黄藤素柔性纳米脂质体水凝胶贴剂的制备及体外透皮给药研究

Studies on the Preparation and Transdermal Drug Delivery of Hydrogel Patches of Palmatine Loaded Flexible Nano-liposomes

关键词:  黄藤素  柔性脂质体  水凝胶贴剂  透皮给药

Key words:  palmatine  flexible liposomes  hydrogel patches  transdermal drug delivery

摘要:

为奶牛乳房炎的治疗提供了一种新型高效的透皮给药制剂，并考察其体外透皮给药的行为特点。采用薄膜分散法制备黄藤素柔性纳米脂质体(PFL)，高效液相色谱仪(HPLC)测定包封率，透射电镜(TEM)观察PFL的结构、激光粒度仪(LPSA)测定PFL的粒径和表面Zeta电位；然后将PFL制备成水凝胶贴剂(PFL-HP)，并采用立式双室扩散池考察PFL-HP体外透皮给药的行为特点，并同药物水凝胶贴剂(P-HP)与加入5%氮酮的水凝胶贴剂(P-A-HP)进行对照。结果表明，PFL对黄藤素的包封率为（79±2.23）%，PFL为圆球形层状囊泡结构，粒径为（190±24）nm，Zeta电位为（-54±2.65）mV；PFL-HP膏体柔软、膏面平整光洁，黏附性良好可48 h黏附于奶牛乳房而不脱落；24 h时，PFL-HP的药物累积透过量是P-HP与P-A-HP的2.12倍(t-test,P<0.05)与1.13倍(t-test, P>0.05)，同时，PFL-HP组中药物在皮肤组织的滞留量（即“储库效应”）也高于P-HP与P-A-HP(t-test,P < 0.05)。黄藤素柔性纳米脂质体水凝胶贴剂(PFL-HP)药物透皮吸收效率高、黏附性良好、使用方便，奶牛对其具有良好的依从性。PFL-HP可作为治疗奶牛乳房炎的一种新型高效透皮给药制剂。

Abstract:

In order to develop a new type of highly effective transdermal drug delivery preparation for the treatment of cow mastitis,and the transdermal drug delivery of the preparation was also investigated.The palmatine loaded flexible nano-liposomes (PFL)were prepared by thin-film homogenization method.The entrapment rate of palmatine was evaluated by HPLC, the pharmaceutical properties(such asstructure, size and zeta potential)of PFL were evaluated by the TEM and LPSA, respectively.Then the PFL added to hydrogel patches and PFL loadedhydrogel patches(PFL-HP)were obtained. The vertical dual chamber diffusion cells were used to investigate the characteristics of palmatine transdermal drug delivery from PFL-HP, and the P-HP and P-A-HP used as control group.Results showed that the prepared PFL had aclosed spherical shape and lamellar structure with a homogeneous size of 190±23nm, and exhibited a negative charge of -54±2.65mV. The PFL-HP with characteristics of better flexibleness, matrix surface smooth and clean,also possess higher adhesive force and adhere to the cow breasts and not fall off in 48 h.At 24 h, the accumulated permeation amount of palmatine from the PFL-HP was 2.12(t-test,P<0.05)and 1.13(t-test, P> 0.05)folds than that of P-HP and P-A-HP, respectively.And the quantityof palmatine remaining in theskin tissue at the end of the 24 h experiment was also significantly greaterfrom the PFL-HP than from P-HP and P-A-HP.The PFL-HP with characteristics of higher transdermal permeability of drug, better flexibleness and adhesive force. Cows also have good compliance with PFL-HP. So, the PFL-HP was shown to be a new and effective transdermal drug delivery preparation for the treatment of cowmastitis and has a broad application prospects.