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One possibility of improving active ingredient penetration into deeper skin layers to enhance the cosmetic product effectiveness, is the application of lipid nanoparticles. The aim of the study presented in this paper was to evaluate the potential of hydrogel formulations enriched with iridoid glycosides-loaded lipid nanoparticles. Lipid nanocarrie...
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... briefly to the cosmetic properties of the studied iridoid glycosides-aucubin and catalpol (Figure 1)-they beneficially affect the regenerative processes of the epidermis by inducing epidermal cell differentiation processes. Thus, they strengthen the protective function of the lipids of the stratum corneum [11,12]. ...
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... amount of released iridoid glycosides was calculated on the basis of the concentrations of aucubin and catalpol in the samples of acceptor fluid, and converted into the percentage value of the degree of release of iridoid glycosides from the hydrogel formulations in relation to their total, theoretical content in the sample of the hydrogel prepared for chromatographic analysis: (i) for aucubin: 22.50 µg/mL (hydrogel 2); 2.50 µg/mL (hydrogel 5); (ii) for catalpol: 22.50 µg/mL (hydrogel 3); 2.25 µg/mL (hydrogel 6). The release profile of iridoid glycosides from hydrogel formulations are presented in Figure 10, as the percentage of released aucubin ( Figure 10A) and catalpol ( Figure 10B) as a function of time. The presented release profiles did not show any differences in the degree of release of aucubin and catalpol from all the tested hydrogel formulations and were determined as classical, indicating a gradual release of the iridoid glycosides from the cosmetic base over time. ...
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... amount of released iridoid glycosides was calculated on the basis of the concentrations of aucubin and catalpol in the samples of acceptor fluid, and converted into the percentage value of the degree of release of iridoid glycosides from the hydrogel formulations in relation to their total, theoretical content in the sample of the hydrogel prepared for chromatographic analysis: (i) for aucubin: 22.50 µg/mL (hydrogel 2); 2.50 µg/mL (hydrogel 5); (ii) for catalpol: 22.50 µg/mL (hydrogel 3); 2.25 µg/mL (hydrogel 6). The release profile of iridoid glycosides from hydrogel formulations are presented in Figure 10, as the percentage of released aucubin ( Figure 10A) and catalpol ( Figure 10B) as a function of time. The presented release profiles did not show any differences in the degree of release of aucubin and catalpol from all the tested hydrogel formulations and were determined as classical, indicating a gradual release of the iridoid glycosides from the cosmetic base over time. ...
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... amount of released iridoid glycosides was calculated on the basis of the concentrations of aucubin and catalpol in the samples of acceptor fluid, and converted into the percentage value of the degree of release of iridoid glycosides from the hydrogel formulations in relation to their total, theoretical content in the sample of the hydrogel prepared for chromatographic analysis: (i) for aucubin: 22.50 µg/mL (hydrogel 2); 2.50 µg/mL (hydrogel 5); (ii) for catalpol: 22.50 µg/mL (hydrogel 3); 2.25 µg/mL (hydrogel 6). The release profile of iridoid glycosides from hydrogel formulations are presented in Figure 10, as the percentage of released aucubin ( Figure 10A) and catalpol ( Figure 10B) as a function of time. The presented release profiles did not show any differences in the degree of release of aucubin and catalpol from all the tested hydrogel formulations and were determined as classical, indicating a gradual release of the iridoid glycosides from the cosmetic base over time. ...
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... changes in epidermis hydration and the associated changes in the TEWL level are illustrated in Figure 11. The hydrophilic base without iridoid glycosides (hydrogel 1), was able to increase the epidermis moisture level by 12%, which was accompanied by an increase in the TEWL parameter by over 25%. ...
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... reason was the very nature of the cosmetic base which, as a highly hydrophilic substrate, does not possess properties predisposing it to the formation of a protective film on the epidermal surface that would inhibit excessive evaporation of water from the skin structures. However, the addition of iridoid glycosides in the form of aqueous phase components, hydrogels 2 (aucubin) and 3 (catalpol) ( Figure 11A) resulted in increasing the epidermis hydration level by 42 and 49%, respectively. In contrast to hydrogel 1, the application of both cosmetic preparations resulted in a decrease in TEWL values, by 47% for the hydrogel with aucubin and by 35% for that with catalpol. ...
