Sanguisorba officinalis L. ethanolic extracts and essential oil - chemical composition, antioxidant potential, antibacterial activity, and ex vivo skin permeation study.

Introduction: Sanguisorba officinalis L. is classified as a medicinal plant and used in traditional medicine. The root of this plant is mainly used as a medicinal raw material, but the above-ground parts are also a valuable source of health-promoting biologically active compounds. Method: The study aimed to evaluate the antioxidant activity and total polyphenol content (TPC) of extracts prepared in 70% and 40% aqueous ethanol solution (dry extract content 50-500 g/L) from the aerial parts of S. officinalis. The essential oil was isolated from the tested raw material, and its composition was determined using GC-MS. Ethanolic extracts and essential oil have been tested for antibacterial activity. The extract in 70% v/v ethanol (dry extract content: 500 g/L) was subjected to HPLC analysis for the content of selected phenolic acids and an ex vivo skin permeation study. The ability of these metabolites to permeate and accumulate in the skin was analysed. Results: Extracts prepared at both ethanol concentrations showed similar antioxidant activity and TPC. Depending on the method, concentration of solvent, and dry extract content (50-500 g/L), the activity ranged from 1.97 to 84.54 g Trolox/L. TPC range of 3.80-37.04 g GA/L. Gallic acid (424 mg/L) and vanillic acid (270 mg/L) had the highest concentrations among the phenolic acids analysed. Vanillic acid (10 µg) permeates the skin at the highest concentration. The highest accumulation in the skin was found for 2,5-dihydroxybenzoic acid (53 µg/g skin), 2,3-dihydroxybenzoic acid (45 µg/g skin), and gallic acid (45 µg/g skin). The tested ethanolic extracts exhibited antibacterial activity. Samples with a dry extract concentration of 500 g/L showed the largest growth inhibition zones. The most sensitive strains to these extracts were P. aeruginosa (24 mm), S. lutea (23 mm), and S. pneumoniae (22 mm). The smallest inhibition zones were observed for B. subtilis (17 mm). The essential oil showed weaker antimicrobial activity (growth inhibition zone 8-10 mm). The GC-MS method identified 22 major components of the essential oil, including aliphatic hydrocarbons, unsaturated terpene alcohols, aliphatic aldehydes, unsaturated and saturated fatty acids, sesquiterpene, phytyl ester of linoleic acid, nitrogen compound, phytosterol, terpene ketone, phenylpropanoids, aliphatic alcohol, diterpenoid, aromatic aldehyde, and aliphatic carboxylic acid. Discussion: The conducted research has shown that ethanolic extracts from Sanguisorbae herba are a valuable source of compounds with antibacterial and antioxidant potential, including phenolic acids. The fact that selected phenolic acids contained in the tested extract have the ability to permeate and accumulate in the skin provides the basis for conducting extended research on the use of extracts from this plant raw material in cosmetic and pharmaceutical preparations applied to the skin.

Antioxidant Activities of Ethanolic Extracts Obtained from α-Pinene-Containing Plants and Their Use in Cosmetic Emulsions.

α-Pinene is the bicyclic, unsaturated terpene hydrocarbon present in many plants. Due to its beneficial chemical properties, this compound is of great interest and has found numerous applications as a raw material in many chemical industries as well as in medicine and cosmetics. The aim of this study was to evaluate the antioxidant activities of ethanolic extracts obtained from plants containing α-pinene and to test the properties of cosmetic emulsions prepared with these extracts. The raw plant materials consisted of fresh parts of Pinus sylvestris L., such as cones, needles, and branches, as well as dried unground and ground pinecones; dried and fresh Rosmarinus officinalis leaves; dried Levisticum officinale leaves; and dried Salvia officinalis L. leaves. The plant materials were individually extracted with 40% (v/v), 70% (v/v), and 96% (v/v) ethanol using ultrasound-assisted extraction (UAE) for 15, 30, or 60 min. This method is a green extraction technique, frequently applied to isolate active substances from plants. For the selected plant materials, Soxhlet extraction with 96% (v/v) ethanol was also performed. The qualitative and quantitative analyses of the components in the selected extracts were performed with gas chromatography coupled with mass spectrometry (GC-MS). The antioxidant activities of the extracts were evaluated with the DPPH and ABTS methods. The extracts of three plant materials with the highest antioxidant activities-dried Rosmarinus officinalis leaves, dried Salvia officinalis L. leaves, and dried and ground Pinus sylvestris L. cones-were selected to be incorporated in cosmetic emulsions containing glyceryl monostearate and Olivem 1000 as emulsifiers. The stabilities and antioxidant activities of the emulsions were evaluated. Moreover, the antimicrobial properties of the emulsions using microbiological tests were also determined. The findings suggest that the prepared emulsions are stable cosmetic products with a high antioxidant potential.

