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以异烟肼为模型药物,合成了异烟肼取代卵磷脂疏水链的两亲性异烟肼磷脂衍生物.用薄膜超声分散法将其制备成脂质体,从而将异烟肼脂质体的药脂比从0.1～0.3提高至2.0,包封率由2%提高到接近100%.通过调节超声处理时间和磷脂浓度可制得粒径大小可控的脂质体.体外释药研究表明,该脂质体具有明显的控制释放性能.这种以药物分子取代卵磷脂疏水链的两亲性磷脂衍生物制备脂质体的方法,为难包封于脂质体的药物实现高包封率提供了新途径.
Isoniazid was used to replace amphipathic isoniazid phospholipid derivative of lecithin hydrophobic chain with isoniazid as a model drug.Ultrahydrazone liposomes Of the lipid ratio increased from 0.1 to 0.3 to 2.0, the encapsulation efficiency increased from 2% to nearly 100% by adjusting the sonication time and phospholipid concentration can be obtained particle size controllable liposomes in vitro release studies have shown that , The liposome has a significant controlled release performance of this drug molecules instead of lecithin hydrophobic chain amphiphilic phospholipid derivatives prepared liposomes for the drug is difficult to encapsulate the liposomes to achieve a high entrapment efficiency Provide a new way.