ScienceRise: Pharmaceutical Science

Towards the chemical standardisation of Epilobium hirsutum leaves

2026-01-15T14:07:09+02:00

Epilobium hirsutum L. is widely used in traditional European medicine to treat urological and inflammatory conditions. Despite its widespread use, no pharmacopoeial monographs on its plant material have been published to date. The aim of this study was to establish physicochemical parameters and identify marker phenolic compounds for the standardisation of plant leaves.

Method. Seven E. hirsutum leaf samples collected in Ukraine, Lithuania, and Poland for analysis. The following parameters were analysed: loss on drying, total ash, and acid-insoluble ash content according to the State Pharmacopoeia of Ukraine. The qualitative composition was analysed using high-performance thin-layer chromatography (HPTLC), and the quantitative analysis of total phenolic compounds, flavonoids, and specific marker compounds was performed using UV spectrophotometry and HPLC-DAD.

Results. As a result, it was established that the content of foreign impurities did not exceed 2% in the analysed samples, the drying loss was 6.4–8.1%, and the total ash was 4.0–5.7%. The HPTLC method was used to determine gallic acid, isoquercitrin, avicularin, guijaverin and hyperoside as key compounds for the plant quality control. Total phenolics ranged between 0.78 and 1.52 mg GAE/g dw, while total flavonoid content was 1.9–5.5 mg HE/g dw. The HPLC method showed that the dominant polyphenolics is oenothein B (39.9–65.7 mg/g), followed by oenothein A, gallic, chlorogenic, and ellagic acids, hyperoside, isoquercitrin, and quercetin. The present components can be proposed for the development of raw material standardisation parameters.

Conclusion. The obtained data confirm that E. hirsutum leaves meet requirements of the State Pharmacopeia of Ukraine and European Pharmacopoeia and can serve as the basis for developing a monograph. Oenothein B, hyperoside, and gallic acid can be proposed as identification markers; in addition, the total phenolic content can be assessed

Application of the method of mathematical planning for the selection of auxiliary components for the creation of a functional-purpose medicinal and cosmetic product

2026-01-26T13:50:04+02:00

The aim of the research: selection of the optimal complex of excipients and development of technology for a therapeutic and cosmetic cream for the acne treatment.

Materials and methods. The following active pharmaceutical ingredients were selected - the dry extract of "Fitoinflam," nicotinamide, salicylic acid, and camphor. Twenty ingredients were used as excipients, acting as a structure-forming agent, emulsifier, emollient, or oil phase. Excipient selection was conducted using a four-factor design based on a 5x5 Greco-Latin square. In vitro studies were conducted using equilibrium dialysis through a semipermeable membrane according to Kruvchinsky. Quantification of total flavonoids, expressed as rutin, was determined by high-performance liquid chromatography.

Results. Using Duncan's ranking test, the most optimal excipients for the cream under development were determined: aerosil (structuring agent), sodium tetraborate (emulsifier), glycerin (emollient), and castor oil (oil medium). The concentration of citric acid as a pH regulator was selected empirically: according to the data obtained, the optimal concentration was 1%.

Conclusions. Based on the results of an experimental design using a 5x5 Greco-Latin square layout, a composition for a medicated, emulsion-type anti-acne cream was developed: dry extract of "Phytoinflam," nicotinamide, salicylic acid, camphor, aerosil, sodium tetraborate, glycerin, castor oil, citric acid, tea tree essential oil, and purified water. A technology for producing cosmetic cream was developed based on the physicochemical properties of the active pharmacological substances and excipients

Research in component composition of essential oils from various organs of Silphium perfoliatum L.

2026-02-20T20:08:22+02:00

Silphium perfoliatum L. (cup plant) is a perennial member of the Asteraceae family indigenous to eastern North America. Its phytochemical profile and biological properties have not yet been comprehensively characterised, and the species is not included in official medical practice. Nevertheless, ethnobotanical records indicate that Indigenous communities of North America traditionally used this plant to alleviate conditions such as neuralgia, respiratory ailments, and rheumatic disorders.