Evaluation of the in vitro permeation parameters of topical ketoprofen and lidocaine hydrochloride from transdermal Pentravan® products through human skin.

In the treatment of pain, especially chronic pain, the rule of multimodal therapy applies, based on various painkillers mechanisms of action. The aim of the conducted study was to evaluate the in vitro penetration of ketoprofen (KET) and lidocaine hydrochloride (LH) through the human skin from a vehicle with transdermal properties. The results obtained with the use of the Franz chamber showed statistically significantly higher penetration of KET from the transdermal vehicle as compared to commercial preparations. It was also shown that the addition of LH to the transdermal vehicle did not change the amount of KET permeated. The study also compared the penetration of KET and LH by adding various excipients to the transdermal vehicle. Comparing the cumulative mass of KET that penetrated after the 24-h study, it was observed that the significantly highest permeation was found for the vehicle containing additionally Tinctura capsici, then for that containing camphor and ethanol, and the vehicle containing menthol and ethanol as compared to that containing Pentravan® alone. A similar tendency was observed in the case of LH, where the addition of Tinctura capsici, menthol and camphor led to a statistically significant higher penetration. Adding certain drugs such as KET and LH to Pentravan®, and substances such as menthol, camphor or capsaicin, can be an interesting alternative to administered enteral drugs especially in the group of patients with multiple diseases and polypragmasy.

Anticancer properties of bacterial cellulose membrane containing ethanolic extract of Epilobium angustifolium L.

Epilobium angustifolium L. is a medicinal plant well known for its anti-inflammatory, antibacterial, antioxidant, and anticancer properties related to its high polyphenols content. In the present study, we evaluated the antiproliferative properties of ethanolic extract of E. angustifolium (EAE) against normal human fibroblasts (HDF) and selected cancer cell lines, including melanoma (A375), breast (MCF7), colon (HT-29), lung (A549) and liver (HepG2). Next, bacterial cellulose (BC) membranes were applied as a matrix for the controlled delivery of the plant extract (BC-EAE) and characterized by thermogravimetry (TG), infrared spectroscopy (FTIR), and scanning electron microscopy (SEM) images. In addition, EAE loading and kinetic release were defined. Finally, the anticancer activity of BC-EAE was evaluated against the HT-29 cell line, which presented the highest sensitivity to the tested plant extract (IC50 = 61.73 ± 6.42 µM). Our study confirmed the biocompatibility of empty BC and the dose and time-dependent cytotoxicity of the released EAE. The plant extract released from BC-2.5%EAE significantly reduced cell viability to 18.16% and 6.15% of the control values and increased number apoptotic/dead cells up to 37.53% and 66.90% after 48 and 72 h of treatment, respectively. In conclusion, our study has shown that BC membranes could be used as a carrier for the delivery of higher doses of anticancer compounds released in a sustained manner in the target tissue.

New amino acid propyl ester ibuprofenates from synthesis to use in drug delivery systems.

This study aimed to evaluate the effect of introducing structural modification of ibuprofen in the form of an ion pair on the permeability of ibuprofen through the skin and the properties of the adhesive layer of the medical patch produced. The active substances tested were the salts of ibuprofen obtained by pairing the anion of ibuprofen with organic cations such as propyl esters of amino acids such as tyrosine, tryptophan, histidine, or phenylalanine. For comparison, the penetration of unmodified ibuprofen and commercially available patches was also tested. Acrylate copolymers based on isobornyl methacrylate as a biocomponent and a monomer increasing the T g ("hard") were used to produce the adhesive layer of transdermal patches. The obtained patches were characterized in terms of adhesive properties and tested for the permeability of the active ingredient and the permeability of the active ingredient through the skin. This study demonstrates the possibility of developing acrylic-based photoreactive transdermal patches that contain biocomponents that can deliver a therapeutically appropriate dose of ibuprofen.

