however, their low aqueous solubility, high photosensitivity, and volatility compromise a broad industrial use of these compounds. To overcome these limitations, we proposed a nanoencapsulation approach to protect EOs, that aims to increase their stability and modulate their release profile. In this study, drug-in-cyclodextrin-in-liposomes encapsulating two essential oils (Lippia sidoides and Syzygium aromaticum) and their respective major compounds (thymol and eugenol) were produced by ethanol injection and freeze-dried to form proliposomes and further physicochemically characterized. Liposomes showed high physical stability over one month of storage at 4 °C, with slight changes in the mean size, polydispersity index (PDI), and zeta potential. Reconstituted proliposomes showed a mean size between 350 and 3300 nm, PDI from 0.29 to 0.41, and zeta potential between -22 and -26 mV. Differential scanning calorimetry and X-ray diffraction of proliposomes revealed a less-ordered crystalline structure, leading to high retention of the major bioactive compounds (between 73% and 93% for eugenol, and 74% and 84% for thymol). This work highlights the advantages of using drug-in-cyclodextrin-in-liposomes as delivery systems to retain volatile compounds, increasing their physicochemical stability and their promising potential to be utilized as carriers in products in the pharmaceutical, food, and cosmetic industries.

Nanostructured Lipid Carriers Loaded with Lippia sidoides Essential Oil as a Strategy to Combat the Multidrug-Resistant Candida auris.

The emerging pathogen Candida auris is an emerging fungal pathogen that was associated with nosocomial infectious outbreaks. Its worldwide incidence and the emerging multidrug-resistant strains highlight the urgency for novel and effective antifungal treatment strategies. Lippia sidoides essential oil (LSEO) proved antifungal activity, including anti-Candida. However, it may undergo irreversible changes when in contact with external agents without adequate protection. Herein, we encapsulated LSEO in nanostructured lipid carriers (NLC) through the hot emulsification method followed by sonication. NLC matrix was based on oleic acid and Compritol® 888, or a combination of carnauba wax and beeswax, stabilized by sodium dodecyl sulfate. Eight formulations were produced and characterized by the determination of the particle size (213.1 to 445.5 nm), polydispersity index (around 0.3), and ζ-potential (-93.1 to -63.8 mV). The antifungal activity of nanoparticles and LSEO against C. auris and the in vivo toxicity in Galleria mellonella model were also evaluated. Both NLC and LSEO exhibited potent activity against the yeast, with Minimum Inhibitory Concentration between 281 and 563 µg/mL, and did not evidence toxicity in the in vivo model. Therefore, this study confirms the viability of NLCs loaded with LSEO in combating drug-resistant pathogens as a potential new therapeutic strategy for managing of candidemia.

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

Rosemary, an aromatic herb with significant antioxidative activity, is frequently used as food preservative and a source of nutraceuticals. Its antioxidant effect is mainly related to the presence of phenolic compounds, molecules considerably unstable and prone to irreversible physicochemical changes when exposed to external agents. We here proposed the loading of rosemary into structured lipid systems to improve its physicochemical properties. Four formulations were prepared using the same amount of rosemary lyophilized extract. The lipid phase was composed of stearic acid and oleic acid, and the aqueous phase, a varying combination of drying carriers (whey protein concentrate or gum Arabic) and surfactant (Poloxamer 188). The formulations were sonicated, spray-dried, and the obtained powders were characterized regarding the density (0.18 g/mL to 0.26 g/mL), particle size distribution (7 µm and 52 µm), and water solubility (29% to 48%). The antioxidant activity was determined by applying ABTS•+ radical-scavenging assay and the results expressed per gram of lyophilized extract (150.6 µmol Trolox/g to 376.4 µmol Trolox/g), with a significantly lower/higher result seen for formulations containing gum Arabic and a higher concentration of Poloxamer. The prepared systems may have potential applications as preservative in foodstuff and as nutraceutical.

Natural Ergot Alkaloids in Ocular Pharmacotherapy: Known Molecules for Novel Nanoparticle-Based Delivery Systems.

