Vol 9, No 5 (2021)


PLGA – the smart polymer for drug delivery

Surya N., Bhattacharyya S.


Polymers have become an integral part of novel drug delivery system. One such successful biodegradable polymer is poly lactic-co-glycolic acid (PLGA) which consists of polyesters of lactic acid and glycolic acid. It is one of the FDA-approved biodegradable polymers which is extensively used for therapeutic purposes in recent times.

The aim. To illuminate researchers on the chemistry, novel properties and applications of PLGA in pharmaceutical fields.

Materials and methods. Various internet sources like Science Direct, Scopus, Web of Science, PubMed and google scholar were used as the data source. The key words search was carried out for the following words and combinations: PLGA, Novel drug delivery, PLGA Nano particles, biomedical applications of PLGA.

Results. Pharmaceutical and biomedical industries are flooded with the use of synthetic and natural polymers. The mechanical and viscoelastic properties of the polymers make them suitable for the temporal and spatial delivery of therapeutic agents for an extended period. Employment of copolymerization techniques lead to the modification of water solubility of the polymers and make them suitable for various applications of drug delivery systems. Biodegradable polymers due to their biocompatibility and biodegradable property have attracted their use in novel drug delivery systems. PLGA is one of them. PLGA is versatile as it can be fabricated into any size, shape, and can be used to encapsulate small molecules, tissue engineering, and bone repair, etc.

Conclusion. The sensitivity and biodegradability of PLGA makes it a smart polymer for targeted and sustained delivery of drugs and in various biomedical applications.

Pharmacy & Pharmacology. 2021;9(5):334-345
pages 334-345 views

Heat shock protein Hsp70: prerequisites for use as a medicinal product

Pokrovsky V.M., Patrakhanov E.A., Antsiferov O.V., Kolesnik I.M., Belashova A.V., Soldatova V.A., Pokopeiko O.N., Karagodina A.Y., Arkhipov I.A., Voronina D.G., Sushkova D.N.


Heat shock protein Hsp70 is one of the main cytoprotection components under the action of various external stimuli. The analysis of the literature data shows that nowadays, the researches’ overwhelming evidence has proven the role of Hsp70 as a biological target for the drug development; however, the ideas about its use as a drug are often multidirectional.

The aim of the article is to analyze and generalize the literature data on the features of the physiological functions of heat shock protein Hsp 70, and indicate the possibilities of its use for the pharmacological correction of various pathological conditions.

Materials and methods. In the process of selecting material for writing this review article, such databases as Google Patents, Science Research Portal, Google Scholar, ScienceDirect, CiteSeer, Publications, ResearchIndex, Ingenta, PubMed, KEGG, etc. were used The following words and word combinations were selected as markers for identifying the literature: Hsp70, Hsp70 stroke, Hsp70 neuroprotection, Hsp70 cytoprotection, recombinant drugs.

Results. In this review, the pharmacology of one of the key members of this family, Hsp70, was focused on. The literary analysis confirms that this molecule is an endogenous regulator of many physiological processes and demonstrates tissue protective effects in modeling ischemic, neurodegenerative and inflammatory processes. The use of recombinant exogenous Hsp70 mimics the endogenous function of the protein, indicating the absence of a number of typical limitations characteristic of pharmacotherapy with high molecular weight compounds, such as immunogenicity, a rapid degradation by proteases, or a low penetration of histohematogenous barriers.

Conclusion. Thus, Hsp70 may become a promising agent for clinical trials as a drug for the treatment of patients with neurological, immunological, and cardiovascular profiles.

Pharmacy & Pharmacology. 2021;9(5):346-355
pages 346-355 views

Methods for quantitative determination of total flavonoids in Quercus robur L. buds

Ryabov N.A., Ryzhov V.M., Kurkin V.A.


Currently, the actual task of modern pharmacy is to study the chemical composition and pharmacological properties of plant objects. Within the framework of this concept, it seems interesting to study Quercus robur L. buds. One of the promising groups of biologically active compounds of Quercus robur L. buds are flavonoids. This group of substances has a wide range of a pharmacological activity, which is significant in the creation of new medicines based on medicinal plant raw materials.