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... of iridoid glycosides into lipid nanoparticles resulted in a progressive improvement of the moisturizing effect of the cosmetic products. For hydrogel 5 ( Figure 11B), containing aucubin encapsulated in lipid nanoparticles, the increase in the epidermis moisturization (46%) was at a level comparable to that obtained for hydrogel 4; however, the former hydrogel permitted preservation of stratum corneum barrier functions to a greater degree (decrease in TEWL by 52%). Nevertheless, the most noticeable moisturizing effect was observed for hydrogel 6 (enriched with nanoparticles incorporated with catalpol) manifested by 60% increase in moisturization with simultaneous reduction of TEWL level by 49%. ...
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... decrease in the values of SELS parameters: (i) SEr (roughness) associated with the number of dark pixels present in the image, reflecting wrinkles and furrows in the skin; (ii) SEsm (smoothness) understood as the homogeneity of the obtained image in terms of the lowest possible variation of grey levels in the images; (iii) SEsc (scaliness) expressed as the number of white pixels in the image, identified as the skin with reduced hydration level [21,23,24]; • increase in NRJ (energy) and HOM (homogeneity) values and decrease in CONT (contrast) values, which are specific indicators of the uniformity and overall condition of the skin surface, calculated by analyzing repetitions of combinations of colors of neighboring pixels in the image and the difference between their levels of grey [21,23]. Figure 12 shows the averaged changes in selected skin topography parameters (expressed in%), between the data recorded in week 0 and the end of the study, week 4. As follows from the results, the addition of iridoid glycosides (hydrogels 2 and 3) to the cosmetic base (hydrogel 1) brought the expected direction of changes in the SELS parameters ( Figure 12A). ...
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... 12 shows the averaged changes in selected skin topography parameters (expressed in%), between the data recorded in week 0 and the end of the study, week 4. As follows from the results, the addition of iridoid glycosides (hydrogels 2 and 3) to the cosmetic base (hydrogel 1) brought the expected direction of changes in the SELS parameters ( Figure 12A). The regular application of the hydrogel formulations containing aucubin and catalpol decreased SEr level to a greater extent, by 16 and 14%, respectively, in comparison with the use of the hydrogel without the active substance (statistically insignificant decrease by 3%), attributing stronger anti-aging properties to aucubin. ...
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... enrichment of the hydrogel formulation with the lipid nanocarriers caused a favorable difference manifested as a decrease in SEr value by further 13%, SEsm-4% and SEsc-21%, while the hydrogel base (hydrogel 1) caused an undesirable increase in SEsc parameter. A tendency of changes in SELS parameters observed for hydrogels 5 and 6 ( Figure 12B) was similar to the fluctuations obtained for the corresponding hydrogels, 2 and 3, indicating a more beneficial effect of the cosmetic products containing aucubin and catalpol in the form of lipid nanoparticles. Aucubin was found to be an anti-ageing active ingredient as the application of hydrogel 5 resulted in further 10% decrease in SEr, while catalpol (encapsulated in lipid carrier-hydrogel 6) was identified as the highly moisturizing active component, reducing the levels of SEsm and SEsc by further 13 and 17%, respectively. ...
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... of the skin macrorelief parameters ( Figure 13) indicated a positive effect of the addition of iridoid glycosides to the hydrogel medium (hydrogel 1). Hydrogels 2 and 3, containing aucubin and catalpol, respectively, reduced the value of skin macrorelief parameters by more than 4% on average in the total wrinkle area and by 1 and 2%, in the average length and depth of the wrinkles, relative to the results obtained for hydrogel 1, which did not contain the active substances ( Figure 13A). ...
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... of the skin macrorelief parameters ( Figure 13) indicated a positive effect of the addition of iridoid glycosides to the hydrogel medium (hydrogel 1). Hydrogels 2 and 3, containing aucubin and catalpol, respectively, reduced the value of skin macrorelief parameters by more than 4% on average in the total wrinkle area and by 1 and 2%, in the average length and depth of the wrinkles, relative to the results obtained for hydrogel 1, which did not contain the active substances ( Figure 13A). The incorporation of lipid nanoparticles into a hydrogel support (comparison of results for hydrogel 1 and 4) resulted in an increase in the reduction of the total wrinkle area by over 7%, again confirming the positive effect of lipid nanoparticles on skin condition, i.e., macrorelief parameters, reduction of the visibility of wrinkles and furrows. ...
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... incorporation of lipid nanoparticles into a hydrogel support (comparison of results for hydrogel 1 and 4) resulted in an increase in the reduction of the total wrinkle area by over 7%, again confirming the positive effect of lipid nanoparticles on skin condition, i.e., macrorelief parameters, reduction of the visibility of wrinkles and furrows. No statistically significant changes were determined in the length and depth of the wrinkles on addition of non-loaded lipid nanocarriers to the hydrogel formulation ( Figure 13B). A beneficial effect of the hydrogels containing incorporated iridoid glycosides was noted in terms of skin macrorelief parameters. ...