Several pharmacological properties are attributed to ergot alkaloids as a result of their antibacterial, antiproliferative, and antioxidant effects. Although known for their biomedical applications (e.g., for the treatment of glaucoma), most ergot alkaloids exhibit high toxicological risk and may even be lethal to humans and animals. Their pharmacological profile results from the structural similarity between lysergic acid-derived compounds and noradrenalin, dopamine, and serotonin neurotransmitters. To reduce their toxicological risk, while increasing their bioavailability, improved delivery systems were proposed. This review discusses the safety aspects of using ergot alkaloids in ocular pharmacology and proposes the development of lipid and polymeric nanoparticles for the topical administration of these drugs to enhance their therapeutic efficacy for the treatment of glaucoma.

Factors Affecting the Retention Efficiency and Physicochemical Properties of Spray Dried Lipid Nanoparticles Loaded with Lippia sidoides Essential Oil.

Essential oils (EOs) are widely used in various industrial sectors but can present several instability problems when exposed to environmental factors. Encapsulation technologies are effective solutions to improve EOs properties and stability. Currently, the encapsulation in lipid nanoparticles has received significant attention, due to the several recognized advantages over conventional systems. The study aimed to investigate the influence of the lipid matrix composition and spray-drying process on the physicochemical properties of the lipid-based nanoparticles loaded with Lippia sidoides EO and their retention efficiency for the oil. The obtained spray-dried products were characterized by determination of flow properties (Carr Index: from 25.0% to 47.93%, and Hausner ratio: from 1.25 to 1.38), moisture (from 3.78% to 5.20%), water activity (<0.5), and powder morphology. Zeta potential, mean particle size and polydispersity index, of the redispersed dried product, fell between -25.9 mV and -30.9 mV, 525.3 nm and 1143 nm, and 0.425 and 0.652, respectively; showing slight differences with the results obtained prior to spray-drying (from -16.4 mV to -31.6 mV; 147 nm to 1531 nm; and 0.459 to 0.729). Thymol retention in the dried products was significantly lower than the values determined for the liquid formulations and was affected by the drying of nanoparticles.

SLN and NLC for topical, dermal, and transdermal drug delivery.

Introduction: From a biopharmaceutical standpoint, the skin is recognized as an interesting route for drug delivery. In general, small molecules are able to penetrate the stratum corneum, the outermost layer of the skin. In contrast, the delivery of larger molecules, such as peptides and proteins, remains a challenge. Nanoparticles have been exploited not only to enhance skin penetration of drugs but also to expand the range of molecules to be clinically used.Areas covered: This review focus on Solid lipid nanoparticles (SLN) and Nanostructured lipid carriers (NLC) for skin administration. We discuss the selection criteria for lipids, surfactants, and surface modifiers commonly in use in SLN/NLC, their production techniques, and the range of drugs loaded in these lipid nanoparticles for the treatment of skin disorders.Expert opinion: Depending on the lipid and surfactant composition, different nanoparticle morphologies can be generated. Both SLN and NLC are composed of lipids that resemble those of the skin and sebum, which contribute to their enhanced biocompatibility, with limited toxicological risk. SLN and NLC can be loaded with very chemically different drugs, may provide a tunable release profile, can be produced in a sterilized environment, and be scaled-up without the need for organic solvents.

Probiotics and prebiotics potential for the care of skin, female urogenital tract, and respiratory tract.

The prebiotics and probiotics market is constantly growing due to the positive effects of its consumption on human health, which extends beyond the digestive system. In addition, the synbiotic products market is also expanding due to the synergistic effects between pre- and probiotics that provide additional benefits to consumers. Pre- and probiotics are being evaluated for their effectiveness to treat and prevent infectious diseases in other parts of the human body where microbial communities exist. This review examines the scientific data related to the effects of pre- and probiotics on the treatment of diseases occurring in the skin, female urogenital tract, and respiratory tract. The evidence suggests that probiotics consumption can decrease the presence of eczema in children when their mothers have consumed probiotics during pregnancy and lactation. In women, probiotics consumption can effectively prevent recurrent urinary tract infections. The consumption of synbiotic products can reduce respiratory tract infections and their duration and severity. However, the outcomes of the meta-analyses are still limited and not sufficiently conclusive to support the use of probiotics to treat infectious diseases. This is largely a result of the limited number of studies, lack of standardization of the studies, and inconsistencies between the reported results. Therefore, it is advisable that future studies consider these shortcomings and include the evaluation of the combined use of pre- and probiotics.

