Mazurkevičiūtė, Agnė

Background: Transdermal films are promising dosage forms for controlled delivery of active pharmaceutical ingredients through the skin. Polyvinyl alcohol (PVA)-based matrices are particularly attractive due to their biocompatibility, film-forming ability, and versatility. However, the development of films for volatile compounds such as menthol remains challenging due to high potential losses during processing and application. This study compares PVA-based transdermal films fabricated by 3D printing, solvent casting, and electrospinning, focusing on the effect of fabrication method on film properties, release behaviour, and skin delivery performance.

Background: Pelargonium sidoides DC. is a perennial plant that belongs to the Geraniaceae plant family and is primarily found in Southern Africa [1]. It‘s secondary metabolites are mostly proanthocyanidins that are linked to antioxidant, anti-inflammatory, immunomodulatory, antitumor and DNA-protective properties [2]. In this study, qualitative analysis of solid capsules containing lyophilized proanthocyanidins extracted from the dry Pelargonium sidoides DC. root extract was performed. Aim: To perform qualitative analysis of solid capsules containing lyophilized proanthocyanidins extracted from the dry Pelargonium sidoides DC. root extract. Methods: Dry Pelargonium sidoides DC. root extract was obtained from International Flavors & Fragrances Inc. (Switzerland). Proanthocyanidins were isolated and purified using Sephadex LH – 20 column chromatography with methanol (50 %) and acetone (70 %) as eluting solvents sequentially. Proanthocyanidin samples were prepared by acetone evaporation followed by lyophilization. For proanthocyanidin quantification spectrophotometric DMAC method was used with epicatechin solution as a standard. Capsule quality was evaluated by uniformity of mass and disintegration tests, as well as an in vitro release study in methanol (50 %) and hydrochloric acid medium (pH = 1.2). The statistical analysis was performed using “Microsoft Excel 2025” (Microsoft Corporation, USA). Results: The average capsule weight, determined by the uniformity of mass test, was 0.370 (0.004) g. Capsules disintegrated after 16 minutes. In methanol (50 %) medium maximum release was 8.72 mg EE/g (87.06 %) and in pH 1.2 medium maximum release was 6.22 mg EE/g (62.03 %). Conclusions: Fewer than 2 capsules out of 20 showed a mass deviation greater than 7.5 %, indicating consistent capsule filling. All capsules disintegrated in less than 30 minutes, demonstrating acceptable disintegration performance. The in vitro release study showed that release of epicatechin equivalents was dependent on the test medium: in 50 % methanol, proanthocyanidin - like compounds were released from capsules almost completely, whereas in a pH 1.2 medium the maximum release was lower, indicating limited release of epicatechin – equivalent compounds under acidic conditions.

Background: UV protection effectiveness depends on the active substances; phenolic compounds like chlorogenic acid can scavenge UVA-induced free radicals, provide mild UV filtering, and activate the Nrf2 pathway to enhance antioxidant defense (1). Gel formulations with release-modifying polymers are promising for effective UV protection and long-term skin cancer prevention. Aim: To evaluate the biopharmaceutical properties of emulgels containing S. aucuparia extracts and assess the influence of gelling agents on their performance. Methods: Poloxamer 407 (P65, P75, P85) and Hydroxypropyl methylcellulose (HPMC55, HPMC65) emulgels with varying compositions were evaluated. In vitro release was measured using Franz diffusion cells with a cellulose membrane (1.33 cm²) separating 1 ± 0.1 g of donor from 10 mL of receptor phase (purified water). Samples were taken at 1–6 h, replaced with fresh medium, and ultimately analyzed by HPLC. Results: The in vitro release test (Figure 1) showed that among Poloxamer 407-based emulgels, P75 exhibited the highest release of chlorogenic acid and P85 of neochlorogenic acid. The HPMC65 formulation showed the highest release of both compounds among HPMC-based emulgels. When comparing emulgels of identical composition differing only in the gelling agent (P65 and HPMC65), formulations with Poloxamer 407 showed a higher release of phenolic compounds. Conclusion: The type of gelling agent significantly affects the biopharmaceutical performance of emulgels, with Poloxamer 407 promoting higher release of phenolic compounds compared to Hydroxypropyl methylcellulose.

