Vol 9, No 1 (2021)


Dendrimers in anticancer targeted drug delivery: accomplishments, challenges and directions for future

Amjad M.W.


Dendrimers are nanoparticles with unique features including globular 3D shape and nanometer size. The availability of numerous terminal functional groups and modifiable surface engineering permit modification of dendrimer surface with several therapeutic agents, diagnostic moieties and targeting substances.

The aim. To enlighten the readers regarding design, development, limitations, challenges and future directions regarding anticancer bio-dendrimers.

Materials and methods. The data base was represented by such systems as Medline, Cochrane Central Register of Controlled Trials, Scopus, Web of Science Core Collection, PubMed. gov, Google-Academy. A search was carried out for the following keywords and combinations: Polypropylene imine (PPI); Poly-L-lysine (PLL); Polyamidoamine (PAMAM); cancer; drug delivery; dendrimers.

Results. High encapsulation of drug and effective passive targeting are also among their therapeutic uses. Herein, we have described latest developments in chemotherapeutic delivery of drugs by dendrimers. For the most part, the potential and efficacy of dendrimers are anticipated to have considerable progressive effect on drug targeting and delivery.

Conclusion. The newest discoveries have shown that the dendritic nanocarriers have many unique features that endorse more research and development.

Pharmacy & Pharmacology. 2021;9(1):4-16
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Biological activity of Hypericum perforatum L. (Hypericaceae): a review

Budantsev A.L., Prikhodko V.A., Varganova I.V., Okovityi S.V.


Hypericum perforatum L. (St. John’s wort) is a medicinal plant that has been intensively studied by clinicians, pharmacologists, and chemists. It has resulted in the publication of both original articles and a number of reviews devoted to the general spectrum of the biological activity of its extracts and the separate chemical components of this species. Unlike many other known medicinal plants, the pharmacological study of which is accompanied by the establishment of new (or rediscovered) structures of chemical compounds, the dynamics of the present study of H. perforatum is mostly associated with a detailed study of the mechanisms of its therapeutic effect and less with the search for new components.

The aim of this work is to review and analyze the data on the biological activity of extracts and individual compounds of Hypericum perforatum L. (Hypericaceae), or St. John’s wort, published in the scientific literature over the past 10 years.

Materials and methods. To collect and analyze the information, such electronic databases as PubMed, Scopus, Web of Science, Google Scholar, and other available resources have been used. The following keywords and word combinations were used for search in the databases for 2010–2020: “Hypericum perforatum”, “St. John’s wort”, “the biological activity of St. John’s wort”, “hypericin”, “hyperforin”.

Results. The review provides information on antidepressant, neuroprotective, nootropic, anxiolytic activity, antibacterial, cytotoxic, anti-inflammatory properties, analgesic, hypoglycaemic effects, and other types of activity of H. perforatum extracts, as well as individual compounds (hypericin, hyperforin, amentoflavone, and others) isolated from this species. It is well known that the secondary metabolites of St. John’s wort are naphthodianthrons, flavonoids and other phenolic compounds, several classes of lipophilic substances including phloroglucinol derivatives and terpenoids. Apart from extracts and their fractions, the biological activity of photoreactive naphthodianthrone hypericin and hyperforin (a phloroglucinol derivative) has been studied in detail.

This review provides an analysis of published data from 2010 to 2020 on the biological activity of St. John’s wort. At the present time H. perforatum is primarily well-known for its antidepressant-like properties, which are confirmed by numerous pharmacological studies and clinical trials. Still there is no consensus on the effective treatment of severe or even moderate depression with St. John’s wort. This review also provides information on the neuroprotective, nootropic, antiepileptic, anxiolytic, antimicrobial, antiviral, antiprotozoal, antitumor, cytotoxic, analgesic, anti-inflammatory and other effects of H. perforatum extracts, as well as its individual compounds.

Conclusion. Despite the popularity of H. perforatum as a plant with an antidepressant-like activity, intensive research work continues to be carried out to elucidate the molecular mechanisms of the actions of extracts and individual compounds in disorders of the nervous system. Studying its antibacterial, antiviral, and cytotoxic activity may also open up some great prospects, along with determining the possibility of using St. John’s wort in metabolic disorders, genitourinary disorders, and other fields of medicine.