Biologically Active Preparations from the Leaves of Wild Plant Species of the Genus Rubus.

The plants of the genus Rubus (R.) are applied as antiseptic agents in the treatment of skin diseases. Despite the great interest in plants of this genus, there are few reports on the antioxidant and biological activities of preparations obtained from the leaves of these plants. Therefore, we decided to evaluate the antioxidant activity of preparations from leaves of wild plant species of the genus Rubus using the frequently applied DPPH, ABTS, and FRAP methods, as well as to determine the total polyphenol content using the Folin−Ciocalteau method and perform qualitative evaluation by gas chromatography−mass spectrometry (GC-MS). The bactericidal and fungicidal activities of the obtained preparations were evaluated by applying laboratory tests: using the disc and the well methods based on the standards EN 13697:2019, EN 13697:2015, and EN 1500:2013. Microbiological tests of the plant preparations against bacteria, fungi, and yeasts isolated from the environment and against reference strains were performed. Moreover, antimicrobial testing of antibiotics against the tested strains was performed for comparison. The n-octanol/water partition coefficient of the obtained preparations was determined by the shake-flask method to determine their lipophilicity. According to the results, a high content of polyphenols and other antioxidant and biologically active compounds can be thought of as the parameter responsible for the effective activity of plant preparations obtained from wild plant species of the genus Rubus. The methods for determining bactericidal and fungicidal activity clearly demonstrates that preparations with reduced ethanol content exhibit bactericidal and fungicidal activity on surfaces. Testing of hand disinfection by means of rubbing with the preparations confirmed their antimicrobial activity against Escherichia coli K12 NCTC 10538. The obtained results show that the tested preparations exhibit on average two times lower activity against the reference bacterial strains than comparable antibiotics. The preparations obtained from the leaves of R. idaeus L. and R. fruticosus L. could complement classical antibiotics. While environmental bacteria showed a similar response to the preparations and antibiotics, their sensitivity was about one-third less than that of the reference strains. Our studies have shown that the obtained preparations are highly hydrophilic (logP < 0). Thus, these preparations can only be used in lipid bilayers in the aqueous core of liposomes, not in the lipid envelope.

Corrigendum: Assessment of the anti-inflammatory, antibacterial and anti-aging properties and possible use on the skin of hydrogels containing Epilobium angustifolium L. extracts.

[This corrects the article DOI: 10.3389/fphar.2022.896706.].

Assessment of the Anti-Inflammatory, Antibacterial and Anti-Aging Properties and Possible Use on the Skin of Hydrogels Containing Epilobium angustifolium L. Extracts.

Epilobium angustifolium L. is an ethnomedicinal plant known as a medicinal plant in many regions of the world, among others, in various skin diseases. Despite the great interest in this plant, there are still few reports of biological activity of ready-made dermatological or cosmetical preparations containing the E. angustifolium extracts. The antioxidant, anti-ageing, anti-inflammatory, antibacterial properties and toxicity, wound healing, and skin permeation of topical hydrogels containing E. angustifolium extracts (HEas) was assessed. First, the plant extracts were prepared using three solvents: 70% (v/v) ethanol, 70% (v/v) isopropanol and water, next by preparing hydrogels witch by dry extracts (HEa-EtOH), (HEa-iPrOH) and (HEa-WA), respectively. Finally, the content of selected phenolic acids in the HEas was evaluated by high-performance liquid chromatography (HPLC). All the HEas were characterized by high antioxidant activity. The most increased antibacterial activity was observed for a strain of Streptococcus pneumoniae ATCC 49619, Escherichia coli, Enterococcus faecalis ATCC 29212, Enterococcus faecium, Sarcina lutea ATCC 9341 and Bacillus pseudomycoides, while the strains of Streptococcus epidermidis, Bacillus subtilis, and Staphylococcus aureus were the least sensitive. All the HEas showed a reduction in the activity of lipoxygenase enzymes, proteases, and inhibition of protein denaturation. The HEa-EtOH and HEa-iPrOH also enhanced the wound healing activity of HDF cells. Additionally, in vitro penetration studies were performed using the Franz diffusion cells. These studies showed that the active ingredients contained in E. angustifolium penetrate through human skin and accumulate in it. Furthermore, the hydrogels containing E. angustifolium extracts showed a broad spectrum of activity. Therefore, they can be considered as an interesting alternative for dermatologic and cosmetic preparations.

