CAJ | 학술논문

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95.5～186.2 nm, Zeta电位为-26.3～-15.7 mV, 包封率为67.43%～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%=6.397 9t1/2+3.152 9, r2=0.951 8);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24 h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.
목적이작산곡안내덕(TAA)위모형약물, 이삼종려산감유지위지질재료제비작산곡안내덕고체지질납미립(SLN)잡파모응효, 고찰기특성이급약물경피삼투성능.방법채용고압유균기술제득TAA-SLN분산액, 병제성잡파모응효, 고찰료잡파모응효중SLN적미관형태、립경、 Zeta전위、포봉솔등이화특성화은정성、체외약물석방행위.채용개진적Franz확산지연구료SLN잡파모응효적약물경피삼투성능.결과제득적TAA-SLN위균균적구형입자, 불동재약량SLN립경위95.5～186.2 nm, Zeta전위위-26.3～-15.7 mV, 포봉솔위67.43%～90.3%; SLN잡파모응효37 ℃저존삼개월후SLN립경략유증대, Zeta전위무명현변화; SLN잡파모응효체외약물석방부합Higuchi방정(DR%=6.397 9t1/2+3.152 9, r2=0.951 8);경피삼투실험결과표명, 여상동약물농도적보통잡파모응효비교, SLN잡파모응효약물경피삼투속솔화약물24 h루적삼투량현저제고. 결론 TAA-SLN잡파모응효은정성호, 대약물석방구유완공석작용, 능현저촉진약물경피삼투,유망성위신형경피급약제제.
Aim To prepare triamcinolone-acetonide-acetate (TAA)-loaded solid lipid nanoparticles (SLN) carbomer gel with tripalmitin glyceride (TPG), and investigate their characteristics and transdermal drug delivery. Methods SLN suspension was prepared by high-pressure homogenization technique, and then mixed with carbomer gel matrix to get SLN gel. The morphology, particle size with polydispersity index (PI) and zeta potential were examined by atomic force microscopy (AFM) and photon correlation spectroscopy (PCS). The entrapment efficiency, stability and in vitro drug release were also studied. The transdermal drug delivery through porcine ear skin was evaluated using modified Franz diffusion cells. Results The SLN had a spherical shape with the average size of (95.5-186.2) nm, the zeta potential of (-26.3--15.7) mV and the entrapment efficiency of 67.4%-90.3% for different TAA encapsulated compounds. TAA-SLN carbomer gel had good stability, the release profile in vitro fitted Higuchi equation. In comparison with conventional hydrogels, TAA-SLN carbomer gel resulted in higher drug permeation amount and drug deposition within porcine ear skin after 24 h penetration experiment. Conclusion TAA-SLN carbomer gel is prepared with stable physicochemical properties. The release profile and improved drug permeation into skin make it be a promising vehicle for transdermal drug delivery.