脂质体载药性能与卵磷脂的关系

探讨了卵磷脂对脂质体载药性能的影响。用逆相蒸发法制备阿糖胞苷脂质体,通过测定脂质体的包封率、平均粒径和药物渗漏量,考察了蛋黄卵磷脂、大豆卵磷脂及猪脑卵磷脂对脂质体载药性能的影响。实验结果表明,在n(PC)∶n(CHOL)=1∶1的条件下,蛋黄卵磷脂脂质体的平均粒径为2.59μm,包封率为(17.02±0.21)%,在37℃经40 h温育后,平均粒径增加0.53μm,药物渗漏量为(0.18±0.01)mg/h。平均粒径和包封率均高于大豆卵磷脂脂质体及猪脑卵磷脂脂质体,平均粒径增加值低于大豆卵磷脂脂质体及猪脑卵磷脂脂质体,渗漏速度高于猪脑卵磷脂脂质体,但低于大豆卵磷脂脂质体。对比实验证明,蛋黄卵磷脂脂质体的载药性能较好。

The Relationship Between Drug Carrying Ability of Liposomes and Phosphatidylcholines

The effect of phosphatidylcholine(PC) on the drug carrying ability of liposome was investigated.Cytarabine(Ara-C) liposome was made by reverse evaporation method.The effect of egg yolk PC(EPC),soya PC(SPC) and pig brain PC(PPC) on the drug carrying ability of liposomes was evaluated by measurement of their encapsulation efficiencies,mean size diameters and drug-leaking amount.Experimental results comfirmed that under the condition of n(PC)∶n(cholesterol)=1∶1 the mean size diameter of EPC liposome is 2.59 μm,the encapsulation efficiency is 17.02%±0.21%,the increase of mean size diameter after cultivation at 37 ℃ for 40 h is 0.53 μm,and the drug-leaking amount is(0.18±0.01) mg/h.Both mean size diameter and encapsulation efficiency of EPC liposome are higher than those of SPC liposome and PPC liposome,but the increase of mean size diameter is lower than that of SPC liposome and PPC liposome.The leakage rate was higher than that of PPC liposome,but lower than that of SPC liposome.The comparative tests show that EPC liposome has better drug carrying ability.