The aim of the article was to work out methods for quantitative determination of total flavonoids in Quercus robur l. buds.

Materials and methods. The research materials were aqueous-alcoholic extracts from Quercus robur L. buds with 70% ethyl alcohol which were analyzed by differential UV spectrophotometry on spectrophotometer “SF 2000” (Russia).

Results. The methods for quantitative determination of total flavonoids in Quercus robur L. buds by differential UV spectrophotometry, has been developed using a standard sample of cynaroside at the analytical wavelength of 400 nm. The optimum parameters for the extraction of total flavonoids from Quercus robur L. buds have been determined. They are: the optimum extractant is 70% ethyl alcohol; the “raw material-extractant” ratio is 1:50; the extraction time is 120 min, the degree of atomization is 2 mm.

The content of total flavonoids for Quercus robur L. buds has been determined; it varies from 0.27%±0.01 to 0.44%±0.02. These results make possible to recommend the content of total flavonoids for this type of raw materials not less than 0.25% as a lower limit.

Conclusion. The data obtained in the course of the experiment, makes it possible to conclude that a further study of Quercus robur L. buds is promising, and it also contributes to the implementation of medicinal plant raw materials “Quercus robur L. buds” in the State Pharmacopoeia (Russia).

Pharmacy & Pharmacology. 2021;9(5):356-366
pages 356-366 views

Synthesis and antioxidant activity of (E)-3-(3-(4-oxo-4H-chromen-3-yl)acryloyl) 2H-chromen-2-one derivatives

Shatokhin S.S., Tuskaev V.A., Gagieva S.C., Pozdnyakov D.I., Oganesyan E.T.


The aim is based on the results of the in silico prediction, to obtain and characterize a number of (E)-3-(3-(4-oxo-4H-chromen-3-yl)acryloyl)-2H-chromen-2-one derivatives, and also to study their antioxidant activity.

Materials and methods. The synthesis of the target compounds was carried out by condensation of substituted 3-formylchromones and 3-acetylcoumarins under the acid catalysis conditions. 1HNMR spectra were recorded on the instruments of Bruker Avance-400 (400 MHz) and Bruker Avance-300 (300 MHz) in the solutions of CDCl3 or DMSO-d6. Mass spectra (ESI) were obtained on a Finnigan LCQ Advantage mass spectrometer (USA). The melting points of the compounds were determined on a PTP (M) instrument. Quantum-chemical calculations were carried out on the basis of a density functional theory using the Gaussian 09 program using the B3LYP/6-311G (d, p) method, as well as using the Way2Drug (PASS Online) online service. The antiradical activity of the compounds was studied by the DPPH test, and the chelating properties were assessed by the o-phenanthroline method.

Results. 15 derivatives of (E)-3-(3-(4-oxo-4H-chromen-3-yl)acryloyl)-2H-chromen-2-one have been obtained and characterized. The calculations based on the density functional theory showed that the highest occupied molecular orbital exhibiting electron-donating properties is localized on the propenone fragment, which confirms the likelihood of the manifestation of antiradical properties. According to the prediction of the probable spectrum of the biological activity, the obtained compounds are more likely to exhibit their direct antioxidant activity. According to the results of the in vitro study of the antioxidant activity, it was found out that compounds 1-15 are the most active in relation to the DPPH radical, which confirms the obtained prognostic data.

Conclusion. Thus, based on the in silico prediction data, 15 derivatives of (E)-3-(3-(4-oxo-4H-chromen-3-yl)acryloyl)-2H-chromen-2-one have been obtained and characterized, for which the method antioxidant activity has been studied in vitro. It was found out that compounds 1-15 exhibit the antiradical activity to a large extent.

Pharmacy & Pharmacology. 2021;9(5):367-376
pages 367-376 views

Type 2 diabetes mellitus’s decompensated form: on the problem of effective pharmacotherapy in real clinical practice

Safronenko A.V., Gantsgorn E.V., Sanina E.A., Khachumova M.A., Panenko S.O., Kuznetsov I.I., Kivva A.A., Polyakova V.I.