Evaluation of the Structural Modification of Ibuprofen on the Penetration Release of Ibuprofen from a Drug-in-Adhesive Matrix Type Transdermal Patch.

This study aimed to evaluate the effect of chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen [IBU] from the acrylic pressure-sensitive adhesive used as a drug-in-adhesives matrix type transdermal patch. The active substances tested were ibuprofen salts obtained by pairing the ibuprofen anion with organic cations, such as amino acid isopropyl esters. The structural modification of ibuprofen tested were Ibuprofen sodium salt, [GlyOiPr][IBU], [AlaOiPr][IBU], [ValOiPr][IBU], [SerOiPr][IBU], [ThrOiPr][IBU], [(AspOiPr)2][IBU], [LysOiPr][IBU], [LysOiPr][IBU]2, [PheOiPr][IBU], and [ProOiPr][IBU]. For comparison, the penetration of unmodified ibuprofen and commercially available patches was also investigated. Thus, twelve transdermal patches with new drug modifications have been developed whose adhesive carrier is an acrylate copolymer. The obtained patches were characterized for their adhesive properties and tested for permeability of the active substance. Our results show that the obtained ibuprofen patches demonstrate similar permeability to commercial patches compared to those with structural modifications of ibuprofen. However, these modified patches show an increased drug permeability of 2.3 to even 6.4 times greater than unmodified ibuprofen. Increasing the permeability of the active substance and properties such as adhesion, cohesion, and tack make the obtained patches an excellent alternative to commercial patches containing ibuprofen.

Epilobium angustifolium L. as a Potential Herbal Component of Topical Products for Skin Care and Treatment-A Review.

Epilobium angustifolium L. (EA) has been used as a topical agent since ancient times. There has been an increasing interest in applying EA as a raw material used topically in recent years. However, in the literature, there are not many reports on the comprehensive application of this plant to skin care and treatment. EA contains many valuable secondary metabolites, which determine antioxidant, anti-inflammatory, anti-aging, and antiproliferative activity effects. One of the most important active compounds found in EA is oenothein B (OeB), which increases the level of ROS and protects cells from oxidative damage. OeB also influences wound healing and reduces inflammation by strongly inhibiting hyaluronidase enzymes and inhibiting COX-1 and COX-2 cyclooxygenases. Other compounds that play a key role in the context of application to the skin are flavonoids, which inhibit collagenase and hyaluronidase enzymes, showing anti-aging and anti-inflammatory properties. While terpenes in EA play an important role in fighting bacterial skin infections, causing, among other things cell membrane, permeability increase as well as the modification of the lipid profiles and the alteration of the adhesion of the pathogen to the animal cells. The available scientific information on the biological potential of natural compounds can be the basis for the wider use of EA in skin care and treatment. The aim of the article is to review the existing literature on the dermocosmetic use of E. angustifolium.

Influence of the Type of Amino Acid on the Permeability and Properties of Ibuprofenates of Isopropyl Amino Acid Esters.

Modifications of (RS)-2-[4-(2-methylpropyl)phenyl] propanoic acid with amino acid isopropyl esters were synthesised using different methods via a common intermediate. The main reaction was the esterification of the carboxyl group of amino acids with isopropanol and chlorination of the amino group of the amino acid, followed by an exchange or neutralisation reaction and protonation. All of the proposed methods were very efficient, and the compounds obtained have great potential to be more effective drugs with increased skin permeability compared with ibuprofen. In addition, it was shown how the introduction of a modification in the form of an ion pair affects the properties of the obtained compound.

