脂质运载蛋白型前列腺素D合成酶作为难溶性药物给药载体的研究进展

Advances in using lipocalin-type prostaglandin D synthase as delivery carrier for poorly water-soluble drugs

增加难溶性药物的溶解度一直是药物开发的极大挑战。脂质运载蛋白型前列腺素D合成酶(L-PGDS)属于脂质运载蛋白超家族成员,可作为一种新型的给药载体,用于制备难溶性药物给药系统。本文通过分析归纳现有文献,对L-PGDS的结构、性质和制备及L-PGDS与难溶性药物的作用机制、制备方法和应用等进行综述。L-PGDS通过亲水-疏水相互作用与难溶性药物形成复合物,显著提高药物的溶解度、生物利用度和疗效,目前已应用于口服和注射给药系统,其处方工艺简单,生物相容性好,在难溶性药物新剂型和新品种开发方面具有良好的应用前景。

Enhancing the solubility of poorly water-soluble drugs in drug development is a great challenge.As a member of the lipocalin superfamily,lipocalin-type prostaglandin D synthase(L-PGDS)can be used as a novel drug carrier for insoluble drug delivery system.Here we summarized the structure,property and production method of L-PGDS,and mechanism of forming complex,preparation process,and application of drug and L-PGDS.L-PGDS formed complexes with poorly water-soluble drugs by hydrophilic and hydrophobic interaction,which significantly enhanced the solubility,dissolution,bioavailability and therapeutic effect of drug,and they had been applied in oral and injected drug delivery systems.L-PGDS has good application prospect in novel dosage forms and new products of poorly water-soluble drugs with simple formulation and preparation process,and good compatibility.