Background: Equisetum arvense L., commonly known as horsetail, is used for several medicinal purposes including wound healing, strengthening of bones, teeth, nails and hair. The topical application of gels to pathological sites offers a significant advantage by providing faster release of drug directly to the site of action [1,2]. The surface of healthy human skin maintains an acidic pH (typically between 4 and 6), which is essential for preserving the integrity of the stratum corneum and maintaining a stable skin microbiome. Therefore, it is important to use topical products that do not disturb the natural skin pH balance [3]. Aim: To determine the pH stability of a methylcellulose gel with Equisetum arvense L. extract. Methods: Gels were prepared using methylcellulose as gelling agents, horsetail extract and distilled water. All the materials were mixed well and the resulting gels were stored in the refrigerator overnight. The pH of gels was measured using a calibrated pH meter. Before each measurement the pH meter was standardized with buffer solutions (pH 7.0) to ensure accuracy. Results were statistically processed by using SPSS version 31.0. Results: The results showed that the pH of the methylcellulose gel containing Equisetum arvense extract remained stable throughout the study period. On the first day, the pH value was 7.17.While at the end of the study (after 4 months), the pH of the gel was 7.75. These results indicate that the E. arvense formulation has good pH stability. Statistical analysis showed that there is no statistically significant difference between the initial pH value of the gel (after one day) and the pH measured after four months of gel storage (p > 0.05). Conclusion: The methylcellulose gel containing Equisetum arvense L. extract demonstrated good pH stability during the study period. The absence of significant pH changes suggests that the formulation is chemically stable and suitable for topical application.

Įžanga. Didėjanti ultravioletinės spinduliuotės ekspozicija yra pagrindinis odos vėžio rizikos veiksnys, o 2020 m. visame pasaulyje buvo diagnozuota daugiau nei 1,5 mln. naujų atvejų [1]. UV apsaugos efektyvumas priklauso nuo aktyviųjų medžiagų savybių, preparato stabilumo ir gebėjimo prasiskverbti į odą. Gelinės formos su skvarbą modifikuojančiais polimerais yra perspektyvios siekiant efektyvios UV apsaugos bei ilgalaikės odos vėžio prevencijos. Tikslas. Atlikti skvarbos į odą tyrimus skirtingos sudėties emulgeliams su S. aucuparia ekstraktais bei parinkti geriausiai prasiskverbiančią į odos sluoksnius formuluotę. Metodai. Ex vivo odos skvarbos tyrimai atlikti naudojant pilvo odos mėginius (etikos leidimo protokolas Nr. BE-2-42, 2023-05-03) ir Bronaugh tipo difuzijos ląsteles (0,64 cm²). Emulgelio dozė užtepta ant epidermio, po 24 val. pašalinta. Epidermio ir dermos sluoksniai atskirti sausos šilumos metodu, ekstrahuoti 96 proc. etanoliu ultragarso vonelėje 30 min. Fenolinių junginių – chlorogeno (CR) ir neochlorogeno rūgšties (NCR) - kiekiai nustatyti ESC. Rezultatai. Epidermis neribojo veikliųjų junginių skvarbos į dermą abiejose emulgelio formuluotėse. Dermoje formuluotė su Hidroksipropilmetilceliulioze (HPMC65) skatino didesnį junginių prasiskverbimą (CR – 0,363 ± 0,072 μg/cm², NCR – 0,056 ± 0,020 μg/cm²) nei emulgelio su Poloksameru 407 (P75) (CR – 0,296 ± 0,003 μg/cm², NCR– 0,039 ± 0,000 μg/cm²), tuo tarpu epidermyje abiejų formuluočių junginių srautai buvo panašūs. Išvados. Skvarbos į odą tyrimai parodė, kad HPMC65 formuluotė lemia didesnį junginių prasiskverbimą į dermą ir galimą stipresnį apsauginį poveikį gilesniuose odos sluoksniuose.

Introduction. Equisetum arvense (L.) is commonly used in traditional medicine as a therapeutic and pain-relieving agent for wound healing, skin diseases and hair loss. It can also be used as an antiseptic, anti-inflammatory, antioxidant and anticancer agent. The topical application of gels at pathological sites offer great advantage in a faster release of drug directly to site of action, independent of water solubility of the drug as compared to creams and ointments [1,2]. Materials and methods. Water extracts of horsetail stems were prepared by comparing raw materials and distilled water with polyethylene glycol in a ratio of 1:100 and by extracting in an ultrasonic bath for 30 minutes. Gels were prepared using methyl cellulose, hydroxypropyl cellulose and pullulan as gelling agents, Equisetum arvense (L.) extract and distilled water. All the materials were mixed well and the resulting gels were stored in a refrigerator overnight. The consistency factor of gels was measured using an MCR102 rotary rheometer with a plate-plate geometry and Peltier system. Results and their discussion. One out of the three prepared gels showed good gelling properties and homogeneity. Gels made with hydroxypropyl cellulose, as well as those with a combination of hydroxypropyl cellulose and pullulan were unstable. The consistency factor values of the prepared gel formulations are shown in Table 1. From the results it is evident that gels made with hydroxypropyl cellulose had a lower consistency factor while the highest consistency factor was determined in the hydrogel produced using methyl cellulose as a gelling agent (220.23 (Pa·s)n ). A statistically significant difference in consistency factor was found between formulations G1 and G2 and G3 (p < 0.01).Conclusion. The study reveals that the consistency factor value depends on the gelling agents used. Gels prepared with methyl cellulose had the highest consistency factor and showed optimal consistency and homogeneity.