Pharmacy & Pharmacology. 2021;9(1):17-31
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Pharmaceutical services: status and development trends

Klimenkova A.A., Geller L.N., Skripko A.A., Gravchenko L.A., Korzhavykh E.A.


The aim of the review is to provide an analysis and generalization of the main directions of research in the sphere of pharmaceutical services, and their characteristics associated with the determination of their main development trends.

Materials and methods. For the analysis, the information store on the basis of scientific publications by Russian and foreign scientists, devoted to research in the field of pharmaceutical services (PSs), has been used. The search for publications was carried out in the open and accessible sources of the latest twenty years (the retrospective period of 2001–2021), located in scientific and technical libraries of institutions, as well as in electronic databases: Elibrary, Medline / PubMed, Cochrane Library, Scopus, CyberLeninka, Google-Academy, J-stage. When forming the information array, the search for publications was carried out according to the following requests: pharmaceutical services (pharmaceutical care services), the provision of pharmaceutical services, the quality of pharmaceutical services. For the conceptualization of the study, 87 scientific publications obtained as a result of information retrieval, have been used.

Results. In the course of the study, a logical and structural analysis of the main directions in which research in the field of providing PSs in our country is developing, has been carried out. The main trends in the study of the providing services’ activity in the sphere of drug circulation, are characterized. A comprehensive analysis of the category of “pharmaceutical service” has been carried out. The terminological content of this concept, the groups of features characterizing the economic and social essence of educational institutions have been generalized, and the most characteristic features that make up the structure and content of educational institutions, have been identified. The existing approaches to the development of the nomenclature and types of PSs have been analyzed and the systematization of pharmaceutical works and services using the process approach, have been proposed by the authors.

Conclusion. The conducted study indicates the presence of several directions in the development of research in the field of providing PSs, aimed at improving the quality of services for the population in pharmaceutical organizations. However, the most important role in the research is assigned to the study and assessment of the quality of educational institutions, the development of approaches to its optimization. As evidenced by the results of the analysis and generalization, the most successful activity in the provision of services in the field of drug circulation requires the implementation of a process approach and the implementation of Quality Management Systems (QMSs).

Pharmacy & Pharmacology. 2021;9(1):32-53
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Approaches to the selection of excipients for dental gel with cetylpyridinium chloride

Zagorulko E.Y., Karavaeva A.S.


The aim of the study was to determine the excipients influence on the characteristics of gels with cetylpyridinium chloride and to select the dental gel formulation gelation agents promising for the development of dental gel compositions. Hereby, the properties of the active pharmaceutical ingredient, characteristics of the specific gelation agents, as well as their influence on stability, biopharmaceutical and application properties of gels, were taken into account.

Materials and methods. In this study, polymers with various gelation mechanisms were considered. Their compatibility with cetylpyridinium chloride as well as storing kinetic and colloid kinds of stability, pH of aqueous solutions, spreadability and textural properties, a penetration ability by the agar diffusion method, an osmotic activity and rheological properties of the gels, were examined. For a complex evaluation of gel compositions study results, a desirability function was used.

Results. Stable homogenous dental gels with cetylpyridinium chloride can be obtained by using 25% poloxamer 407 and 5.0% high molecular weight chitosan as the basis.

The addition of poloxamer 188 to high molecular weight chitosan gels can produce stable systems with improved textural characteristics as well as increase their osmotic activity. Agar and low molecular weight chitosan addition significantly decrease, whereas poloxamer 188 and various molecular weight polyethyleneglycol increase the osmotic activity of 25% poloxamer 407 gels which are also characterized by a high penetration ability.

Conclusion. A complex evaluation of biopharmaceutical, physicochemical and application properties of the gels made it possible to establish that combinations of poloxamer 407 with polyvinylpyrrolidone, agar, and low molecular weight chitosan, can be recommended as a base for a dental gel with cetylpyridinium chloride.

Pharmacy & Pharmacology. 2021;9(1):54-63
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Multisensory colorimetric analysis of drugs dydrogesterone, troxerutin and ademetionine using barcodes

Monogarova O.V., Chaplenko A.A., Oskolok K.V.


