RESEARH OF THE LIPID MEMBRANE COMPOSITION DURING LIPOSOMAL IRINOTECAN CREATION

• Main Authors: O. V. Stadnichenko, Y. M. Krasnopolsky, Т. G. Yarnih
• Format: Article
• Language: English
• Published: Ukrmedknyha Publishing House 2017-03-01
• Series: Фармацевтичний часопис
• Subjects: ліпосоми; іринотекан; ліпідний бішар; фосфатидилхолін; холестерин; гомогенізація методом високого тиску.
• Online Access: https://ojs.tdmu.edu.ua/index.php/pharm-chas/article/view/7557

The aim of the work. Research the effect of lipid membrane composition on the encapsulation degree and the size of nanoparticles in the pharmaceutical development of liposomal irinotecan. Materials and Methods. Reagents were purchased from Lipoid, Germany and Sigma-Aldrich, USA. The following instruments were used: Buchi 210, Zetasizer Nano ZS, Minim2 with cassettes with an upper cut-off limit of 30 kDa, Shimadzu LC-20 HPLC. Liposomes with irinotecan were obtained by the "chemical gradient" technology. Results and Discussion. For purposes of liposomal irinotecan creation, lipid membranes with different phosphatidylcholine/cholesterol ratio were studied. It was determined that increasing of the cholesterol weight ratio in the membrane, improves the encapsulation of irinotecan when a «chemical gradient» method was used. On the other hand, at a mass ratio of phosphatidylcholine / cholesterol 75/25 and 70/30 it was impossible to avoid particles larger than 1000 nm formation, that is unacceptable from the position of industrial technology application. Conclusions. An experiment was performed to research the optimal composition of the lipid membrane using three types of cryoprotectants. It was studied the in uence of liposomal membranes with the ratio of lipids phosphatidylcholine/cholesterol: 85/15; 80/20; 75/25; 70/30 on liposomes size and encapsulation degree. The ratio of 80/20 was de ned as optimum for obtaining liposomes with irinotecan. Ways of improving of irinotecan encapsulation into liposomes were outlined.