PRODUCTION AND ANALYSIS OF THE NANOSOMAL DRUG FORM OF DEXAMETHASONE IN A HYPEROSMOLAR AQUEOUS MEDIUM

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Issue: 
6
Year: 
2017

O.A. Kulikov Ph.D. (Med.), Associate Professor, National Research Ogaryov Mordovia State University (Saransk) E-mail: oleg-kulikov-84@mail.ru

Objective. A new liposomal form of dexamethasone in a hyperosmolar solution of sodium chloride is obtaining and analysis. Materials. The drug "Dexamethasone"; Lecithin; Cholesterol; Chloroform; Purified deionized water; Sodium hydroxide; Solution "Sterofundin" isotonic; Sodium chloride. Equipment. Rotary evaporator; Extruder; Nanoparticle size analyzer; Spectrophotometer; Chamber for ultrafiltration; Dialysis bag; Magnetic stirrer with heating; Dialysis bag clamp. A method for obtaining liposomal dispersion of dexamethasone in 7.5% NaCl solution. Liposomes were obtained by reversing the phases from lecithin and cholesterol. Dexamethasone was encapsulated by passive loading. Lecithin and cholesterol were dissolved in chloroform. The organic solvent was evaporated in vacuo. The lipid film was hydrated with a hypertonic sodium chloride solution containing dexamethasone. The dispersion of multilamellar vesicles was ground with an extruder. The size of the liposomes was determined with the aid of Nanoparticle size analyzer. The average diameter of the liposomes was 320 ± 50 nm. Purification of liposomes from free dexamethasone was performed by dialysis. UV-spectrophotometry was used for the quantitative determination. Optical density of dialysate was determined at λ = 241 nm. The concentration of dexamethasone in the dialysate was found using a calibration schedule. The concentration of dexamethasone in the purified liposomal dispersion was 2.9795 mg / ml ± 0.015 mg / ml; The effectiveness inclusion to the liposomes of the drug was 74.5% ± 0.4%; The ratio of dexamethasone and lecithin to liposomes af-ter purification: 0.06. The comparison of the kinetics of dexamethasone release from liposomes. In the experiment, the rate of dexame-thasone release from liposomes and its accumulation in a biorelevant environ were compared. As a biorelevant environment the infu-sion soline "Sterofundin ISO" was taken. The experiment was carried out at a constant temperature of 35.5 ° C and a magnetic stirrer speed of 120 / min. The release rate was evaluated by sampling from the biorelevant environ at regular intervals. The concentration of dexamethasone in the samples was determined by spectrophotometry. The concentration-time curves showed that dexamethasone is released much more quickly from liposomes prepared in 7.5% NaCl solution.

Keywords: 
Key words: liposomes
dexamethasone
spectrophotometry.

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