Citations
... A superior moisturizing effect was observed for the hydrogel preparations containing lipid nanoparticles incorporated with aucubin and catalpol. They caused an increase in the epidermis hydration level and a decrease in the TEWL value, contrary to hydrophilic bases without iridoid glycosides [57]. Moreover, hydrogel alone, as a substrate without lipid components in its composition, was not able to maintain TEWL at such a high level of stratum corneum hydration [58]. ...
Due to the growing popularity of herbal extract-loaded hydrogels, this study assessed the biological activity of extracts and hydrogels containing three types (water (WE), water–ethanol (EE) and water–glycerin (GE)) of Cornus mas L. (dogwood) extracts. The content of biologically active compounds in the extracts was assessed using the UPLC-DAD-MS technique. Antioxidant properties were assessed by using DPPH and ABTS radicals and measuring the intracellular level of reactive oxygen species. Alamar Blue and Neutral Red tests were used to measure the cytotoxicity of the tested samples on skin cells—fibroblasts and keratinocytes. Cell migration and the anti-aging activity of the tested extracts and hydrogels were assessed. Transepidermal water loss and skin hydration after applying the hydrogels to the skin were also determined. A chromatographic analysis revealed that the extracts contained polyphenols, including gallic, caftaric, protocatechuic, chlorogenic, ellagic and p-coumaroylquinic acids, as well as iridoids, with loganic acid as the predominant component. Additionally, they contained cyanidin 3-O-galactoside, pelargonidin 3-O-glucoside and quinic acid. The obtained results show that the tested extracts and hydrogels had strong antioxidant properties and had a positive effect on the viability of skin cells in vitro. Additionally, it was shown that they stimulated the migration of these cells and had the ability to inhibit the activity of collagenase and elastase. Moreover, the tested hydrogels increased skin hydration and prevented transepidermal water loss. The obtained results indicate that the developed hydrogels may be effective delivery systems for phytochemicals contained in dogwood extracts.
... Aucubin is known with CAS: 479-98-1 and chemical formula: (2S,3R,4S,5S,6R)-2-[[(1S,4aR,5S,7aS-5-hydroxy-7-(hydroxymethyl)-1,4a,5,7a-tetrahydrocyclopenta[c]pyran-1-yl]oxy]-6-(hydroxymethyl)oxane-3,4,5-triol [10]. ...
... Catalpol is introduced with CAS: 2415-24-9 and chemical formula: (2S,3R,4S,5S,6R)-2-{[(1aS,1bS,2S,5aR,6S,6aS)-6-Hydroxy-1a-(hydroxymethyl)-1a,1b,2,5a,6,6ahexahydr ooxireno [20,30:4,5]cyclopenta [1,2-c]pyran-2-yl]oxy}-6-(hydroxymethyl)oxane-3,4,5-triol [10]. ...
... MEKC Separating highly hydrophobic analytes, which is difficult with MEKC Quick analysis, satisfactory resolution between iridoids and their good isolation, specificity, resolution, acceptable accuracy, and precision. a worthwhile tool in fingerprint analysis [47,65,132] FT-NIR Not mentioned A rapid and low-cost method [129,130] Abbreviations: TLC: Thin-layer chromatography; LC-UV: liquid chromatography-UV; HPLC: high-performance liquid chromatography; HPTLC: high-performance thin-layer chromatography; CE: capillary electrophoresis; MECC, micellar electrokinetic capillary chromatography; CZE: capillary zone electrophoresis; MEKC: Micellar electrokinetic chromatography; FTNIR: Fourier-transform near-infrared spectroscopy when iridoid glycosides were used as lipid nanoparticles [10]. However, several properties have been reported for the compounds aucubin and catalpol, and understanding the mechanism of action of many of these properties requires more extensive studies. ...
Background: Plantago species contain aucubin and catalpol iridoid glycosides used in traditional medicine for many purposes.
Objectives: To accelerate the utilization of aucubin and catalpol in Plantago species, research should be focused on introducing advanced purification and detection methods. In this regard, the therapeutic activities of aucubin and catalpol compounds are mentioned to confirm their effectiveness in medicinal uses.
Methods: An extensive literature search was conducted using the keywords “Aucubin and Catalpol + Plantago” in the public domains of Google scholar.