The aim of this retrospective study was to analyze the pharmacotherapy regimens of the decompensated form of type 2 diabetes mellitus (DM2) and to evaluate its effectiveness, its compliance with clinical recommendations.

Materials and methods. A retrospective analysis of 54 medical cards of patients with decompensated DM2 was conducted. The 1st group (n=24; 44%) included the patients who had a decrease in glycated hemoglobin (HbA1c) by 50% or more in 3 months after hypoglycemic therapy; and the 2nd group (n=30; 56%) – the patients whose HbA1c level decreased by less than 50%.

Results. A HbA1c level was 10.4% in the 1st group and 13.2% in the 2nd group (р<0.001). However, the target levels of venous blood plasma glucose and HbA1c were not achieved in any of the patient groups. The total number of the drugs prescribed to the patients ranged from 4 (in 25% (n=6) and 10% (n=3) cases in the 1st and the 2nd groups, respectively) to 8 (in 12.5% (n=3) and 20% (n=6) cases in the 1st and the 2nd, groups, respectively). However, in a number of cases some violations of clinical recommendations were recorded: the prescription to the obese patients of insulin drugs, the administration of sulfonylureas derivatives to patients with a history of cardiovascular diseases of the atherosclerotic origin, but modern hypoglycemic drugs with proven benefits in reducing cardiovascular risks were rarely prescribed.

Conclusion. The tactics of pharmacotherapy in the patients with a decompensated form of DM2 does not fully comply with the approved clinical guidelines, which requires the effectiveness of treatment optimization of this medically and socially significant pathology.

Pharmacy & Pharmacology. 2021;9(5):377-386
pages 377-386 views

Cost-minimization analysis of using short and long-acting erythropoesis-stimulating agents for correction of nephrogenic anemia against the background of substitution therapy

Krysanov I.S., Ermakova V.Y., Vaskova L.B., Tiapkina M.V.


Clinical trials conducted in various countries indicate that the use of epoetin alfa in patients with nephrogenic anemia in chronic kidney disease can increase the effectiveness of treatment, reduce the incidence of cardiovascular and infectious complications, and reduce mortality in patients with chronic kidney disease.

The aim of the article was to conduct a comparative clinical and economic assessment of the treatment costs of nephrogenic anemia in adult dialysis patients with recombinant human erythropoietins: epoetin alfa, darbepoetin and long-acting methoxy polyethylene glycol – epoetin beta.

Materials and methods. The study took into account direct medical costs of nephrogenic anemia pharmacotherapy on the basis of 1 year maintenance therapy according to the following scheme: epoetin alfa – 3 times per week, darbepoetin alfa – once per week, methoxy polyethylene glycol – epoetin beta – once per 2 or 4 weeks. A “costs minimization” analysis was performed for equivalent maintenance epoetins doses for intravenous and subcutaneous administrations. Epoetin alpha equivalents were calculated for an average patient weighing 75 kg by converting a weekly dose of short-acting epoetin (7500 IU) into equivalent doses using dose conversion factors.

Results. In the hypothetical cohort of patients under study, epoetin alfa, darbepoetin alfa, and methoxy polyethylene glycol – epoetin beta not differ in effectiveness in achieving target Hb values and in safety. With the equal effectiveness of the investigated drugs, in the studied patients, intravenous epoetin alfa can be less expensive drug therapy relative to the equivalent doses obtained by the calculation: darbepoetin by 14–24% and methoxy polyethylene glycol – epoetin beta by 4–30%. The change-over of patients to the subcutaneous administration makes it possible to decline a weekly dose of epoetin alfa by 20–30% by reducing the frequency of taking the drug to twice a week, and to reduce the cost of drug therapy by a third.

Conclusion. Intravenous and subcutaneous administrations of epoetin alfa 2500 IU may be a more economical drug therapy in comparison with the equivalent doses of darbepoetin and methoxy polyethylene glycol – epoetin beta.

Pharmacy & Pharmacology. 2021;9(5):387-399
pages 387-399 views

Antihistamines: research and analysis of the regional retail market

Prokopenko V.V., Kabakova T.I., Chernikov M.V., Goryachev A.B., Mikhailova S.A., Knysh O.I.