New Ferulic Acid and Amino Acid Derivatives with Increased Cosmeceutical and Pharmaceutical Potential.

Ferulic acid (FA) has been widely used in the pharmaceutical and cosmetics industry due to its, inter alia, antioxidant, antiaging and anti-inflammatory effects This compound added to cosmetic preparations can protect skin because of its photoprotective activity. However, the usefulness of FA as a therapeutic agent is limited due to its low solubility and bioavailability. The paper presents the synthesis, identification, and physicochemical properties of new FA derivatives with propyl esters of three amino acids, glycine (GPr[FA]), L-leucine (LPr[FA]), and L-proline (PPr[FA]). The NMR and FTIR spectroscopy, DSC, and TG analysis were used as analytical methods. Moreover, water solubility of the new conjugates was compared with the parent acid. Both ferulic acid and its conjugates were introduced into hydrogel and emulsion, and the resulting formulations were evaluated for stability. Additionally, in vitro penetration of all studied compounds from both formulations and for comparative purposes using Franz diffusion cells was evaluated from the solution in 70% (v/v) ethanol. Finally, cytotoxicity against murine fibroblasts L929 was tested. All of the analyzed compounds permeated pig skin and accumulated in it. LPr[FA] and PPr[FA] were characterized by much better permeability compared to the parent ferulic acid. Additionally, it was shown that all the analyzed derivatives are characterized by high antioxidant activity and lack of cytotoxicity. Therefore, they can be considered as an interesting alternative to be applied in dermatologic and cosmetic preparations.

Epilobium angustifolium L. Essential Oil-Biological Activity and Enhancement of the Skin Penetration of Drugs-In Vitro Study.

Epilobium angustifolium L. is a popular medicinal plant found in many regions of the world. This plant contains small amounts of essential oil whose composition and properties have not been extensively investigated. There are few reports in the literature on the antioxidant and antifungal properties of this essential oil and the possibility of applying it as a potential promoter of the skin penetration of drugs. The essential oil was obtained by distillation using a Clavenger type apparatus. The chemical composition was analyzed by the GC-MS method. The major active compounds of E. angustifolium L. essential oil (EOEa) were terpenes, including α-caryophyllene oxide, eucalyptol, ß-linalool, camphor, (S)-carvone, and ß-caryophyllene. The analyzed essential oil was also characterized by antioxidant activity amounting to 78% RSA (Radical Scavenging Activity). Antifungal activity against the strains Aspergillus niger, A. ochraceus, A. parasiticum, and Penicillium cyclopium was also determined. The largest inhibition zone was observed for strains from the Aspergillus group. The EOEa enhanced the percutaneous penetration of ibuprofen and lidocaine. After a 24 h test, the content of terpene in the skin and the acceptor fluid was examined. It has been shown that the main compounds contained in the essential oil do not penetrate through the skin, but accumulate in it. Additionally, FTIR-ATR analysis showed a disturbance of the stratum corneum (SC) lipids caused by the essential oil application. Due to its rich composition and high biological activity, EOEa may be a potential candidate to be applied, for example, in the pharmaceutical or cosmetic industries. Moreover, due to the reaction of the essential oil components with SC lipids, the EOEa could be an effective permeation enhancer of topically applied hydrophilic and lipophilic drugs.

Novel Naproxen Salts with Increased Skin Permeability.

The paper presents the synthesis, full identification, and characterization of new salts-L-proline alkyl ester naproxenates [ProOR][NAP], where R was a chain from ethyl to butyl (including isopropyl). All obtained compounds were characterized by Nuclear Magnetic Resonance (NMR), Fourier transform infrared spectroscopy (FTIR), X-ray powder diffractometry (XRD), and in vitro dissolution studies. The specific rotation, phase transition temperatures (melting point), and thermal stability were also determined. In addition, their lipophilicity, permeability, and accumulation in pigskin were determined. Finally, toxicity against mouse L929 fibroblast cells was tested. The obtained naproxen derivatives showed improved solubility and higher absorption of drug molecules by biological membranes. Their lipophilicity was lower and increased with the increase in the alkyl chain of the ester. The derivative with isopropyl ester had the best permeability through pigskin. The use of L-proline isopropyl ester naproxenate increased the permeation of naproxen through the skin almost four-fold. It was also shown that the increase in permeability is not associated with additional risk: all compounds had a similar effect on cell viability as the parent naproxen.

