Preliminary Studies on X-Ray-sensitive Liposome

Abstract

Abstract: The synthesis of a new type of X-ray-sensitive compound “di-(1-hydroxylundecyl) diselenide” and its application in the preparation of a new type of liposome with X-ray sensitivity was reported. This new liposome was synthesized to encapsulate doxorubicin hydrochloride(Dox), with its physical and chemical properties, stability, and radiation sensitivity determined. Based on the pH-gradient method, liposomal Dox was prepared via ultrasonic emulsification and then purified on a Sephadex G50 mini-column. UV spectrophotometry and liquid chromatography were used to detect the encapsulation efficiency and radiation sensitivity of the Dox-loaded liposome. The results show that through changes in release rate, this liposome shows a relative radiosensitivity. In terms of radiation sensitivity, the drug leak rate of the X-ray-sensitive Dox-loaded liposome increased gradually and peaked at 65.4% under the X-ray radiation of a dose of 10 Gy or more than 10 Gy, which is significantly different from that of ordinary liposomes. Meanwhile, X-ray-sensitive Dox-loaded liposome has a good dispersion stability, with an average particle size of approximate 120 nm. The efficiency of this liposome encapsulating Dox was 75.84%, slightly lower than that of ordinary liposomes. The X-ray-sensitive Dox-loaded liposome exhibited suspension stability within 30 d of storage at 4 °C, without visible precipitation. Di-(1-hydroxylundecyl) diselenide is safe and noncytotoxic and compared with those of synthetic phospholipids its synthesis is low cost and does not require complex conditions.

Key words: Drug delivery system, Selenium, Radio-chemo-concurrent, Liposome

MENG Fan-xu, XU Hua-ping, QI Yan-fei, XU Kun, SONG Xiu-ling, NIU Shu, LI Juan. Preliminary Studies on X-Ray-sensitive Liposome[J]. Chemical Research in Chinese Universities, 2012, 28(2): 319-322 .

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