The aim of this study is to develop a universal, rapid and affordable method for the identification of dydrogesterone, troxerutin, and ademetionine in drugs by multisensor digital colorimetry using a unique two-dimensional code. The developed approach can be applied to rapid detection of counterfeit drugs at the preliminary stage of the analysis (before using more expensive specialized equipment).

Materials and methods. To implement the proposed approach, the substances of dydrogesterone (“Abbott Biologicals B.V.”, Netherlands), troxerutin (JSC “Interfarma”, Prague, Czech Republic) and ademetionine (LLC “Farmamed”, Moscow, Russia), troxerutin capsules 300 mg (LLC “Pranafarm”, Samara, Russia), lyophilisate for an intravenous solution and the intramuscular administration “Heptral”® (ademetionine) 400 mg (“Abbott Laboratories”, GMBH, Germany), tablets “Duphaston”® (dydrogesterone) 10 mg (“Abbott Healthcare Products B.V.”, Netherlands), were used. A multisensor colorimetry method has been implemented using the following set of 8 sensors (C1–C8): an intact solution – a 96% (v/v) aqueous ethanol solution – C1; 1 mM alcoholic solution of anthraquinone green (CAS#4403-90-1) – C2; a 0.2% aqueous solution of 3-methylbenzothiazolinone hydrazone (CAS#1128-67-2) – C3; a 0.2% methyl orange aqueous solution (CAS#547-58-0) – C4; a 1 mM alcoholic solution of sulforhodamine B (CAS#3520-42-1) – C5; a 1 mM alcoholic solution of 1-hydroxypyrene (CAS#5315-79-7) – C6; 1 mM alcoholic solution of allura red AC (CAS#25956-17-6) – C7; a 1 mM aqueous solution of iron (III) chloride – C8. Transparent flat-bottomed polypropylene plates with 96 cells, with a cell volume of 350 µl (Thermo Fischer Scientific, USA, cat. No. 430341) were used as a base for the chip. For obtaining raster images, an Epson Perfection 1670 office flatbed scanner (CCD-matrix) with a removable cover was used. The obtained digital images of the cells were processed using the ImageJ software (Wayne Rasband, National Institutes of Health, USA; http://imagej.nih.gov/ij) with a 24-bit RGB color model (8 bits per channel).

Results. The adequacy of the developed approach was confirmed by the analysis of the above-listed drugs. It has been shown that the results obtained have no statistically significant differences from the values determined by the spectrophotometric method.

Conclusion. The possibility of using multisensor digital colorimetry for pharmaceutical analysis has been shown. The developed methods for the identification of the active substances can serve as a good supplement to more expensive traditional methods.

Pharmacy & Pharmacology. 2021;9(1):64-72
pages 64-72 views

Study of the safety of antianemic preparations by method of the system of problems related to medicinal preparations

Matveev A.V., Egorova E.A., Koniaeva E.I., Bekirova E.Y., Adzhimamutova L.A.


Iron deficiency is the most common micronutrient deficiency worldwide. Prevention and treatment of iron deficiency conditions are some of the most important health problems in many countries of the world. At the same time, the main problems for it remain the timely diagnosis, elimination of the cause, as well as the choice of replacement therapy with iron-containing drugs and correction of adverse reactions (ADR) that occur during their use.

The aim. This research aims to study the peculiarities of the development of antianaemic drugs ADRs in patients living in the territory of the Republic of Crimea.

Materials and methods. The objects of research were cases of ADR occurrence associated with the use of a group of antianaemic drugs and revealed during the 2009-2018 period in the territory of the Republic of Crimea. The main tasks in the analysis of notification forms were the study of the ADR severity, the causality assessment for suspected drugs and ADRs, as well as analysis of particular problems associated with the use of antianaemic drugs (Drug-related problems, DRP).