Assessment of the Effect of Structural Modification of Ibuprofen on the Penetration of Ibuprofen from Pentravan® (Semisolid) Formulation Using Human Skin and a Transdermal Diffusion Test Model.

The effect of transdermal vehicle (Pentravan®) on skin permeability was examined for unmodified ibuprofen (IBU) and ion pairs of ibuprofen with new L-valine alkyl esters [ValOR][IBU]. The percutaneous permeation across the human skin and transdermal diffusion test model (Strat-M® membranes) of ibuprofen and its structural modification were measured and compared using Franz diffusion cells. For comparison, the penetration of ibuprofen from a commercial product was also investigated. The cumulative amount of drug permeated through human skin at the end of the 24 h study was highest for ibuprofen derivatives containing propyl (C3), isopropyl (C3), ethyl (C2), and butyl (C4) esters. For Strat-M®, the best results were obtained with the alkyl chain length of the ester from C2 to C5. The permeation profiles and parameters were appointed, such as steady-state flux, lag time, and permeability coefficient. It has been shown that L-valine alkyl ester ibuprofenates, with the propyl, butyl, and amyl chain, exhibit a higher permeation rate than ibuprofen. The diffusion parameters of analyzed drugs through human skin and Strat-M® were similar and with good correlation. The resulting Pentravan-based creams with ibuprofen in the form of an ionic pair represent a potential alternative to other forms of the drug-containing analgesics administered transdermally. Furthermore, the Strat-M® membranes can be used to assess the permeation of transdermal preparations containing anti-inflammatory drugs.

Permeability of Ibuprofen in the Form of Free Acid and Salts of L-Valine Alkyl Esters from a Hydrogel Formulation through Strat-M™ Membrane and Human Skin.

This paper aimed to evaluate the effect of vehicle and chemical modifications of the structure of active compounds on the skin permeation and accumulation of ibuprofen [IBU]. In vitro permeation experiments were performed using human abdominal skin and Strat-M™ membrane. The HPLC method was used for quantitative determinations. The formulations tested were hydrogels containing IBU and its derivatives and commercial gel with ibuprofen. The results obtained indicate that Celugel® had an enhancing effect on the skin penetration of IBU. The average cumulative mass of [IBU] after 24 h permeation test from Celugel® formulation through human skin was over 3 times higher than for the commercial product. Three ibuprofen derivatives containing [ValOiPr][IBU], [ValOPr][IBU], and [ValOBu][IBU] cation were evaluated as chemical penetration enhancers. The cumulative mass after 24 h of penetration was 790.526 ± 41.426, 682.201 ± 29.910, and 684.538 ± 5.599 µg IBU cm-2, respectively, compared to the formulation containing unmodified IBU-429.672 ± 60.151 µg IBU cm-2. This study demonstrates the perspective of the transdermal hydrogel vehicle in conjunction with the modification of the drug as a potential faster drug delivery system.

The Use of Ginkgo Biloba L. as a Neuroprotective Agent in the Alzheimer's Disease.

Alzheimer's disease, a neurodegenerative disease, is one of the most common causes of dementia if elderly people worldwide. Alzheimer's disease leads to the alienation of individuals and their exclusion from social and professional life. It is characterized mainly by the degradation of memory and disorientation, which occurs as a result of the loss of neuronal structure and function in different brain areas. In recent years, more and more attention has been paid to use in the treatment of natural bioactive compounds that will be effective in neurodegenerative diseases, including Alzheimer's disease. G. biloba L. and its most frequently used standardized extract (EGb 761), have been used for many years in supportive therapy and in the prevention of cognitive disorders. The paper presents an overview of reports on the pathogenesis of Alzheimer's disease, as well as a summary of the properties of G. biloba extract and its effects on the possible pathogenesis of the disease. By exploring more about the pathogenesis of the disease and the benefits of G. biloba extract for patients with Alzheimer's disease, it will be possible to create an individualized therapeutic protocol to optimize the treatment.

