| 一种新型的地塞米松棕榈酸酯脂质体制剂及其对小鼠的抗炎作用研究 |
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| 引用本文： | 李继 a,杨静b,王文新c,于吉臣c,傅经国c,王晓来a. 一种新型的地塞米松棕榈酸酯脂质体制剂及其对小鼠的抗炎作用研究[J]. 中国化学, 2009, 27(7): 1411-1414. DOI: 10.1002/cjoc.200990237 |
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| 作者姓名： | 李继 a 杨静b 王文新c 于吉臣c 傅经国c 王晓来a |
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| 作者单位： | a中国科学院兰州化学物理研究所，中国兰州，730000 ;b河南中医学院药学院, 中国郑州，450008 ;c河南省科学院化学研究所,中国郑州， 450002 ; |
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| 摘 要： | 本文报道了一种新型的长循环脂质体地塞米松棕榈酸酯 (DPL long-circulating) 的药物运载系统。将磷脂和胆固醇通过薄膜分散-挤压法得到该DPL long-circulating。考察了该DPL long-circulating配方的稳定性。用老鼠实验来评价DPL long-circulating, DPL和DSP的抗炎活性与急毒性。应用薄膜分散-挤压的方法可以成功得到DPL long-circulating。实验结果表明DPL long-circulating有均匀的粒径和稳定的性质。在抗炎实验中，DPL long-circulating和DPL表现出比DSP更强的抗炎效果。急性毒性实验则表明DSP注射液与DPL long-circulating和DPL相比有较小的毒性，提示DPL long-circulating和DPL可能因为被动靶向作用从而提高了生物利用度。使用上述方法得到的DPL long-circulating满足了质量要求，并且有较高的抗炎活性及急毒性。
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| 关 键 词： | 地塞米松棕榈酸酯 长循环脂质体 急性毒性 抗炎性 |
| 收稿时间： | 2009-03-31 |
| 修稿时间： | 2009-04-22 |
A Novel Liposomal Dexamethasone Palmitate Formulation and Anti‐inflammatory Effects on Mice |
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| Ji LI,Jing YANG,Wenxin WANG,Jichen YU,Jingguo FU,Xiaolai WANG. A Novel Liposomal Dexamethasone Palmitate Formulation and Anti‐inflammatory Effects on Mice[J]. Chinese Journal of Chemistry, 2009, 27(7): 1411-1414. DOI: 10.1002/cjoc.200990237 |
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| Authors: | Ji LI Jing YANG Wenxin WANG Jichen YU Jingguo FU Xiaolai WANG |
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| Affiliation: | 1. Tel.: 0086‐0371‐65511752;2. Fax: 0086‐0371‐65718110;3. School of Pharmacy, Henan University of Traditional Chinese Medicine, Zhengzhou, Henan 450008, China;4. Institute of Chemistry, Henan Academy of Science, Zhengzhou, Henan 450002, China;5. Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences, Lanzhou, Gansu 730000, China |
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| Abstract: | A novel dexamethasone palmitate liposomal long‐circulating (DPL long‐circulating) drug delivery system was established. The DPL long‐circulating and DPL (dexamethasone palmitate liposomal) systems were prepared by film‐distributed extrusion with phospholipid and cholesterol. The formulation stability of DPL long‐circulating and DPL were investigated. The anti‐inflammatory activity and acute toxicity of DPL long‐circulating, DPL and dexamethasone sodium phosphate injection (DSP) were evaluated with mice. The DPL long‐circulating systems were successfully prepared by film‐distributed extrusion methods. The experimental results showed that the DPL long‐circulating had uniform particle size and stable property. The DPL long‐circulating and DPL showed stronger anti‐inflammatory effect than DSP in an anti‐inflammatory test. Acute toxicity tests showed that DSP injection had lower toxicity than the DPL long‐circulating and DPL, which suggested that DPL long‐circulating and DPL had higher bioavailability with passive targeting efficacy of liposomes. The DPL long‐circulating formulation product can meet quality requirement. This formulation had stronger anti‐inflammatory effect and higher acute toxicity. |
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| Keywords: | dexamethasone palmitate long‐circulating liposome acute toxicity anti‐inflammatory |
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