新型抗肝损伤化合物XXH-32脂质体的制备及其药剂学性质研究
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摘要
目的制备新型抗肝损伤化合物XXH-32脂质体,并对其药剂学性质进行研究。方法采用薄膜分散法制备脂质体,正交试验设计考察影响制备工艺的因素,用扫描电镜观察脂质体表面形态,对制备的XXH-32脂质体的粒径、载药量、包封率等性质及体外释放特性进行了研究。结果 XXH-32脂质体的最佳制备工艺稳定,脂质体形态圆整,粒径分布适宜。优化工艺制得的脂质体平均粒径为(175.2±2.55)nm,多分散系数为0.262±0.01,载药量为(2.60±0.12)%,包封率为(95.05±1.06)%,体外释放符合一级动力学方程,ln(100-Q)=-0.06t+4.79(R~2=0.9794)。结论本实验获得了较理想的新型抗肝损伤化合物XXH-32脂质体,其体外释药特性符合缓释制剂特征。
OBJECTIVE To prepare a novel anti-liver injury compound XXH-32 liposome and study its pharmaceutical properties. METHODS The liposome was prepared by thin-film dispersion method. The optimized preparation process was investigated by a series of experiments under orthogonal design. The surface morphology of the liposome was observed by scanning electron microscopy. The particle size and drug loading of the liposome was measured, and XXH-32 release behavior from the liposome was studied. RESULTS Under the optimal preparation process, the liposome was presented round in shape with average diameter of(175.2±2.55)nm, polymer dispersity index was 0.262±0.01. The content of XXH-32 in the liposome was(2.60±0.12)%, and the entrapment efficiency was(95.05±1.06)%. The release of XXH-32 from the liposome presented a first-order kinetic behavior. The equation as follow ln(100-Q)=-0.06t+4.79, R~2=0.979 4. CONCLUSION XXH-32 liposome was prepared successfully with high drug entrapment efficiency. XXH-32 in the liposome showed a significantly slower release behavior.
OBJECTIVE To prepare a novel anti-liver injury compound XXH-32 liposome and study its pharmaceutical properties. METHODS The liposome was prepared by thin-film dispersion method. The optimized preparation process was investigated by a series of experiments under orthogonal design. The surface morphology of the liposome was observed by scanning electron microscopy. The particle size and drug loading of the liposome was measured, and XXH-32 release behavior from the liposome was studied. RESULTS Under the optimal preparation process, the liposome was presented round in shape with average diameter of(175.2±2.55)nm, polymer dispersity index was 0.262±0.01. The content of XXH-32 in the liposome was(2.60±0.12)%, and the entrapment efficiency was(95.05±1.06)%. The release of XXH-32 from the liposome presented a first-order kinetic behavior. The equation as follow ln(100-Q)=-0.06t+4.79, R~2=0.979 4. CONCLUSION XXH-32 liposome was prepared successfully with high drug entrapment efficiency. XXH-32 in the liposome showed a significantly slower release behavior.
引文
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[2]ZHANG Z W,WU S S,HUANG L N,et al.Cost-effectiveness analysis of magnesium isoglycyrrhizinate used in the treatment of antineoplastic drugs-induced acute liver injury[J].Pharm Today(今日药学),2017,27(10):701-705.
[3]KHAN S R,ALJUHANI N,MORGAN A G,et al.Cytoprotective effect of isoniazid against H2O2 derived injury in HL-60 cells[J].Chem Biol Interact,2016(244):37-48.
[4]JU L P,XI J J,ZHAO Y M,et al.Synthesis and Anti-liver injury activities evaluation of novel acetylcysteine derivatives with disulphide and thioester bonds[J].Chin J Mod Appl Pharm(中国现代应用药学),2018,35(3):340-344.
[5]DA S C L,BRANCH D R,DUONG T T,et al.The immune-stimulation capacity of liposome-treated red blood cells[J].J Liposome Res,2018,28(3):173-181.
[6]WANG Z,JAY C M,EVANS C,et al.Preclinical biodistribution and safety evaluation of a pbi-sh RNA STMN1lipoplex after subcutaneous delivery[J].Toxicol Sci,2017,155(2):400-408.
[7]WANG X,HUANG H,ZHANG L,et al.PCM and TATco-modified liposome with improved myocardium delivery:in vitro and in vivo evaluations[J].Drug Deliv,2017,24(1):339-345.
[8]LI S,ZHOU G Y.Antitumor activity of lipusu on ovarian cancer transplantation tumor in F344 rats[J].Chin Hosp Pharm J(中国医院药学杂志),2015,35(19):1746-1749.
[9]ZHANG N,CHEN H,LIU A Y,et al.Gold conjugate-based liposomes with hybrid cluster bomb structure for liver cancer therapy[J].Biomaterials,2016(74):280-291.
[10]MAGARKAR A,ROG T,BUNKER A.A computational study suggests that replacing PEG with PMOZ may increase exposure of hydrophobic targeting moiety[J].Eur J Pharm Sci,2017(103):128-135.
[11]中国药典.四部[S].2015:121,354-356,368-369.
[12]ZHAO Y N,ZHANG S B,CUI S H,et al.The development of cholesterol embedded cationic liposomes for gene transfer[J].Chin J Cell Biol(中国细胞生物学学报),2014,36(9):1257-1261.