Results. Iron supplements in combination with other drugs became the leaders in the incidence of ADR among antianaemic drugs (28 cases, 42.4% of all cases of ADR). The largest number of cases was registered in patients aged from 18 to 30 years, with female patients prevailing. Among the clinical manifestations of ADR, the most cases were drug hypersensitivity reactions of varying severity (40 cases) and disorders of the gastrointestinal tract (18 cases). The study of the problems associated with the use of antianaemic drugs made it possible to determine that the highest rates of DRP values were observed with the use of iron preparations for parenteral use and cyanocobalamine. The minimal DRP values were observed when prescribing iron protein succinylate preparations.

Conclusion. The basis of pharmacotherapy for various types of anemias is the replenishment of iron and vitamin B12 (cyanocobalamin) depots. The effectiveness of the treatment in these cases largely depends on the patient’s adherence to treatment, which is, in turn, depends on the frequency and severity of ADRs that occur during the use of antianaemic drugs.

Pharmacy & Pharmacology. 2021;9(1):73-83
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Molecular design of N-acyl derivatives of 2-(2-oxopyrolidin-1-yl)-acetamide with GABA-ergic and glutamatergic activities

Kodonidi I.P., Chiriapkin A.S., Tworowski D.E.


The first of the most successfully implemented nootropic drugs in medical practice is piracetam, which should be attributed to cyclic derivatives of gamma-aminobutyric acid. The production of new piracetam derivatives with high nootropic activity is a promising direction in the development of new neuroprotective drugs.

The aim of the study is to predict GABA-ergic and glutamatergic activities of N-acyl derivatives of 2-(2-oxopyrolidin-1-yl)-acetamide by a molecular docking method through the energy analysis of interaction of modeled structures with GABAA and AMPA receptors with their subsequent targeted synthesis.

Materials and methods. The objects of the research are new N-acyl derivatives of 2-oxo-1-pyrrolidineacetamide and a virtual model of the GABAA receptor of the Homo sapiens organism with the identification code 6D6U and a three-dimensional model of the AMPA-receptor of the Rattus norvegicus organism with the identification code 3LSF from the RCSB PDB database. The simulated compounds were designed in the HyperChem 8.0.8 program. This program was also used to optimize geometry using the force field of molecular mechanics MM+. Molecular docking was carried out using the Molegro Virtual Docker 6.0.1 program. The preparation of N-acyl derivatives of 2-(2-oxopyrrolidin-1-yl)-acetamide was carried out by the interaction of 2-(2-oxopyrrolidin-1-yl)-acetamide with an excess of the corresponding anhydride under conditions of acid catalysis.

Results. Based on the results of molecular docking, a high affinity of all simulated compounds for the binding site of GABAA and AMPA receptors can be estimated. According to the predict, the maximum GABA-ergic activity should be expected for (N-[2-(2-oxopyrrolidin-1-yl)-acetyl]-butyramide. N-acyl derivatives of 2-oxo-1-pyrrolidineacetamide form a more stable complex with amino acid residues Arg207, Phe200, Thr202, Tyr97, Tyr157, Tyr205 and Phe65 of the GABAA receptor binding site than the GABA molecule. In terms of the minimum interaction energy, the N-acyl derivatives of 2-(2-oxopyrrolidin-1-yl)-acetamide are superior to a number of known ligands such as GABA, piracetam, anipiracetam, picamilon and pramiracetam. The tested compounds have also shown a high affinity for the binding site of the AMPA receptor. The leader compound is also the compound PirBut, as in the case of the GABAА receptor.

Conclusion. Molecular modeling of the ligands interaction with the active binding site of gamma-aminobutyric acid of the GABAA receptor by molecular docking showed that all virtual N-acyl derivatives of 2-oxo-1-pyrrolidineacetamide can exceed a number of nootropic drugs by activity. In the course of molecular design, a method for predicting a glutamatergic activity for 2-pyrrolidone derivatives has been developed. It suggests a significant nootropic activity for N-[2-(2-oxopyrrolidin-1-yl)-acetamide amides.

Pharmacy & Pharmacology. 2021;9(1):84-97
pages 84-97 views

Obituary for Yuri N. Chernov. 5 nov 1937 – 1 jan 2021

Vasin M.V., Esaulenko I.E., Kukes V.G., Petrov V.I., Ushakov I.B., Khokhlov A.L.




Pharmacy & Pharmacology. 2021;9(1):98-100
pages 98-100 views

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