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目的 以醋酸曲安奈德 (TAA)为模型药物 ,以三棕榈酸甘油酯为脂质材料制备醋酸曲安奈德固体脂质纳米粒(SLN)卡波姆凝胶 ,考察其特性以及药物经皮渗透性能。方法 采用高压乳匀技术制得TAA SLN分散液 ,并制成卡波姆凝胶 ,考察了卡波姆凝胶中SLN的微观形态、粒径、Zeta电位、包封率等理化特性和稳定性、体外药物释放行为。采用改进的Franz扩散池研究了SLN卡波姆凝胶的药物经皮渗透性能。结果 制得的TAA SLN为均匀的球形粒子 ,不同载药量SLN粒径为 95 . 5～ 186 . 2nm ,Zeta电位为 - 2 6 .3～ - 15 . 7mV ,包封率为 6 7. 4 3%～ 90 . 3% ;SLN卡波姆凝胶 37℃储存三个月后SLN粒径略有增大 ,Zeta电位无明显变化 ;SLN卡波姆凝胶体外药物释放符合Higuchi方程 (DR % =6 . 3979t1/2 +3. 15 2 9,r2 =0 . 95 18) ;经皮渗透实验结果表明 ,与相同药物浓度的普通卡波姆凝胶比较 ,SLN卡波姆凝胶药物经皮渗透速率和药物 2 4h累积渗透量显著提高。结论 TAA SLN卡波姆凝胶稳定性好 ,对药物释放具有缓控释作用 ,能显著促进药物经皮渗透 ,有望成为新型经皮给药制剂。
Objective To prepare triamcinolone acetonide solid lipid nanoparticles (SLN) carbomer gel with tripalmitin as lipid material by taking triamcinolone acetonide acetate (TAA) as a model drug and investigate its characteristics and transdermal drug permeation performance. Methods TAA SLN dispersion was prepared by high-pressure homogenization technique and carbopol gel was prepared. The physicochemical properties and stability of SLA micro-morphology, particle size, Zeta potential and entrapment efficiency were investigated. , In vitro drug release behavior. The drug percutaneous permeability of SLN carbomer gel was investigated using a modified Franz diffusion cell. Results TAA SLN obtained uniform spherical particles, different drug loading SLN particle size of 95 5 ~ 186 2nm, Zeta potential of -26 3 ~ - 15 7mV, encapsulation efficiency of 6 7.4 3% -90.3%. The particle size of SLN increased slightly after stored for 3 months at 37 ℃ and there was no significant change in Zeta potential. The in vitro drug release of SLN carbomer gel was in accordance with Higuchi’s equation (DR% = 6.37979t1 / 2 +3.15 2 9, r2 = 0.95 18); transdermal permeation test results show that, compared with the same drug concentration of ordinary carbopol gel, SLN carbomer gel drug percutaneous Penetration rate and drug 24 h accumulated infiltration significantly increased. CONCLUSION TAA SLN carbomer gel has good stability and sustained and controlled release of drug release, which can significantly promote transdermal drug penetration and is expected to become a new transdermal drug delivery preparation.