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目的研究不同粒径辅酶Q10乳剂和脂质体小鼠药物动力学和组织分布。方法以市售辅酶Q10注射液(S)为对照,考察其60 nm乳剂(E60)、120 nm乳剂(E120)、60 nm脂质体(L60)和120nm脂质体(L120)小鼠尾静脉给药后的药物动力学及组织分布特征;采用DAS2.1.1药物动力学软件,进行房室模型和统计矩两种模式拟合;以组织相对摄取率(re)为指标,评价载体的粒径和种类对组织靶向性的影响。结果不同粒径辅酶Q10乳剂和脂质体体内分布均符合双隔室模型;E60、E120、L60和L120的统计矩AUC分别是S组的1.17、1.50、5.99和8.65倍;re结果显示,E60组在心、脾和脑的含量分别是S组的2.64、2.74和1.95倍,E120组在心、脾和脑的含量分别是S组的4.89、3.77和2.38倍;L60组在脑中的含量是S组的1.56倍,L120组在脑和肺的含量分布是S组的2.28和1.85倍。结论载体粒径和种类对辅酶Q10体内分布的影响十分明显,市售注射液组、乳剂组和脂质体组的AUC依次增大,且同一载体中,120 nm组较60 nm组的AUC高;相对市售注射液,乳剂组对心、脾和脑有一定的靶向性,而脂质体组主要靶向于脑和肺,同一载体内,120 nm组在多数组织的富集量多于60 nm组。
Objective To study the pharmacokinetics and tissue distribution of Coenzyme Q10 emulsion and liposome mice with different particle size. Methods The tail vein of 60 nm emulsion (E60), 120 nm emulsion (E120), 60 nm liposome (L60) and 120 nm liposome (L120) was tested with Coenzyme Q10 injection (S) Pharmacokinetics and tissue distribution characteristics after administration; DAS2.1.1 pharmacokinetic software was used to fit the two models of atrioventricular model and statistical moment; the relative tissue uptake rate (re) as an index to evaluate the particle size of the carrier And the impact of species on tissue targeting. Results The distribution of Coenzyme Q10 emulsion and liposome with different particle size all accorded with the double compartmental model. The AUC of E60, E120, L60 and L120 were 1.17,1.50, 5.99 and 8.65 times respectively in S group. The re results showed that E60 The content of heart, spleen and brain in group S were 2.64, 2.74 and 1.95 times respectively in group S, the content of heart, spleen and brain in group E120 were 4.89, 3.77 and 2.38 times respectively in group S; the content in brain of group L60 was S Group 1.56 times, L120 group in the brain and lung content distribution is 2.28 and 1.85 times in the S group. CONCLUSION: The particle size and the type of carrier have an obvious effect on the distribution of coenzyme Q10 in vivo. The AUC of commercially available injection group, emulsion group and liposome group increase in sequence and the AUC of 120 nm group is higher than that of 60 nm group ; Compared with the commercially available injection, the emulsion group had certain targeting to the heart, spleen and brain, while the liposome group mainly targeted to the brain and lung. In the same vector, the concentration of 120 nm group in most tissues At 60 nm group.