Brailoiu E, Huhurez G, Slatineanu S, Filipeanu C M, Costuleanu M, Branisteanu D D
Department of Physiology, University of Medicine and Pharmacy Gr. T. Popa, Iasi, Romania.
Biomed Chromatogr. 1995 Jul-Aug;9(4):175-8. doi: 10.1002/bmc.1130090405.
The thin-layer chromatographic (TLC) behaviour of liposomes containing inositol phosphates (IPs) was studied. The liposomes contained different concentrations of D-myo-inositol 1,4,5k-trisphosphate (IP3), D-myo-inositol 1,2,6-trisphosphate (alpha-trinositol, PP 56, a novel Perstorp Pharma derivative), D-myo-inositol 1,3,4,5-tetrakisphosphate (IP4), D-myo-inositol 1,3,4,5,6-pentakisphosphate (IP5) and D-myo-inositol 1,2,3,4,5,6-hexakisphosphate (IP6). Migration of all liposome batches was compared to that of control liposomes (containing only triple distilled water), and to that of free phosphatidylcholine (PC); the same amount of lipid was used in all situations. Thin-layer chromatography was performed on silica gel as adsorbent. As solvent we used an n-buthanol:ethanol:water mixture in a 4:3:3 volume ratio. Significant differences were found between PC and all liposome batches, as well as between control liposomes and the ones containing IP3, alpha-trinositol, IP4, or IP5, in various concentrations. Liposomes containing IP6 migrate completely differently compared not only to phosphatidylcholine and control liposomes, but also to the ones containing other IPs ( < 10(-3) M). Unlike the other IPs studied, liposome-entrapped IP6 elicits dose-dependent contractions of the isolated rat aorta. This suggests that liposomes loaded with IP6 undergo, during or after their preparation, physico-chemical alterations that eventually change their drug-delivery capacity.
对含有肌醇磷酸酯(IPs)的脂质体的薄层色谱(TLC)行为进行了研究。这些脂质体含有不同浓度的D-肌醇1,4,5-三磷酸(IP3)、D-肌醇1,2,6-三磷酸(α-三肌醇,PP 56,Perstorp Pharma公司的一种新型衍生物)、D-肌醇1,3,4,5-四磷酸(IP4)、D-肌醇1,3,4,5,6-五磷酸(IP5)和D-肌醇1,2,3,4,5,6-六磷酸(IP6)。将所有脂质体批次的迁移情况与对照脂质体(仅含三蒸水)以及游离磷脂酰胆碱(PC)的迁移情况进行比较;所有情况下使用的脂质量相同。以硅胶为吸附剂进行薄层色谱分析。作为溶剂,我们使用体积比为4:3:3的正丁醇:乙醇:水混合物。在PC与所有脂质体批次之间,以及对照脂质体与含有不同浓度IP3、α-三肌醇、IP4或IP5的脂质体之间发现了显著差异。含有IP6的脂质体的迁移情况与磷脂酰胆碱和对照脂质体完全不同,与含有其他IPs(<10^(-3) M)的脂质体也不同。与所研究的其他IPs不同,脂质体包裹的IP6可引起离体大鼠主动脉的剂量依赖性收缩。这表明装载有IP6的脂质体在制备过程中或制备后会发生物理化学变化,最终改变其药物递送能力。