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棉酚为我国首创男用节育药。目前认为棉酚能干扰睾丸精子发生的后期,镜检付睾尾部,精子活力下降,畸形率增高,但口服棉酚分布于睾丸内的含量极低,可能与棉酚不易透过血睾屏障有关。我们试图应用脂质体作为药物载体,使更多的棉酚能选择性地进入睾丸,提高局部浓度,以达到降低用药剂量、减低对主要脏器的毒副作用、缩短起效时间的目的。为此,探讨了研制棉酚脂质体的条件。我们采用卵磷脂、胆固醇为膜料,与棉酚共置于圆底烧瓶内,溶于氯仿,减压除去氯仿,使在瓶壁形成一层薄膜,然后加磷酸盐缓冲液(pH7.0),在通氮
Gossypol is the first male birth control medicine in our country. At present, gossypol can interfere with testicular spermatogenesis late, microscopic examination of the tail attached to the tail, decreased sperm motility, increased deformity, but oral gossypol content in the testis is extremely low, may not be related to gossypol penetration of the blood testis barrier . We tried to use liposome as a drug carrier, so that more gossypol can selectively enter the testis and increase the local concentration in order to reduce the dosage, reduce the side effects of major organs and shorten the onset time. Therefore, the conditions for the development of gossypol liposomes were discussed. We use lecithin and cholesterol as the membrane material, co-placed with gossypol in a round-bottomed flask, dissolved in chloroform and chloroform removed under reduced pressure to form a thin film on the wall of the bottle followed by addition of phosphate buffer (pH 7.0) In nitrogen