Kinetics of distribution and retention of 3H-oestradiol-17 beta in rat tissues: a comparative study with free oestradiol and after its incorporation into liposomes.

Endokrinologie Pub Date : 1982-07-01
Q Jehan, S Srivasta, M Akhlaq, A Ahmad, B S Setty
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Abstract

With a view to impart selective uptake of estrogen by the target tissues of rat, liposomes in which (6,7-3H) oestradiol-17 beta constituted a part of lipid bilayer were used as carriers of the hormone. The distribution and retention of the radioactivity was determined in blood plasma, uterus, liver, kidney, spleen and leg muscle of ovariectomized rat at different time intervals up to 72 hr following a single intravenous injection of free oestradiol (1.61 muCi) or an equivalent amount of liposomal-oestradiol. When free oestradiol was administered, uterus showed peak amount of radioactivity between 30 min to 2 hr and remained high up to 6 hr. In the other tissues examined, maximum amount of radioactivity was seen at 15 min followed by a marked fall at 30 min and also at other subsequent intervals. The pattern of uptake and retention of radioactivity after administration of liposomal-oestradiol was not much different from that of free oestradiol between 1 and 6 hr. A moderate increase in the amount of radioactivity in the nongenital tissues at 24 hr was the only difference noticed with liposomal-oestradiol. It is concluded that targeting of oestradiol preferentially to the uterus could not be achieved through liposomal delivery system.

3h -雌二醇-17 β在大鼠组织中的分布和保留动力学:与游离雌二醇及与脂质体结合后的比较研究。
为了使大鼠靶组织选择性摄取雌激素,脂质体(6,7- 3h)雌二醇-17 β构成脂质双分子层的一部分,作为激素的载体。在单次静脉注射游离雌二醇(1.61 muCi)或等量的脂质体-雌二醇后,测定去卵巢大鼠的血浆、子宫、肝脏、肾脏、脾脏和腿肌在不同时间间隔内的放射性分布和保留情况。当给予游离雌二醇时,子宫放射性在30分钟至2小时内达到峰值,并在6小时内保持高水平。在检查的其他组织中,放射性在15分钟达到最大值,随后在30分钟和其他后续时间间隔显著下降。在1 ~ 6小时内,脂质体-雌二醇对放射性的吸收和保留模式与游离雌二醇没有太大差异。脂质体-雌二醇的唯一区别是24小时非生殖器组织中放射性的适度增加。由此可见,通过脂质体给药系统无法将雌二醇优先靶向至子宫。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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