Results: The iridoid patterns exhibited a significant correlation with morphological and other chemical specifications of the representatives of the genus Plantago. Commonly, iridoid glycosides are detected with gas chromatography, liquid chromatography, thin-layer chromatography, high-performance liquid chromatography (HPLC), high-performance thin-layer chromatography (HPTLC), and capillary electrophoresis techniques. The most common methods are HPLC and HPTLC. Aucubin and catalpol are active compounds possessing biological activities, including anti-cancer, anti-aging, anti-inflammatory, anti-oxidant, hepatoprotective, osteoprotective, and neuroprotective properties.
Conclusion: This review article comprehensively summarizes cytotoxic activities and detection methods of aucubin and catalpol in Plantago species. The results suggest that Plantago species and their metabolites may benefit human health beyond their traditional uses.
... Formulations A, E, and F remained stable for 60 days, showing no phase separation, while formulations B, C, and D showed phase separation at 30 days of storage. As presented in Figure 2a, formulations B and C were slightly acidic with pH values in the range of 6.3-6.9 throughout the storage period (60 days), whilst formulations A, D, E, and F had pH values above 7. Skin care products must not affect the acid-base balance of the skin's individual layers nor disrupt the stratum corneum barrier function [29]. Given the skin's surface pH (5.5), an acceptable formulation should have a pH value ranging from 4.0 to 7.0 [26,30,31], to avoid skin irritation [32]. ...
... Cosmetic preparation stability over storage time is related to its tendency to exhibit changes in particle migration [29]. In fact, for the FucoPol-based formulations ( Figure 4a-c, Table 2), compared to formulation A (8.7 Pa.s), there was an increase of the viscosity to 19.5 Pa.s in formulation B with the addition of 1.5 wt.% cetyl alcohol ( Figure 4b); in formulation C ( Figure 4c) the addition of both glycerin (3.0 wt.%) and cetyl alcohol (1.5 wt.%) further increased the viscosity to 34.3 Pa.s. ...
... On the other hand, formulations C and E showed lower spreadability than the others. Consistency, a textural parameter directly influenced by viscosity, determines the cosmetic formulation application on the skin (higher consistency means a higher difficulty of application and vice-versa) [29]. In terms of adhesiveness, formulations B (0.467 mJ), C (0.387 mJ), and E (0.499 mJ) seemed to be more adhesive than formulations A (0.244 mJ), D (0.338 mJ), and F (0.317 mJ). ...
Driven by the customers’ growing awareness of environmental issues, the production of topical formulations based on sustainable ingredients is receiving widespread attention from researchers and the industry. Although numerous sustainable ingredients (natural, organic, or green chemistry-derived compounds) have been investigated, there is a lack of comparative studies between conventional ingredients and sustainable alternatives. In this study, olive oil (30 wt.%) and α-tocopherol (2.5 wt.%) containing oil-in-water (O/W) emulsions stabilized with the bacterial fucose-rich polysaccharide FucoPol were formulated envisaging their validation as cosmetic creams. After formula composition design by Response Surface Methodology (RSM), the optimized FucoPol-based emulsion was prepared with 1.5 wt.% FucoPol, 1.5 wt.% cetyl alcohol, and 3.0 wt.% glycerin. The resulting emulsions had an apparent viscosity of 8.72 Pa.s (measured at a shear rate 2.3 s−1) and droplet size and zeta potential values of 6.12 µm and −97.9 mV, respectively, which are within the values reported for cosmetic emulsified formulations. The optimized formulation displayed the desired criterium of a thin emulsion system, possessing the physicochemical properties and the stability comparable to those of commercially available products used in cosmeceutical applications.
... By taking advantage of the hydrogel in controlling drug release, the active ingredients are added to cosmetics to increase their efficacy, which has great prospects in the development of cosmetics. The applications of hydrogels in the field of cosmetics are mainly in terms of anti-oxidation [215], whitening [216], moisturizing [217], embedding and controlled release [218], and facial masks [219]. In particular, an important advantage of bioadhesive hydrogels over conventional hydrogels is that they have a longer residence time on the application site, which can maintain a high local concentration of active ingredients in the surrounding tissue for a longer time, which is very beneficial for active ingredients that are used for surface action, as well as active ingredients that should be active deep in the skin [220]. ...
Hydrogel is a kind of three-dimensional network structure polymer prepared from natural or synthetic materials by physical/chemical cross-linking. It is insoluble in water but can absorb dozens or even thousands of times itself of water. The unique network structure makes it have good inherent strength and adhesion. Through one or more bonding mechanisms (such as mechanical interlocking, diffusion, wet adhesion, etc.), hydrogels can achieve strong adhesion with matrix materials. The adhesion mechanism and application of hydrogels are reviewed in this paper. First, the raw material source, stimulus–response and network structure classification of hydrogels are briefly introduced; then, the research on the design strategy and adhesion mechanism of adhesive hydrogels in recent years is summarized; finally, the applications of adhesive hydrogels in biomedicine, food science, cosmetics, and textiles are introduced, and the improvement of human life quality brought by adhesive hydrogels is expounded.
