Russian Journal of BiotherapyRussian Journal of BiotherapyРоссийский биотерапевтический журнал1726-97841726-9792Publishing House ABV Press161510.17650/1726-9784-2026-25-1-28-40REVIEWОБЗОР ЛИТЕРАТУРЫReview ArticleLipophilicity of drugs: general characteristics and methods of determinationЛипофильность лекарственных средств: общая характеристика и методы определенияhttps://orcid.org/0000-0003-3034-750XShprakhZoya S.ШпрахЗ. С.
Russian Federation
z.shprakh@ronc.ruhttps://orcid.org/0000-0001-6740-5692DmitrievaMaria V.ДмитриеваМ. В.
Russian Federation
z.shprakh@ronc.ruN. N. Blokhin National Medical Research Center of Oncology, Ministry of Health of RussiaФГБУ «Национальный медицинский исследовательский центр онкологии им. Н. Н. Блохина» Минздрава России3004202625128402704202627042026Copyright ©; 2026, ABV-PressCopyright ©; 2026, АБВ-пресс2026ABV-PressАБВ-прессhttps://bioterapevt.abvpress.ru/jour/about/editorialPolicieshttps://bioterapevt.abvpress.ru/jour/article/view/1615

Background. Lipophilicity is one of the most significant and widely used physico-chemical characteristics of a drug, which determines its path in the body.

Aim. To systematize and generalize the literature data on the main parameters of lipophilicity and methods of its determination.

Materials and methods. The search for materials on the subject under study was carried out using the following search and information and library databases: PubMed, CyberLeninka, eLibrary, ResearchGate. The search for publications was carried out by keywords / phrases: “lipophilicity”, “lipophilicity of drugs”, “octanol / water distribution coefficient”, “assessment of lipophilicity”, etc.

Results. Lipophilicity shows the affinity of a compound to a lipophilic medium, and is traditionally expressed as the logarithm of the distribution coefficient of a molecule between two immiscible liquids − an organic solvent and water. There are various approaches to assessing lipophilicity. The standard method is “shaking in a flask”, which is based on the extraction of the test substance in the octanol-water system. Alternatively, reverse-phase thin-layer chromatography or high-performance liquid chromatography is used to assess lipophilicity. Chromatographic methods make it possible to determine the lipophilicity of a wide range of newly synthesized compounds and are characterized by low cost of experiments, simplicity and high accuracy. For ionized compounds, it is possible to use potentiometric approaches that are based on potentiometric titration or potential measurement through the use of ion-selective electrodes. Computational methods that provide quick information on lipophilicity are usually used for screening chemical libraries and have significant advantages over experimental methods. Many programs have been developed to calculate the logarithm of the distribution coefficient, which are freely available both in the form of software and on online platforms.

Conclusion. This review provides basic information about lipophilicity, describes key parameters and criteria for its assessment, and presents modern approaches to determining this characteristic.

Введение. Липофильность – oдна из наиболее значимых физико-химических характеристик лекарственного средства, определяющих его путь в организме.

Цель исследования – систематизировать и обобщить данные литературы об основных параметрах липофильности и методах ее определения.

Материалы и методы. Поиск материалов по исследуемой тематике проводили с использованием поисково-информационных и библиотечных баз данных: PubMed, CyberLeninka, eLibrary, ResearchGate. Поиск осуществляли по ключевым словам / словосочетаниям: «липофильность» (lipophilicity), «липофильность лекарственных препаратов» (lipophilicity of drugs), «коэффициент распределения октанол / вода» (octanol / water distribution coefficient), «оценка липофильности» (assessment of lipophilicity) и др.

Результаты. Липофильность показывает сродство соединения к липофильной среде и выражается традиционно в виде логарифма коэффициента распределения вещества между двумя несмешивающимися жидкостями – органическим растворителем и водой (logP). Стандартным является метод «встряхивание в колбе», который основан на экстракции исследуемого вещества в системе «октанол–вода». В качестве альтернативных для оценки липофильности используют хроматографические методы – обращенно-фазовую тонкослойную или высокоэффективную жидкостную хроматографию, которые позволяют определять липофильность вновь синтезированных соединений и характеризуются низкой стоимостью, простотой и высокой точностью. Для ионизированных соединений возможно применение потенциометрического титрования или измерение потенциала с использованием ионселективных электродов. Вычислительные методы, которые предоставляют быструю информацию о липофильности и обычно используют для скрининга химических библиотек, имеют значительные преимущества по сравнению с экспериментальными.

Заключение. В обзоре представлены базовые сведения о липофильности, описаны важнейшие параметры и критерии ее оценки, а также приведены современные подходы к определению данной характеристики.

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