Solubilization of hydrophobic bacteriochlorin-based photosensitizers in micelles of surfactants

Plotnikova, Еkaterina А.; Страмова, В. О.; Morozova, N. B.; Плютинская, А. Д.; Ostroverkhov, Petr; Grin, M. A.; Миронов, А. Ф.; Якубовская, Р. И.; Каприн, А. Д.

doi:10.24931/2413-9432-2019-8-1-18-23

Cited by 2 publications

(2 citation statements)

References 15 publications

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“…Both substances are surfactants capable of forming direct micelles in aqueous solutions for loading hydrophobic compounds that are sparingly soluble in water. We chose a 4% concentration of Kolliphor ELP as the initial concentration that is suitable for the solubilization of hydrophobic dyes but is safe for clinical use, including for intravenous administration [30][31][32]. In the case of other administration routes, for example, for ophthalmic use, this concentration can be increased [33].…”

Section: Selection Of Conditions For Ethercaine Solubilizationmentioning

confidence: 99%

Development of a Dosage form for a Photoswitchable Local Anesthetic Ethercaine

Noev,

Morozova,

Suvorov

et al. 2023

Pharmaceuticals

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The toxicity of local anesthetics is a serious problem, given their widespread use. One of the main causes of the side effects of local anesthetics is their non-selectivity of action in the body. A possible way to increase the selectivity of the action of drugs is to use the photopharmacology approach. Previously, we described the light-controlled local anesthetic ethercaine, the biological effect of which can be controlled using light, thereby increasing its selectivity of action. An important limitation of ethercaine was its low solubility in water, limiting the potential of this compound. In this work, we developed a dosage form of ethercaine, which allowed us to increase its solubility from 0.6% to 2% or more. The resulting 1% solution of ethercaine hydrochloride in 4% Kolliphor ELP had high biological activity on the surface anesthesia model, while demonstrating low acute toxicity in mice with intravenous administration (4–5 times less than that of lidocaine).

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Section: Selection Of Conditions For Ethercaine Solubilizationmentioning

confidence: 99%

Development of a Dosage form for a Photoswitchable Local Anesthetic Ethercaine

Noev,

Morozova,

Suvorov

et al. 2023

Pharmaceuticals

View full text Add to dashboard Cite

show abstract

“…В настоящее время в фармацевтической технологии существует множество методов солюбилизации [10,11]. Они включают применение поверхностно-активных веществ, комплексообразователей [12][13][14][15], введение в состав органических растворителей [16], получение систем доставки [17] и мн. др.…”

Section: Introductionunclassified

Solubilization of 3-hydroxyquinazoline derivative with antitumor activity

Sanarova,

Lantsova,

Nikolaeva

et al. 2023

Rossijskij bioterapevtičeskij žurnal

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Background. Increasing the solubility of new pharmacologically active substances is one of the main tasks of pharmacy. It becomes even more relevant in the field of creating dosage forms for difficult-to-solubilise substances with a new mechanism of action, as in the case of 3-hydroxyquinazoline derivatives, which have shown in vivo experiments the ability to activate tumour cell death by ferroptosis. This includes OVF-009 – an original domestic substance. Due to the solubility of this compound in oils, the technology of its solubilisation using modified castor oil (Kolliphor® ELP, BASF, Germany), approved for parenteral use, was proposed.Aim. To create a model dosage form for a new hydrophobic quinazoline derivative in order to further evaluate the spectrum of its antitumour activity in in vivo experiments.Materials and methods. OVF-009, Kolliphor® ELP, 95 % ethanol, Kollidon 17 PF (BASF, Germany), sodium hydroxide, phosphate buffer, water for injection; spontaneous micelle formation, ultrasound, potentiometry, dynamic light scattering, electrophoretic method, viscometry method, etc.Results. The main properties of micelle-forming solubiliser Kolliphor® ELP and its aqueous solutions were considered; 10 model solutions OVF-009 based only on Kolliphor® ELP and with addition of ethanol and Kollidon 17PF in different concentrations were obtained; the quality of the obtained compositions was evaluated by parameters – appearance, solution transparency, pH, stability over time and tolerability by laboratory animals. As a result, two formulations prepared on phosphate buffer were chosen: formulation No 5, which contains 10 % Kolliphor® ELP and additionally 10 % polyvinylpyrrolidone, and formulation No 8, in which in addition to the main solubiliser 10 % ethanol and 16 % polyvinylpyrrolidone were added. Both formulations have neutral pH, can be stored for 24 h and are tolerated by laboratory animals.Conclusion. The selected model compositions for solubilisation of the substance OVF-009 on the basis of Kolliphor® ELP allowed to provide the concentration of the active substance in the solution suitable for further biological experiments on animals.

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Solubilization of hydrophobic bacteriochlorin-based photosensitizers in micelles of surfactants

Cited by 2 publications

References 15 publications

Development of a Dosage form for a Photoswitchable Local Anesthetic Ethercaine

Development of a Dosage form for a Photoswitchable Local Anesthetic Ethercaine

Solubilization of 3-hydroxyquinazoline derivative with antitumor activity

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