Įžanga. Dirvinis asiūklis (Equisetum arvense L.) mokslinėje literatūroje aprašomas kaip augalas, turintis priešuždegiminių savybių, naudingų žaizdų gydymui ar kitoms uždegiminėms ligoms tokioms kaip artritas, podagra, cistitas gydyti. Augalinės vaistinės žaliavos fitocheminė sudėtis priklauso nuo augavietės, žaliavos surinkimo bei paruošimo būdų. Skirtingose geografinėse vietovėse, kuriose auga dirvinių asiūklių žolė, gali skirtis fitocheminė šio augalo sudėtis dėl egzistuojančių dviejų E. arvense chemotipų [1,2]. Tikslas. Nustatyti dirvinio asiūklio (E. arvense L.) vandeninio ekstrakto kokybinę ir kiekybinę sudėtį. Metodai. Dirvinio asiūklio žolė susmulkinama elektriniu malūnėliu. Ekstraktas ruošiamas santykiu 1:20. Kaip ekstrahentas naudojamas polietilenglikolis, kuris ištirpinamas išgrynintame vandenyje. Į 200 ml kolbą atsveriama 20 g susmulkintos augalinės žaliavos, įdedama 30 g polietilenglikolio ir užpilama 100 ml išgryninto vandens. Ekstrakcija vykdoma 60 min ultragarso vonelėje. Pagamintas ekstraktas filtruojamas per filtrinį popierių, siekiant atskirti žaliavos likučius nuo gauto tirpalo. Rezultatai. E. arvense L. vandeniniame žolės ekstrakte identifikuoti šie junginiai: kvercetino-3-O- (6“-O-malonil)-gliukozidas ir izokvercitrinas. Nustatyta, kad suminis fenolinių rūgščių kiekis ekstrakte yra 402,90 µg CRE/ml (CRE – chlorogeno rūgšties ekvivalentas). Paruošto ekstrakto sudėtyje kvercetino-3-O-(6“-O-malonil)-gliukozido buvo nustatyta: 390,42 µg/ml. Mažiausiai ekstrakte apskaičiuota izokvercetino (52,49 µg/ml). Suminis flavonoidų kiekis mėginyje – 442,91 µg/ml. Vandeniniame ekstrakte nustatytas suminis fenolinių junginių kiekis – 845,82 µg/ml. Išvados. Tyrimo metu buvo nustatyta, kad Equisetum arvense L. žolės vandeninio ekstrakto sudėtyje yra kvercetino-3-O-(6“-O-malonil)-gliukozido ir izokvercitrino. Suminis fenolinių junginių kiekis ekstrakte – 845,82 µg/ml.

Introduction. Equisetum arvense (L.), commonly known as horsetail, is used for several medicinal purposes including wound healing, strengthening of bones, teeth, nails and hair. The topical application of gels to pathological sites offers a great advantage by providing faster release of drug directly to site of action [1,2]. The surface of healthy human skin maintains an acidic pH (typically between 4 and 6), which is essential for preserving the integrity of the stratum corneum and maintaining a stable skin microbiome. Therefore, it is important to use topical products that do not disturb the natural skin pH balance [3]. Materials and methods. Gels were prepared using methyl cellulose as gelling agents, E. arvense (L.) extract 11% and distilled water. All the materials were mixed well and the resulting gels were left in the refrigerator overnight. The pH of gels was measured using a calibrated pH meter. Before each measurement the pH-meter was standardized with buffer solutions (pH 7.0) to ensure accuracy. Results were statistically processed by using SPSS version 30.0. Results and discussion. The results showed that the pH of the Equisetum arvense gel remained stable throughout the study period. After the first month, the pH value was 7.17.While at the end of the study (after 2 months), the pH of the gel was measured at 7.18. These results indicate that the E. arvense formulation has good pH stability. Statistical analysis also indicated no significant differences between months (p=1.000, when the level of statistical significance is p <0.05). Conclusions. The Equisetum arvense gel formulation with methyl cellulose maintained a nearly constant pH during the observation period, showing no significant fluctuations between measurements. This stability indicates that the formulation is chemically stable and that there is no visible degradation or interaction of ingredients over time.

