布洛芬固体脂质纳米粒的制备及家兔体内药动学研究

采用乳化分散-超声法制备布洛芬固体脂质纳米粒(IB-SLN),对其粒径、zeta电位、包封率、载药量、体外释放等进行体外评价,并考察IB-SLN经皮给药后兔体内药动学特征.结果显示,研究制备的IB-SLN的平均粒径为(100±20)nm,zeta电位为-43.9mV,包封率为92.6%,载药量为3.33%.兔体内药动学研究显示,IB-SLN可有效促进布洛芬的经皮吸收,布洛芬固体脂质纳米粒凝胶剂经皮给药后的AUC和Cmax分别为640.86ng·h/mL和65.94 ng/mL,分别是布洛芬凝胶剂的12.6倍和4.5倍.研究结果提示,固体脂质纳米粒作为布洛芬经皮给药载体可有效促进药物的透皮吸收,并可使药物缓慢平稳释放,其应用前景广泛.

Preparation of Ibuprofen Solid Lipid Nanoparticles and Its Pharmacokinetics in Rabbit

Ibuprofen solid lipid nanoparticles （IB-SLN） is prepared by using the method of emulsification dispersion-ultrasonication. The particle size, zeta potential, encapsulation efficiency, drug loading and release behaviors of IB-SLN are evaluated in vitro, the pharmacokinetic characteristics in rabbits are investigated after percutaneous administration. The results are as follows： the particle size is 100 ＋ 20 nm, the zeta potential is -43.9 mV, the drug loading of IB-SLN is 3.33% , and the encapsulation efficiency is 92.6%. The pharmaeokinetie study in rab- bits after percutaneous administration demonstrates that IB-SLN can improve the transdermal absorption of ibuprofen effectively. The AUC and Cmax of IB-SLN transdermal gels are 640.86 ng ·h · mL^-1 and 65.94 ng · mL^-1 , which are 12.6 and 4.5 folds, respectively, compared with the eases of ibuprofen transdermal gels. The SLN can effectively enhance the transdermal penetration and bring a slow and balanced release of IB. Therefore, SLN could be a potential delivery system for TDDS.