Effects of lipid formulations on clove extract spray dried powders: comparison of physicochemical properties, storage stability and in vitro intestinal permeation.

Clove is an aromatic plant spice with potent antioxidant and anti-inflammatory activity. Eugenol is the main compound which contributes to such medicinal and nutritional benefits. To date, the formulation of unstable, volatile and poorly water-soluble compounds remains a challenging task. Lipid formulations can be used to improve physicochemical and biopharmaceutical properties of poorly soluble compounds. The aim of this study is to investigate the effects of lipids, such as Gelucire and Compritol on physicochemical properties; stability and in vitro intestinal permeation of spray dried powdered formulations loaded with clove's bioactive compounds. Results showed that eugenol retention in spray-dried powders could be correlated with antioxidant activity and with mass recovery after spray drying. Adding Gelucire but not Compritol to clove extract formulations, improved solubility of spray dried powders. Stability test in high humidity environment (63.5% RH) suggested that formulations including both Gelucire and Compritol were significantly more stable compared to the formulation without any lipid at the two tested temperatures (25 °C and 40 °C). This suggests that lipid additions to clove (Syzygium aromaticum) extract formulations provide protective effects for the spray dried powders in high-humidity environments. In addition, results from in vitro intestinal permeation studies suggested that eugenol uptake, was not being hindered by transporters nor was the absorption being affected by lipid formulations.

Spray drying of lipid-based systems loaded with Camellia sinensis polyphenols.

In this work, spray-dried lipid systems based on soy phosphatidylcholine, cholesterol and lauroyl polyoxylglycerides for entrapping Green tea polyphenols were produced. The aim was to study the effects of the encapsulating composition and spray drying conditions on the system performance and physicochemical product properties. The spray dryer powder production yield falls around 50.7 ± 2.8%, which is typical for lab scale spray dryers. Wrinkled and rounded particles, with low surface porosities were generated, independent of the drying carriers (trehalose or lactose) used. The product showed high encapsulation efficiency of Green tea polyphenols, which was promptly redispersible in water. It presented low density, and good compressive and flow properties. The results herein reported confirm the feasibility of the entrapment of Green tea polyphenols in lipid-based compositions by spray drying in presence of the drying carriers evaluated. The spray-dried microparticles show high potential to be used as additive in food, nutraceutical and pharmaceutical products.

Bioactive compounds in Bidens pilosa L. populations: a key step in the standardization of phytopharmaceutical preparations

The total flavonoid content (TFC), total polyphenols content (TPC), and in vitro antioxidant activity (AA) of six Bidens pilosa L., Asteraceae, populations harvested from different localities were evaluated in this work. The plants were separated in roots, stems, and leaves/flowers, and the influence of extraction methods was investigated.Areversed-phase high-performance liquid chromatography method (HPLC) was developed and employed to obtain characteristic HPLC fingerprints of the bioactive compounds present in the extractive solutions, which were correlated with the TFC, TPC, and AA. Extractive solutions of leaves/flowers presented a higher AA when compared with those obtained from other parts of the plant (IC50 of 35.35±0.10 µg/mL). The stem extracts presented the lowest AA (IC50 117.2±1.96 µg/mL). A direct correlation of AA with TFC and TPC was evidenced. The highest AA was obtained by dynamic maceration and was statistically different from the AA presented by the extractive solutions obtained by other extraction methods. The results of this work evidenced differences that can be found at different stages of development of phytopharmaceutical preparations from B. pilosa and highlighted the importance of using the concentration of marker compounds as well as HPLC fingerprints as quality control parameters.

Use of Carnobacterium maltaromaticum cultures and hydroalcoholic extract of Lippia sidoides Cham. against Listeria monocytogenes in fish model systems.

