Development of novel pharmaceutical forms of drug compounds and materials for biomedical use

Head of the department: 
Scope of research: 

Transition to personalized medicine, high-tech health care and health protection technologies, including those based on rational administration of drug compounds, is impossible without developing materials for medical use and new generation drugs. The research community and pharmaceutical industry have recently paid a lot of attention to developing bioavailable preparations. A literature analysis shows that about 40% of commercial substances and 80% of compounds being developed now by pharmaceutical companies are poorly soluble in aqueous media. This fact considerably lowers the therapeutic effectiveness of drug compounds and causes side effects. The solubility and permeability parameters can be improved by applying conceptually new approaches based on fine-tuning of physicochemical properties of multicomponent molecular crystals (cocrystals). The economic effect of such pharmaceutical systems is comparable with launching a new drug on the market. Besides, the innovative technologies we are working at can increase the lifetime of generic compounds on the market as the compounds acquire better functional properties and a new brand name. The research department's studies concern the properties of individual active pharmaceutical ingredients (drug compounds / lead compounds) in biological media and crystals. We are also designing pharmaceutical systems for targeted delivery of drug molecules to their sites of action.

Key words: 
Drug compounds
Membrane permeability
Delivery systems

- South-West University "Neofit Rilski" (Blagoevgrad, Bulgaria);

- Indian Institute of Chemical Technology (IICT) (Hyderabad, India);

- Sat-sun Yen University (Guangzhou, China);

- Tianjin University of Technology (China);

- Beijing Institute of Technology (China);

- Shanghai Institute of Materia Medica, Chinese Academy of Sciences (Shanghai, China);

- University of Cape Town, Department of Chemistry, Center of Supramolecular Chemistry (Cape Town, Republic of South Africa);

- Institute of Pharmaceutics, University of Tromsø, (Norway);

- Institute of Chemical Sciences, University of Bologna (Italy);

- Biomedical Research Center (Borstel, Germany);

- Federal Institute for Materials Research and Testing (Berlin, Germany);

- Institute of Pharmaceutics, University of Helsinki (Finland);

- Pharmaceutical and Analytical R&D, AstraZeneca R&D (Molndal, Sweden);

- Institute of Pharmaceutics, University of Glasgow (Scotland);

- Institute of Physics and Chemistry, University of Southern Denmark (Odense, Denmark);

- Institute of Physiologically Active Substances, RAS (Chernogolovka);

- Federal Research Center of Problems of Chemical Physics and Medicinal Chemistry, RAS (Chernogolovka);

- Institute of General and Inorganic Chemistry, RAS (Moscow).


1. Perlovich G.L. Thermodynamic characteristics of cocrystal formation and melting points for rational design of pharmaceutical two-component systems // CrystEngComm. – 2015. – V. 17. – P. 7019 – 7028. DOI: 10.1039/c5ce00992h

2. Perlovich G.L. Prediction of solubility of two-component molecular crystals // CrystEngComm. - 2022. – V. 24. – Art. 2217 DOI: 10.1039/d2ce00105e

3. Surov A.O., Voronin A.P., Drozd K.V., Gruzdev M.S., Perlovich G.L., Prashanth J., Balasubramanian S. Polymorphic forms of antiandrogenic drug nilutamide: structural and thermodynamic aspects // Phys. Chem. Chem. Phys. -  2021. – V. 23(16). – P. 9695-9708. DOI: 10.1039/d1cp00793a.

4. Surov A.O., Churakov A.V., Perlovich G.L. Three Polymorphic Forms of Ciprofloxacin Maleate: Formation Pathways, Crystal Structures, Calculations and Thermodynamic Stability Aspects // Cryst. Growth Des. – 2016. – V. 16(11). – P. 6556-6567. DOI: 10.1021/acs.cgd.6b01277

5. Volkova T.V., Simonova O.R., Perlovich G.L. Another move towards bicalutamide dissolution and permeability improvement with acetylated beta-cyclodextrin solid dispersion // Pharmaceutics. – 2022. - V. 14(7). – Art. 1472. DOI: 10.3390/pharmaceutics14071472

6. Volkova T.V., Simonova O.R., Perlovich G.L. Permeability of diverse drugs through a lipid barrier: impact of pH and cyclodextrin // Journal of Molecular Liquids. – 2022. – V. 357(9). – Art. 115931. DOI: 10.1016/j.molliq.2022.11913

7. Blokhina S.V., Sharapova A.V., Ol’khovich M.V., Volkova T.V., Perlovich G.L., Solubility, lipophilicity and membrane permeability of some fluoroquinolone antimicrobials // Eur. J. Pharm. Sci. – 2016. – V. 105. – P. 29-37. DOI: 10.1016/j.ejps.2016.07.01

8. Blokhina S.V., Ol'khovich M.V., Sharapova A.V., Levshin I.B., Perlovich G.L. Thermodynamic insights to solubility and lipophilicity of new bioactive hybrids triazole with thiazolopyrimidines // J. Mol. Liq. – 2021. – Art. 114662. DOI: 10.1016/j.molliq.2020.114662.

9. Drozd, K.V., Manin A.N., Voronin A.P., Boycov D.E., Churakov A.V., Perlovich G.L. A combined experimental and theoretical study of miconazole salts and cocrystals: crystal structures, DFT computations, formation thermodynamics and solubility improvement // Phys. Chem. Chem. Phys. -  2021. - V. 23(21). – P.12456-12470. DOI: 10.1039/D1CP00956G

10. Drozd K.V., Manin A.N., Churakov A.V., Perlovich G.L. Novel Drug-Drug Cocrystal of Carbamazepine with para-Aminosalicylic Acid: Screening, Crystal Structure and Comparative Study of Carbamazepine Cocrystals Formation Thermodynamics // CrystEngComm. -  2017. - V. 19. – P. 4273-4286. DOI: 10.1039/C7CE00831G