Herbal teas used both for food and treatment purposes should be consumed with an understanding of restrictions. The hydroxyanthracenes of senna (Senna alexandrina Mill.) are stimulants of bowel movements and modulators of water and electrolyte absorption in the intestinal tract, resulting in a laxative effect. The EFSA has set a daily acceptable intake of 24.83 mg/person per day for an adult (70 kg) for periods not exceeding two weeks. It is important to note that the use of senna teas in children below 12 years of age, during pregnancy or lactation is not recommended. High intakes of hydroxyanthracenes via food products may be subject to restrictions by some authorities. The WHO standardized daily dose is equivalent to 10–30 mg. The aim of this study was to explore the labelling and content of senna teas on the Lithuanian market. The labelling was found to be non-compliant with the recommendations set by the EFSA due to the absence of warnings regarding exemptions for groups of consumers. Furthermore, only two products included restrictions on the duration of use. The content (assayed according to 04/2020:0206 Eur. Ph.; accreditation LA.184-01.) and the daily exposure (from 19.8 to 106.2 mg of hydroxyanthracene glycosides) was found to be sufficiently potent to induce the physiological effects associated with the pharmacological activity of phytochemicals, which could potentially lead to adverse reactions. To ensure the safety of consumers, it is essential to modify the labelling of senna teas, in conjunction with adapting the existing regulatory framework.

Background: Ciclopirox olamine is a lipophilic antifungal agent used in the treatment of skin and nail fungus. In the development of dermatological formulations, it is important to determine the influence of excipients on the penetration of active compounds into the skin layers. Emulgels are a semi-solid dosage form that has the properties of both hydrogels and emulsions. It is important to study the influence of oil phase components on the penetration of compounds into the skin. Mineral oil, isopropyl myristate and oleic acid were chosen as a lipophilic phase. Objectives: To determine the penetration of ciclopirox olamine into human skin from gels with different lipophilic agent and distribution between the epidermis and dermis. Methods: Four different poloxamer 407 gels with 1% ciclopirox olamine and 30% polyethylene glycol 400 were prepared: without additional substances, with 10% mineral oil, with 10% oleic acid, with 10% isopropyl myristate. Ethics permission for research with human skin was obtained from the Kaunas Regional Bioethical Committee BE-2-42 (May 3, 2023). Ex vivo skin-permeation studies were performed using Bronaugh-type flow-through diffusion cells and Caucasian women’s abdominal skin. The epidermis layer was separated from the dermis by heat treatment. The concentration of ciclopirox olamine was determined using Ultra-performance liquid chromatography validated method. Rheological properties of tested gels were determined using an MCR102 rotary rheometer and temperature ramp test. Results: Rheological measurements showed that the complex viscosity of hydrogel was 2166.6–2599.7 Pa·s. The addition of oleic acid and mineral oil statistically significantly (p < 0.01) reduced complex viscosity values over the entire temperature range studied, while isopropyl myristate statistically significantly increased it.Ex vivo skin penetration studies revealed the flux of ciclopirox olamine from an aqueous 30% polyethylene glycol 400 solution into the epidermis was 73.7 (6.0) μg/cm², and into the dermis was 109.8 (26.1) μg/cm². The penetration into the epidermis from the tested gels was: hydrogel –7.5 (4.6) μg/cm², with mineral oil –7.0 (2.1) μg/cm2, isopropyl myristate –10.9 (5.9) μg/cm², oleic acid –11.9 (4.9) μg/cm².The penetration into the dermis from the tested gels was: hydrogel –31.4 (16.1) μg/cm², with mineral oil –30.2 (6.7) μg/cm², isopropyl myristate –27.0 (11.0) μg/cm², oleic acid –26.4 (10.2) μg/cm². There was not statistically significant (p > 0.05) difference in ciclopirox olamine fluxes into either the epidermis or dermis between the tested gels. Conclusions: The complex viscosity of gels is affected by the type of oil chosen. However, the oil phase has no significant effect on the penetration and distribution of ciclopirox olamine between the epidermis and dermis. The rheological properties and composition of the tested gels do not affect the biopharmaceutical properties.