Minimally processed refrigerated ready-to-eat fishes may offer health risk of severe infection to susceptible individuals due to contamination by the psychrotolerant bacterium L. monocytogenes. In this work, inhibition of L. monocytogenes by a plant extract and lactic acid bacteria (LAB) was studied in model fish systems kept at 5 °C for 35 days. For that, fillets of tropical fish "surubim" (Pseudoplatystoma sp.) and hydroalcoholic extract of the plant Lippia sidoides Cham. ("alecrim pimenta") were used. Fish peptone broth (FPB), "surubim" broth and "surubim" homogenate were inoculated with combinations of L. monocytogenes and bacteriocin-producing Carnobacterium maltaromaticum (C2 and A9b(+)) and non bacteriocin-producing C. maltaromaticum (A9b(-)), in the presence or absence of extract of "alecrim pimenta" (EAP). In all model systems, monocultures of L. monocytogenes and carnobacteria reached final populations ≥10(8) CFU/ml after 35 days, except for L. monocytogenes in "surubim" homogenate (10(4) CFU/ml). In FPB, EAP alone and combined with cultures of LAB inhibited L. monocytogenes but carnobacteria without EAP were only weakly antilisterial. In "surubim" broth, EAP alone did not prevent L. monocytogenes growth but cultures of carnobacteria combined or not with EAP inhibited L. monocytogenes, with more pronounced effect being observed for C. maltaromaticum C2, which produced bacteriocin. In "surubim" homogenate, EAP alone and combined with cultures of C. maltaromaticum A9b(-) and A9b(+) were strongly inhibitory to L. monocytogenes, while C. maltaromaticum C2 with EAP caused transient inhibition of L. monocytogenes. No significant inhibition of L. monocytogenes was observed for carnobacteria in "surubim" homogenate without EAP. In conclusion, it was observed that the use of EAP and cultures of carnobacteria have potential to inhibit L. monocytogenes in fish systems and the applications should be carefully studied, considering the influence of food matrix.

Storage conditions for stability testing of pharmaceuticals in hot and humid regions.

A review of the methodology for determination of the storage conditions for stability testing according to Schumacher/Grimm is presented in this paper. The purpose is to provide scientific information useful for the definition of storage conditions for stability testing of pharmaceuticals suitable to the region where the product will be dispensed. Special attention is given to stability testing in the new markets located in developing countries with very hot and humid climates. Finally, storage conditions for stability testing in the Brazilian regions were derived and examined comparatively with the guidelines of the world health organization (WHO) and regulatory bodies. The storage conditions were derived from the calculated values of the mean kinetic temperature and the relative humidity (RH). These parameters were estimated from daily values of dry and dew point temperatures of all Brazilian capitals from 1998 to 2002; collected in the morning (9 a.m.), in the afternoon (3 p.m.), and at night (9 p.m.). The Brazilian Center of Weather Forecast and Climatic Studies of the National Institute of Spatial Research (CPTEC/INPE) kindly furnished these data. Significant differences of the mean kinetic temperature (MKT) and relative humidity (RH) for Brazilian regions were observed. These results indicate the existence of a high climatic diversity between the Brazilian regions, making challenging the definition of a single storage condition for the stability testing. Some regions present RH values higher than 80%, giving support to the concerns of the WHO, indicating the necessity of revision of existing guidelines for stability testing mainly for very hot and humid regions.

Technical aspects of the production of dried extract of Maytenus ilicifolia leaves by jet spouted bed drying.

This work presents an evaluation of the performance of jet spouted bed with inert particles for production of dried extracts of Maytenus ilicifolia leaves. The development of the extraction procedure was carried-out with the aid of three factors and three levels Box-Behnken design. The effects of the extraction variables, temperature (Text); stirring time (theta); and the ratio of the plant to solvent mass (m(p)/m(s)) on the extraction yield were investigated. The drying performance and product properties were evaluated through the measurement of the product size distribution, loss on drying (Up), flavonoid degradation (D) and, process thermal efficiency (eta). These parameters were measured as a function of the inlet temperature of the spouting gas (Tgi), the feed mass flow rate of the concentrated extract relative to mass flow rate of the spouting gas (Ws/Wg), the ratio between the feed flow rate of spouting gas relative to feed flow rate at a minimum spouting condition (Q/Qms) and the static bed height (H0). A powder product with a low degradation of active substances and good physical properties were obtained for selected operating conditions. These results indicate the feasibility of this drying equipment for the production of dried extracts of M. ilicifolia Martius ex Reiss leaves.