Study of optimal parameters of extrusion for creation liposome with irinotecan

  • A. V. Stadnichenko National Technical University «Kharkiv Polytechnic Institute»
  • Yu. M. Krasnopolskiy National Technical University «Kharkiv Polytechnic Institute»
  • T. G. Yarnykh National University of Pharmacy, Kharkiv
Keywords: liposomes, irinotecan, extrusion, high pressure homogenization method


Today, the development of drug delivery systems is focused on creating of products with improved pharmacological efficacy and safety of action for the patient. Therefore, the development of systems such as liposomes, emulsions and polymer nanoparticles is a promising direction of development of modern pharmacy.

The objective of the work: To study the optimal extrusion parameters during liposomal irinotecan creation. For the experiment: egg phosphatidylcholine (Lipoid, Germany); cholesterol (Sigma-Aldrich, USA) were using. Liposomes were obtained by «chemical gradient» method.

During the experiment, two homogenization techniques were tested. Sonication and extrusion at high pressure methods were applied to cholesterol modified lipid membranes. It is proved that the sonication method is not applicable because of the particles with diameters greater than 1 000 nm formation.

Two different extruders were used. It was determined, that Microfluidics Microfluidiser M-110P more appropriate for preparation of current liposomal emulsion. Chosen extruder can be applicable for preparation on the homogenous liposomal emulsion without the presence of particles larger than 1 000 nm.

It was tested extrusion mode for liposomes with the following composition of the lipid bilayer: egg phosphatidylcholine/cholesterol 80/20 by weight. For achieving liposomes with diameter 107 nm it is necessary 7 extrusion cycles at 1 500 bar at 20 °C.


1. Keosuke Yoshino, Koji Nakamura, Yoko Terajima et al. Comparative studies of irinotecan-loaded polyethylene glycol-modified liposomes prepared using different PEG modification methods // Biochim. Biophys. Acta - 2012. - N 1818. - P. 2901-2907.
2. Xiong Ying, Liang Li-zhi, Cao Li-ping, et al. Clinical effects of irinotecan hydrochloride in combination with cisplatin in neoadjuvant chemotherapy in locally advanced cervical cancer // Gynecologic Oncology. - 2011. - V. 123, N 1, P. 99-104.
3. Megoa M., Chovanec J., Vochyanova-Andrezalova I. et al. Prevention of irinotecan induced diarrhea by probiotics: A randomized double blind, placebo-controlled trial study // Complementary Therapies in Medicine. - 2015. -V 23, N 3, - pp. 356-362.
4. Bozzuto G., Molinari A. Liposomes as nanomedical devices // Int. J. Nanomedicine. - 2015 - N 10 - R. 975-999.
5. Torchilin V. Tumor delivery of macromolecular drugs based on EPR effect // Adv. Drug Deliv. Rev. - 2011. - N 63. - P. 131-135.
6. Fujita Ken-ichi, Kubota Yutaro, Ishida Hiroo, Sasaki Yasutsuna. Irinotecan, a key chemotherapeutic drug for metastatic colorectal cancer // World J. Gastroenterol. - 2015 - V. 21, N 43. - P. 12234-12248.
7. West-Ward Pharmaceuticals Corp. / Irinotecan prescribing information. [Electronic Resourc]. 2016. - Access mode: irinotecan.html
8. Hongyan Weia, Juan Songa, Hao Lib et al. Active loading liposomal irinotecan hydrochloride: Preparation, in vitro and in vivo evaluation // Asian J. Pharmac. Sci - 2013. - V. 8, N 5. - P. 303-311.
9. Ko A. H., Tempero M. A., Shan Y.-S. et al A multinational phase 2 study of nanoliposomal irinotecan sucrose (PEP02, MM-398) for patients with gemcitabine-refractory metastatic pancreatic cancer // Br. J. Cancer. - 2013. -V 109, N 4. - P. 920-925.
10. Shvets V.I., Krasnopolsky Yu.M. Liposomes in pharmacy products of nanobiotechnology // Provizor. - 2008. - N 03. - P. 22-25.
How to Cite
Stadnichenko, A. V., Krasnopolskiy, Y. M., & Yarnykh, T. G. (2018). Study of optimal parameters of extrusion for creation liposome with irinotecan. Farmatsevtychnyi Zhurnal, (2), 77-82. Retrieved from
Pharmaceutical technology

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