The aim. The aim of this study was to conduct a comprehensive analysis of the qualitative and quantitative composition of essential oils isolated from different organs of S. perfoliatum L. to identify organ-dependent variations and expand current knowledge on the phytochemical profile of this species.

Materials and methods. The plant materials of S. perfoliatum used in this study were collected in Ivano-Frankivsk, Ukraine. Hydrodistillates obtained from dried various organs of S. perfoliatum L. according to the methods of the European Pharmacopoeia were analyzed using gas chromatography coupled with mass spectrometric detection (GC–MS) using an Agilent 6890/5973 GC–MS system operated with ChemStation software for mass- selective detectors (MSD). Agilent HP-5MSI capillary column (30 m × 0.25 mm i.d., film thickness 0.25 µm) were used.

Research results. The yields of essential oils (EOs) in S. perfoliatum L. organs ranged from 2.66 to 5.46 mL/kg. In total, 84 volatile compounds were identified in the raw materials, including monoterpenoids, sesquiterpenes, diterpenes, aldehydes, and other aroma compounds. Sesquiterpenes were the dominant class in all samples (60.44–77.53%). Caryophyllene oxide, germacrene-type alcohols, and caryophyllene prevailed in the aerial parts, whereas root distillates were characterised by silphiperfol derivatives such as silphiperfol-5-ene and presilphiperfol-7-ene. Monoterpenes were most abundant in flowers (23.60%), with α-pinene and camphene as key constituents, while roots contained negligible amounts. Diterpenes, mainly phytol, were detected predominantly in leaves, highlighting organ-specific differences in volatile biosynthesis. A comparative analysis of leaf essential oils collected in 2023 and 2024 demonstrated qualitative stability with quantitative variation. Sesquiterpenes remained dominant in both years (67.19% in 2023; 60.51% in 2024). Caryophyllene oxide and germacrene-type alcohols were major constituents in both samples, though phytol content increased markedly in 2024 (16.54% vs 5.46%). In contrast, 2023 samples showed higher levels of monoterpenes (7.97% vs 5.88%) and aldehydes (7.72% vs 4.36%), indicating seasonal shifts in volatile composition.

Conclusions. This research elucidates the volatile profiles of S. perfoliatum from different organs and harvest years, demonstrating clear organ-related and interannual variability. The content of volatile fractions varied from 2.66 to 5.46 mL/kg, depending on the plant organs. A total of 84 volatile compounds were identified, with sesquiterpenes representing the dominant class in all samples (60.44–77.53%). Aerial parts were enriched in oxygenated sesquiterpenes such as caryophyllene oxide and germacrene-derived alcohols, whereas roots showed a distinct chemotype dominated by silphiperfol-type hydrocarbons. Monoterpenes were most abundant in the flowers (23.60%), with α-pinene, camphene, and oxygenated monoterpenes contributing substantially to the volatile profile, while their content in roots was negligible. Overall, these results broaden current understanding of the phytochemical diversity of S. perfoliatum and support further investigation of its essential oils for potential biological and applied uses

Analysis of the current state of development of micro-needle systems for transdermal drug delivery (a scoping review)

2026-02-23T18:29:19+02:00

The aim is to examine the current state of development of microneedle systems for transdermal drug delivery.

Materials and methods. Analysis, systematization, and generalization of data from scientific literature sources on the development of microneedle systems, research on their effectiveness, and prospects for use in pharmacy. A modified Arskey O'Malley methodology was used, refined by a research group led by H.M. Daudt. A total of 480 publications from the last ten years were analysed.

Results. The results of the analysis show that most of the experimental studies focus on the development of microneedle systems for transdermal delivery of vaccines, insulin, and analgesics. In contrast, studies devoted to the creation of drugs with a different direction of action or drugs for the gradual release of active substances using microneedles occupy a smaller segment of the total number.

