甲氧沙林脂质体凝胶基质的筛选研究

Study on base screening of 8-methoxypsoralen liposomal gels

目的对不同浓度的卡波姆—934和泊洛沙姆—407为基质的甲氧沙林脂质体(LMOP)凝胶体外释药模式进行考察研究,以筛选出较优的凝胶基质及浓度。方法分别制备卡波姆—934浓度为0.5%、1%和2%以及泊洛沙姆—407浓度为20%、25%和30%的LMOP凝胶,用高效液相色谱法(HPLC)测定累积释药量Q,将数据进行释放动力学模型拟合。结果体外初步筛选实验表明,各凝胶剂的体外释药均符合Higuchi方程。0.5%卡波姆—934:Q=9.785 7 t1/2+18.932 7(r=0.997);1%卡波姆—934:Q=10.065 6 t1/2+20.394 3(r=0.999);2%卡波姆—934:Q=10.744 9 t1/2+21.468 9(r=0.994);20%泊洛沙姆—407:Q=11.625 8 t1/2+30.191 9(r=0.989);25%泊洛沙姆—407:Q=10.584 6 t1/2+29.433 4(r=0.996);30%泊洛沙姆—407:Q=9.229 1 t1/2+29.452 7(r=0.993)。结论经由Higuchi方程比较,0.5%卡波姆—934是经筛选的较佳的LMOP凝胶基质。

Objective To study the 8-methoxypsoralen liposomal gel （LMOP） using different concentrations of carbomer and poloxamer, respectively in vitro-release model, and to screen the optimal base and its concentration for LMOP gel base. Methods LMOP gels using different bases in different concentrations ie. 0.5 %, 1%, 2 % of carbomer and 20 %, 25 %, 30 % of poloxamer were prepared. High performance liquid chromatography （HPLC） was used to determine the accumulative release amount of the 8-methoxypsoralen from the gels in vitro. The data were fitted in with pharmacokineties model. Results The experiment of screening showed the drug release model in vitro of the different gels could be described as Higuchi equations： 0.5% carbomer -934： Q= 9.785 7t1/2 ＋ 18.932 7（ r = 0.997） ; 1% carbomer -934：Q= 10.065 6 t1/2 ＋ 20.394 3（ r = 0.999） ; 2% carbomer -934： Q= 10.744 9 t1/2 ＋ 21.468 9（ r = 0. 994） ; 20 % poloxamer -407： Q = 11.625 8 t1/2 ＋ 30.191 9 （ r = 0. 989） ; 25 % poloxamer -407： Q = 10.584 6 t1/2 ＋ 29.433 4（r=0.996）;30% poloxamer-407：Q=9.229 1 t1/2＋29.452 7（r=0.993）.Conclusion Higuchi equations showed 0.5 % carbomer -934 is a better base for LMOP gels.