... Due to the low bioavailability of iridoids, seco-iridoids and their glycosides, various attempts were reported to enhance their bioavailability, distribution, dissolution rate, stability and release. Aucubin and catalpol were loaded on lipid nanoparticles in hydrogel formulation to increase their skin penetration and level of release (Dąbrowska and Nowak, 2021). Also aucubin was micronized by anti-solvent precipitation method using ethanol as solvent and n-hexane as anti-solvent. ...
Background
Iridoids are naturally occurring oxygenated monoterpenes with wide range of pharmacological activities. Scrophulariaceae Juss. is a family of flowering plants with 74 genera and 1533 species well known as rich sources of iridoids.
Purpose
The aim of this review is to describe the phytochemistry and structural diversity of iridoids isolated from various genera of the family. Also, their reported activities and pharmacokinetics are highlighted to provide an overall overview of iridoids in Scrophulariaceae as a fundament for further studies on this important class of compounds.
Methods
A literature survey was performed by searching for relevant information through different scientific databases as SciFinder, ScienceDirect, PubMed, Google Scholar and The World Flora Online.
Results
More than 190 scientific works of literature were consulted from 1980 to 2022. Nearly 250 compounds belonging to iridoid glycosides, seco-iridoids glycosides and non-glycosidic iridoids are reported herein from 102 species. They are isolated from polar alcoholic or aqueous alcoholic extracts of the plant. These compounds exhibit anti-inflammatory, antiprotozoal, neuroprotective, cardioprotective, antioxidant and anticancer activities. Pharmacokinetic studies reported differences in their behaviour due to structural variations. However, most of these iridoids showed low oral bioavailability.
Conclusions
The collected data indicates that more than 70% of iridoids of the family were isolated and identified from Scrophularia, Verbascum and Buddleja genera. Moreover, glycosides of C9 iridoids are the major class representing more than 80% of the total iridoids and third of the identified compounds show activity against inflammation. Further future investigations are recommended regarding the molecular mechanism of action of iridoids, their structure activity relationship, effective doses, toxicity and clinical effects, in order to promote the use of iridoids from Scrophulariaceae as source of new therapeutic medications.
A two-step method based on polyethylene glycol (PEG)-coated nanoscale hydroxyapatite (nHA) was used to form a catalpol (CTP)-loaded delivery system (PEG-nHA/CTP). PEG-nHA/CTP showed a drug-loading ratio of 18.75 ± 0.89% on CTP. In vitro release showed that PEG-nHA/CTP could continuously release CTP for 552 h. The cell proliferation assay showed that PEG-nHA/CTP could promote the proliferation of MC3T3-E1. The alkaline phosphatase assay and alizarin red staining showed that PEG-nHA/CTP could increase the secretion of alkaline phosphatase and formation of mineralized nodules. These results indicate that PEG-nHA/CTP is a highly effective osteopromoting material.Graphical abstract
Oxidative stress damage caused by sun exposure damages the appearance and function of the skin, which is one of the essential inducements of skin aging and even leads to skin cancer. Oroxylin A (OA) is a flavonoid with excellent antioxidant activity and has protective effects against photoaging induced by UV irradiation. However, the strong barrier function of the skin stratum corneum prevents transdermal absorption of the drug, which limits the application of OA in dermal drug delivery. Studies have shown that nanostructured lipid carriers (NLC) can promote not only transdermal absorption of drugs but also increase drug stability and control drug release efficiency, which has broad prospects for clinical applications. In this paper, NLC loaded with OA (OA-NLC) was prepared in order to improve the skin permeability and stability of OA. In vitro studies revealed that OA-NLC had better therapeutic effects than OA solution (OA-Sol) in the cellular model of UVB radiation. OA-Sol and OA-NLC were immobilized in a hydrogel matrix to facilitate application to the dorsal skin of mice. It was found that OA-NLC-gel showed significant antioxidant and anti-apoptotic activity compared to OA-Sol-gel, which was able to protect against skin damage in mice after UV radiation. These results suggest that OA-NLC can improve the deficiencies of OA in skin delivery and show better resistance to UV-induced oxidative damage. The application of OA-NLC to skin delivery systems has good prospects and deserves further development and investigation.
Data Availability
The data used to support the findings of this study are available from the corresponding authors upon request.