Conclusions. It has been established that most scientists choose to develop microneedle-based drugs for systemic use. The main areas of publication are reviews of literature sources, the development of new microneedle systems, etc. The results obtained indicate the potential and relevance of conducting research on the development of microneedle systems

Development of two spectrophotometric methods for the determination of bilastine in tablets

2026-02-23T19:05:25+02:00

The aim of the work was to develop two simple, rapid, economically available spectrophotometric methods for the determination of bilastine in tablets based on the reaction with sulfonephthalein dyes (bromphenol blue (BPB) and thymol blue (TB)).

Materials and methods. Analytical instrumentation: Shimadzu UV-1800 double beam UV-VIS spectrophotometer (Japan) with attached UV-Probe ver. 2.62 software, RAD WAG AS 200/C precise analytical balance (Poland). Bilastine (purity ≥99% (LC)) was purchased from Ukrainian Scientific Pharmacopoeial Center for Quality of Medicines. Nixar tablets 20 mg were purchased from a local pharmacy.

Results and discussion. Two spectrophotometric methods for the determination of bilastine in tablets have been developed. Different sulfophthalein dyes (bromphenol blue, thymol blue, bromocresol green, bromthymol blue, bromocresol purple) have been tested in order to choose the optimal reagent for the method development. The experimental research results led to the selection of BPB and TB as the reagents. Methanol was used as the solvent in reaction of bilastine with BPB, while 20% methanol-ethyl acetate solution was used for TB.

The optimal conditions for the quantitative determination of bilastine in tablets by using BPB were established: concentration – 1.08×10^-3 mol/L, volume of BPB solution – 1.00 mL, wavelength – 596 nm, reaction time – 5 min, solution temperature – 25°C. The optimal conditions for the quantitative determination of bilastine in tablets by using TB were established: concentration – 4.34×10^-4 mol/L, volume of TB solution – 1.00 mL, wavelength – 416 nm, reaction time – 5 min, solution temperature – 25°C.

The spectrophotometric method of the quantitative determination of bilastine in tablets by using BPB was linear in the concentration range of 0.5-7.5 μg/mL, LOD – 0.25 μg/mL, LOQ – 0.76 μg/mL; by using TB was linear in the concentration range of 2.00–18.00 μg/mL, LOD – 0.63 μg/mL, LOQ – 1.92 μg/mL. Both methods demonstrated acceptable robustness, accuracy, and precision, meeting all validation criteria. The «greenness» assessment results confirmed that both methods are excellent from a green analytical chemistry perspective.

Conclusions. The developed methods can be used as an alternative method for the routine analysis of bilastine in tablets

Engineering chitosan-Exenatide nanocomplexes with fatty acids for improved peptide delivery

2025-10-08T17:30:07+03:00

Diabetes Mellitus (DM) is a common endocrine disorder responsible for high morbidity and mortality worldwide. The standard medical treatment for DM is oral hypoglycemic agents and/or insulin. Exenatide, a glucagon-like peptide, has been used to reduce blood sugar and treat DM in the last 20 years. Exenatide administration is limited to parenteral routes. The development of an orally administered Exenatide represents a worthy study that provides significant benefits to patients with diabetes by improving compliance and adherence to the treatment and reduce the burden of frequent injections and enhance treatment outcomes.

The aim of the study is to prepare Exenatide as an oral drug delivery system by combining the advantages of nanoencapsulation with the use of an oily vehicle using fatty acids.

Method: The polyelectrolyte complexation method was used to prepare Exenatide-chitosan complexes (PEC) as an aqueous environment in order to create orally administered Exenatide. The potential of PEC -fatty acids nanoparticles as oral delivery carriers of Exenatide was studied.

