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目的筛选口服槲皮素纳米结构脂质载体的处方和制备工艺,并对其进行体外评价。方法采用溶解度考察和正交优化设计法结合,优选出较优的处方,并通过伪三元相图验证,评价其粒子形态、多分散性、包封率。通过测定不同稀释倍数、不同缓冲液对粒径的影响及药物的体外溶出行为,对槲皮素纳米结构脂质载体进行体外评价。结果最佳处方组成为硬脂酸-Labrafac lipophile WL1349-Cremophor EL-Transcutol P(3:5:5:2),所得纳米结构脂质载体为圆整的类球形粒子,平均粒径为69nm,包封率为89.0%,PDI=0.251。同槲皮素混悬液比较,槲皮素纳米结构脂质载体的体外溶出明显提高。结论口服纳米结构脂质载体释药系统制备工艺简便,粒子性状符合要求,可提高难溶性药物的体外溶出。
Objective To screen prescription and preparation technology of orally administered quercetin nanostructured lipid carrier and evaluate it in vitro. Methods The combination of solubility study and orthogonal design method was used to optimize the prescription and the particle morphology, polydispersity and entrapment efficiency were evaluated by pseudo-ternary phase diagram. The quercetin nanostructured lipid carrier was evaluated in vitro by measuring the different dilution times, the effect of different buffers on the particle size and the in vitro dissolution behavior of the drug. RESULTS: The optimal formulation consisted of spherical liposomes with the average particle diameter of 69 nm and the average particle size of 69 nm, including stearic acid-Labrafac lipophile WL1349-Cremophor EL-Transcutol P (3: 5: 5: 2) The encapsulation efficiency was 89.0%, PDI = 0.251. Compared with the quercetin suspension, quercetin nanostructured lipid carrier dissolution significantly increased in vitro. Conclusions Oral nanostructured lipid carrier drug delivery system has the advantages of simple preparation process, satisfactory particle characteristics and improved dissolution of insoluble drugs in vitro.