The aim. Focused on optimizing the assortment portfolio of pharmacy organizations and improving the process of drug supply to end-consumers, the aim of the study was to analyze the regional pharmaceutical market for antihistamines.

Materials and methods. In the study, the following methods were used: a content analysis of regulatory documents; a documentary observation method of the volume of antihistamines sales; a sociological survey method. The objects of the study were accounting registers in 32 pharmacy organizations for 2020, as well as the sociological survey results of 174 respondents – consumers of antihistamines.

Results. The classification analysis of 38 international non-proprietary trade names of antihistamines, represented by 187 names of drugs, revealed the prevalence of the first-generation drugs (63%). On the Russian pharmaceutical market, there were also 55% of foreign production drugs. At the regional level, there are 66 types of drugs in circulation, 50% of which are second-generation ones. The cost analysis showed rather a wide rage of the pricing proposal and the economic availability of antihistamines for patients. The sociological survey revealed the fact that 46% of the consumers were ready to pay for the necessary drugs in the price range “over 100 and up to 500 rubles” (over $ 1.38 and up to $ 6.88) for one conventional package. A medical-demographic profile of the antihistamines consumer at the regional level has been made up, and guidelines for pharmaceutical specialists on managing the assortment portfolio of pharmaceutical organizations have been developed.

Conclusion. As a result of the study, the following facts have been established: the seasonal peaks in the antihistamines consumption; a gradual renewal of the pharmacies assortment portfolio due to the increased consumption of the second and third generation antihistamines. The medical and demographic profile of the consumer should be taken into consideration when planning a drug provision for the patients with allergic pathologies, and it is connected with the growth in pharmacies profits due to the sale of drugs in the range from 100 to 500 rubles (from $ 1.38 to $ 6.88). The methodical recommendations have been brought to the attention of the management of regional pharmacy organizations.

Pharmacy & Pharmacology. 2021;9(5):400-409
pages 400-409 views

Actual problems of professional and personal development of qualified persons responsible for quality of medicinal products for human use

Aladysheva Z.I., Pyatigorskaya N.V., Belyaev V.V., Nikolenko N.S., Nesterkina E.I., Loseva S.A.


The aim of the study is to investigate topical problems of the professional and personal development of qualified persons responsible for quality of medicinal products for human use.

Materials and methods. In the period from April 6 to May 10, 2020, an online survey of leading employees in the field of quality assurance of Russian manufacturers was conducted. 176 people took part in the survey; the return of questionnaires was about 17.9%.

Results. From the standpoint of D. Super’s theory of professional development, the largest number of respondents was at the maintenance stage, holding their achieved positions (53.2%). All respondents, regardless of age, were motivated for professional development. Most often qualified persons had chemical engineering (27.3%) and pharmaceutical education (22.2%). Most of them had a working experience in 1–2 divisions of the enterprise, and combined the functions of qualified persons with managerial positions (74.5% and 71.9%, respectively). The majority of the qualified persons (86.4%) indicated the sufficiency of the available knowledge and the lack of knowledge on certain issues. Knowledge and skills in the quality risk management, specific GMP issues and statistical methods (59.0%, 49.2 and 44.2%, respectively); communication and interpersonal skills and, in particular, stress management, emotion management and the art of negotiation (49.4%, 41.3% and 40.9%, respectively), were most popular. About 36% of respondents notified the need for the digital economy competencies, while only 5.1% notified the presence of an electronic batch production record at the enterprise. Finally, only half of the respondents (50.5%) had a formal training plan for qualified persons.

Conclusion. This pilot study revealed the need for the revision of the Exemplary Additional Professional Training Program for Qualified Persons and the professional standard, the urgent need for the regulatory body to develop a scheme and principles for the continuous professional development of qualified persons, and showed the direction of further research in this area.

Pharmacy & Pharmacology. 2021;9(5):410-422
pages 410-422 views

This website uses cookies

You consent to our cookies if you continue to use our website.

About Cookies