Results: The sizes of the formed nanodispersed particles were different when loaded with diluted chitosan or PEC. The vortex mechanical mixing method produced superior results and provided about 20% greater Exenatide gastrointestinal protection than the stirring mechanical method. The results indicated that hydroxypropyl-β-cyclodextrin (HP-β-CD) had a more promising effect on oleic acid formula (F4), providing 87.1% Exenatide gastrointestinal protection but with a larger nanodispersed particle size of 200 nm. However, it did not produce significantly better results for linoleic acid (F8), which provided 81.6% gastrointestinal protection and a nanodispersed particle size of 210 nm. An in vivo study showed that formula F4 has the C_max of Exenatide with T_max of 3 h. Blood glucose was effectively reduced to a level of 91 mg/dl level within 3 h, with a sustained reduction up to 8 h.

Conclusion: Exenatide could be protected from gastrointestinal enzymes by incorporation into chitosan lipid-based formulation. The vortexing mechanical mixing method is preferred method for the preparation. The use of the HP-β-CD improved gastrointestinal protection. The formula F4 is a promising oral alternative to the paraenteral Exenatide

Preformulation studies on the development of a transdermal therapeutic system with captopril

2026-02-25T16:00:58+02:00

The article presents the results of a study of the process of captopril penetration through a semipermeable membrane by in vitro dialysis to practically confirm the possibility of its use for creating new forms of delivery – transdermal therapeutic systems (TTS).

The aim: Preformulation studies of pharmaceutical development of a transdermal dosage form of TTS with antihypertensive action with captopril, determination of the nature and kinetic parameters of the process of captopril permeability through a semipermeable membrane in vitro, as well as the influence of the initial concentration of the selected active pharmaceutical ingredient (API) on this process.

Materials and methods: At the initial stage of development of antihypertensive TTS, the in vitro process of captopril permeability through a semi-permeable membrane by dialysis was investigated at (37±0.5) °C. A phosphate buffer solution (pH 7.4) was used as a diffusion medium. The initial concentration of captopril in the donor solution was 30 mg/ml.

Results: Based on the analysis of the obtained experimental values of the amount of the studied substance in the sample of dialysate Хi and the specific flux gradient per unit of time ΔQ_t it was noted that the process of captopril permeability in model conditions is characterized by a uniform rate and corresponds to zero-order kinetics. The high value of the correlation coefficient R = 0.9996 for the obtained kinetic equation confirms the linear dependence of passage through the membrane of the studied substance on time.

Conclusion: Studies conducted to determine quantitative permeability characteristics have shown, first, the ability of molecules of the selected substances to overcome membrane barriers and allow a positive assessment of the acceptability of this active pharmaceutical ingredient as attractive for the creation of TTS

Synthesis and antibacterial activity of nitrogen-doped carbon dots

2025-12-08T17:49:32+02:00

The aim of our work is to synthesize N-CD and to evaluate its antibacterial activity against Gram-positive and Gram-negative bacteria.

Material and Methods. N-CDs were synthesized from citric acid and urea using a bottom-up approach using microwave-assisted treatment. The nitrogen doping in the CDs structure was studied on an FTIR (Shimadzu IR Prestige-21). The optical properties of N-CDs were detected using fluorescence spectroscopy (Shimadzu RF-6000) and UV-Vis absorption spectroscopy (Shimadzu 1800). The size of N-CDs nanoparticles was confirmed on a TEM (JEOL-JEM 1400). Elemental analysis was performed on an ELEMENTAR vario EL cube. The antibacterial activity of N-CDs was investigated using the agar disk diffusion and dilution method against S.aureus and E.coli bacteria.

Results. The structure and characteristics of N-CDs were confirmed through several stages. The size of N-CDs based on TEM images ranged from 2.4 to 2.6 nm with a fairly uniform size distribution. The success of nitrogen doping was confirmed through fluorescence spectra, UV-vis absoption spectra, FTIR spectra and elemental analysis. The antibacterial activity tests showed that N-CDs were able to inhibit the growth of Gram-positive bacteria (S. aureus, clear zone=9.93±0.2 mm, MIC=50 µg/mL, IC₅₀=272 µg/mL) and Gram-negative bacteria (E. coli, clear zone=8.29±0.3 mm, MIC=50 µg/mL, IC₅₀=339 µg/mL) which makes it a broad-spectrum antibacterial candidate.