Sustainable UV-Crosslinkable Acrylic Pressure-Sensitive Adhesives for Medical Application.

This study aimed to investigate the potential of photoreactive acrylate patches as systems for transdermal drug delivery, in particular, using more renewable alternatives and more environmentally friendly synthesis routes of transdermal patches. Therefore, the aim of this study was to develop a transdermal patch containing ibuprofen and investigate its performance in vitro through the pigskin. Transparent patches were prepared using four acrylate copolymers with an incorporated photoinitiator. Two types of transdermal patches based on the photocrosslinking acrylic prepolymers with isobornyl methacrylate as biocomponent and monomer increasing Tg ("hard") were manufactured. The obtained patches were characterized for their adhesive properties and tested for permeability of the active substance. It turns out that patches whose adhesive matrix is photoreactive polyacrylate copolymers have a higher cohesion than patches from commercial adhesives, while the modification of the copolymers with isobornyl methacrylate resulted in an improvement in adhesion and tack. This study demonstrates the feasibility of developing photoreactive acrylic-based transdermal patches that contain biocomponents that can deliver a therapeutically relevant dose of ibuprofen.

Transdermal Delivery Systems for Ibuprofen and Ibuprofen Modified with Amino Acids Alkyl Esters Based on Bacterial Cellulose.

The potential of bacterial cellulose as a carrier for the transport of ibuprofen (a typical example of non-steroidal anti-inflammatory drugs) through the skin was investigated. Ibuprofen and its amino acid ester salts-loaded BC membranes were prepared through a simple methodology and characterized in terms of structure and morphology. Two salts of amino acid isopropyl esters were used in the research, namely L-valine isopropyl ester ibuprofenate ([ValOiPr][IBU]) and L-leucine isopropyl ester ibuprofenate ([LeuOiPr][IBU]). [LeuOiPr][IBU] is a new compound; therefore, it has been fully characterized and its identity confirmed. For all membranes obtained the surface morphology, tensile mechanical properties, active compound dissolution assays, and permeation and skin accumulation studies of API (active pharmaceutical ingredient) were determined. The obtained membranes were very homogeneous. In vitro diffusion studies with Franz cells were conducted using pig epidermal membranes, and showed that the incorporation of ibuprofen in BC membranes provided lower permeation rates to those obtained with amino acids ester salts of ibuprofen. This release profile together with the ease of application and the simple preparation and assembly of the drug-loaded membranes indicates the enormous potentialities of using BC membranes for transdermal application of ibuprofen in the form of amino acid ester salts.

Bacterial Cellulose Membrane Containing Epilobium angustifolium L. Extract as a Promising Material for the Topical Delivery of Antioxidants to the Skin.

Bacterial cellulose membranes (BCs) are becoming useful as a drug delivery system to the skin. However, there are very few reports on their application of plant substances to the skin. Komagataeibacter xylinus was used for the production of bacterial cellulose (BC). The BC containing 5% and 10% ethanolic extract of Epilobium angustifolium (FEE) (BC-5%FEE and BC-10%FEE, respectively) were prepared. Their mechanical, structural, and antioxidant properties, as well as phenolic acid content, were evaluated. The bioavailability of BC-FESs using mouse L929 fibroblasts as model cells was tested. Moreover, In Vitro penetration through the pigskin of the selected phenolic acids contained in FEE and their accumulation in the skin after topical application of BC-FEEs was examined. The BC-FEEs were characterized by antioxidant activity. The BC-5% FEE showed relatively low toxicity to healthy mouse fibroblasts. Gallic acid (GA), chlorogenic acid (ChA), 3,4-dihydroxybenzoic acid (3,4-DHB), 4-hydroxybenzoic acid (4-HB), 3-hydroxybenzoic acid (3-HB), and caffeic acid (CA) found in FEE were also identified in the membranes. After topical application of the membranes to the pigskin penetration of some phenolic acid and other antioxidants through the skin as well as their accumulation in the skin was observed. The bacterial cellulose membrane loaded by plant extract may be an interesting solution for topical antioxidant delivery to the skin.