Hayakawa E, Nakakura M, Kato Y, Okubo Y, Hosokawa T
Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Shizuoka, Japan.
Chem Pharm Bull (Tokyo). 1991 Mar;39(3):773-6. doi: 10.1248/cpb.39.773.
When doxorubicin was encapsulated into liposomes by freeze-thawing, the percentage of encapsulated doxorubicin (EN%) was found to vary according to the type of buffer solution used. The reason for this was investigated in the present report. Drug-free liposomes prepared by hydration were mixed with doxorubicin dissolved in a certain type of buffer solution that shows a pH decrease on freezing, and this mixture was subjected to freeze-thawing. Doxorubicin was encapsulated by the liposomes due to the difference in pH between freezing and thawing. EN% depended on the pH of the buffer solution before freezing and increased significantly at over pH 7. About 60% of doxorubicin was encapsulated into liposomes after the Ist freeze-thawing cycle, and EN% was increased gradually with the number of freeze-thawing cycles. The addition of sugar to the experimental system was seen to affect doxorubicin encapsulation and the particle size of liposomes.
当通过冻融法将阿霉素包封到脂质体中时,发现包封的阿霉素百分比(EN%)会因所用缓冲溶液的类型而有所不同。本报告对此原因进行了研究。通过水化制备的无药物脂质体与溶解在某种在冷冻时pH值会降低的缓冲溶液中的阿霉素混合,并对该混合物进行冻融处理。由于冷冻和解冻之间的pH值差异,阿霉素被脂质体包封。EN%取决于冷冻前缓冲溶液的pH值,在pH值超过7时显著增加。在第一次冻融循环后,约60%的阿霉素被包封到脂质体中,并且EN%随着冻融循环次数的增加而逐渐增加。在实验体系中添加糖会影响阿霉素的包封以及脂质体的粒径。