Conclusions: N-CD was successfully synthesized and exhibited broad bacterial inhibitory activity. However, its inhibitory performance against Gram-positive bacteria was much better, as seen from the clear zone diameter and IC₅₀ values

Comparative analysis of approaches in renal cell carcinoma pharmacotherapy in different countries and in Ukraine

2026-02-26T18:05:22+02:00

Renal cell carcinoma (RCC) is one of the most common malignant kidney tumors, characterized by a steady increase in incidence and high mortality worldwide, including in Ukraine, which necessitates timely diagnosis and comprehensive multimodal treatment.

The aim of the study was to examine approaches to RCC pharmacotherapy in different countries to further develop measures to improve pharmaceutical care for RCC patients in Ukraine.

Materials and methods. The study was based on scientific publications on RCC pharmacotherapy, international RCC treatment guidelines - National Comprehensive Cancer Network (USA), European Society for Medical Oncology (EU), and American Society of Clinical Oncology (USA) - national RCC treatment protocols, as well as Ukrainian regulatory legal acts governing pharmaceutical care for oncology patients. Content analysis, comparison, information synthesis, and analytical review were used.

Results. International guidelines emphasize personalized therapy, wide use of immunotherapy–targeted therapy combinations, IMDC-based risk stratification, and multidisciplinary patient management. Combinations such as pembrolizumab + axitinib, nivolumab + cabozantinib, and nivolumab + ipilimumab are recommended as first-line therapy for metastatic RCC, while adjuvant pembrolizumab is indicated for patients at high risk of recurrence. The Ukrainian clinical protocol partially aligns with these standards but remains limited in immunotherapy options, risk stratification, adjuvant treatment, and the defined role of clinical pharmacists. Access to innovative medicines is further constrained by high costs and insufficient reimbursement.

Conclusions. Significant differences in approaches to RCC pharmacotherapy between Ukraine and other countries were identified, indicating the need to harmonize national protocols with international guidelines, expand access to innovative therapies, and implement a multidisciplinary approach with pharmacist involvement to improve the effectiveness and accessibility of RCC treatment in Ukraine

Gas chromatographic determination of methylsulfonylmethane in an anti-arthritic combined pharmaceutical product

2026-02-27T14:04:52+02:00

Methylsulfonylmethane is a pharmacologically active compound that is widely used in mono- and combined pharmaceutical preparations to maintain the functional state of the musculoskeletal system. The development of promising anti-arthritic drugs requires proper analytical support, particularly the use of validated methods suitable for routine quality control in accordance with modern pharmaceutical requirements.

The aim. The aim of the study was to develop and validate methods for the quantitative determination of methylsulfonylmethane in a combined medicinal product using gas chromatography with mass-selective detection (GC-MS) and flame ionization detection (GC-FID), and to compare their validation characteristics.

Materials and methods. The object of the study was a combined medicinal product in the form of a powder containing methylsulfonylmethane, glucosamine sulfate, chondroitin sulfate sodium and excipients. The study was conducted using Shimadzu GC/MS GCMS-QP2020 EI and Shimadzu GC-2010 Plus AF gas chromatographs with a flame ionization detector using capillary columns of type 5MS and the external standard method. The validation of the methods was carried out in accordance with the requirements of the State Pharmacopoeia of Ukraine and ICH Q2(R1) recommendations.

Results. Two methods for the identification and quantitative determination of methylsulfonylmethane by gas chromatography were developed. The retention time of MSM by the GC-MS method was 9.157 min in the reference solution and 9.163 min in the test solution, and by the GC-FID method - 8.456 and 8.442 min, respectively. The validation characteristics of the methods were confirmed in the range of 80–120% of the nominal content (0.32–0.48 mg/ml) with correlation coefficients r > 0.9981. The relative standard deviations did not exceed 0.42%, and the total analytical uncertainty met the pharmacopoeial acceptance criteria

Conclusions. The proposed methods are accurate, reproducible and suitable for routine quality control of combination medicinal products containing methylsulfonylmethane