鹽酸萬古霉素陽離子多囊脂質體的制備及質量考察_《中國修復重建外科雜志》

作者：

楊杜明 ^1,2 , 徐永清 ¹ , 李福兵 ¹ , 劉華 ¹ , 何曉清 ¹

1 成都軍區昆明總醫院骨科全軍創傷骨科研究所（昆明，650032）;;
2昆明醫科大學研究生部;

關鍵詞：

鹽酸萬古霉素陽離子多囊脂質體復乳法正交設計

DOI：

10.7507/1002-1892.20130106

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目的制備鹽酸萬古霉素陽離子多囊脂質體（multivesicular liposome，MVL）并對其質量進行考察。方法以復乳法制備鹽酸萬古霉素陽離子MVL；制備萬古霉素儲備液，建立萬古霉素的體外分析方法，并對方法的專屬性、精密度及回吸收率進行評估；采用反相高效液相色譜分析法測定萬古霉素藥物含量、包封率和體外釋放特性；以包封率為主要考察指標，單因素篩選和正交設計優化工藝和處方；光鏡和透射電鏡下觀察脂質體形態；激光散射法測定脂質體的粒徑和Zeta電位；動態分析法考察脂質體體外穩定性。結果建立了反相高效液相色譜分析法測定鹽酸萬古霉素陽離子MVL中萬古霉素含量的方法，該方法簡便可行，各項方法學符合要求；確定了最優的制備工藝及處方。以最優工藝和處方制備的鹽酸萬古霉素陽離子MVL外觀呈圓形，粒徑均一，平均粒徑為 3.3 μm，平均包封率為24.9%，平均Zeta電位為24.53 mV；37℃溫度下以生理鹽水為釋放介質，264 h釋放藥物約為90.5%。將新鮮制備的鹽酸萬古霉素陽離子MVL放置于4℃冰箱中保存1個月，脂質體穩定性良好。結論以復乳法制備的鹽酸萬古霉素陽離子MVL外觀良好，包封率高，穩定性好，具有良好的緩釋效應。

引用本文： 楊杜明,徐永清,李福兵,劉華,何曉清. 鹽酸萬古霉素陽離子多囊脂質體的制備及質量考察. 中國修復重建外科雜志, 2013, 27(4): 443-448. doi: 10.7507/1002-1892.20130106 復制

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2.	Costerton JW, Stewart PS, Greenberg EP. Bacterial biofilms: a common cause of persistent infections. Science, 1999, 284(5418): 1318-1322.
3.	Kim S, Turker MS, Chie Y, et al. Preparation of multivesicular liposomes. Biochim Biophys Acta, 1983, 728(3): 339-348.
4.	Mantripragada S. A lipid based depot (DepoFoaml technology) for sustained release drug delivery. Prog Lipid Res, 2002, 41(5): 392-406.
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6.	Kim HJ, Gias M, Jones MN. The adsorption of cationic liposomes to Staphylococcus aureus biofilms. Colloids Surf A Physicochem Eng Asp, 1999, 149(1-3): 561-570.
7.	Ye Q, Asheman J, Stevenson M, et al. DepoFoam technology a vehicle for controlled delivery of protein and peptide drugs. J Control Release, 2000, 64(1-3): 155-156.
8.	Taylor G, Kellaway IW, Steven J. Drug entrapment and release from multilamellar and reverse phase evaporation liposomes. Int J Pharm, 1990, 58(1): 49-55.
9.	New RRC. Influence of liposome characteristics on their properties and fate//Philippot JR, Schuber F. Liposomes as tools in basic research and industry. Boca Raton: CRC Press, 1995: 3-20.
10.	張淼, 于葉玲, 唐星. 阿糖胞苷多囊脂質體的制備及體外釋放度考察. 沈陽藥科大學學報, 2009, 26(1): 1-5.
11.	肖超菊, 齊憲榮, 艾尼瓦爾, 等. 順鉑緩釋多囊脂質體的制備和體外釋放性能研究. 藥學學報, 2003, 38(2): 133-137.
12.	馬濤, 尚北城, 徐貴麗, 等. 鹽酸萬古霉素陽離子脂質體的制備及其性質研究. 廣東藥學院報, 2010, 26(6): 551-555.

1. Sutherland IW. The biofilm matrix: an immobilized but dynamic microbial environment. Trends Microbiol, 2001, 9(5): 222-227.
2. Costerton JW, Stewart PS, Greenberg EP. Bacterial biofilms: a common cause of persistent infections. Science, 1999, 284(5418): 1318-1322.
3. Kim S, Turker MS, Chie Y, et al. Preparation of multivesicular liposomes. Biochim Biophys Acta, 1983, 728(3): 339-348.
4. Mantripragada S. A lipid based depot (DepoFoaml technology) for sustained release drug delivery. Prog Lipid Res, 2002, 41(5): 392-406.
5. Tamilvanan S, Venkateshan N, Ludwig A. The potential of lipid—and polymer-based drug delivery carriers for eradicating biofilm consortia on device-related nosoeomial infections. J Control Release, 2008, 128(1): 20-22.
6. Kim HJ, Gias M, Jones MN. The adsorption of cationic liposomes to Staphylococcus aureus biofilms. Colloids Surf A Physicochem Eng Asp, 1999, 149(1-3): 561-570.
7. Ye Q, Asheman J, Stevenson M, et al. DepoFoam technology a vehicle for controlled delivery of protein and peptide drugs. J Control Release, 2000, 64(1-3): 155-156.
8. Taylor G, Kellaway IW, Steven J. Drug entrapment and release from multilamellar and reverse phase evaporation liposomes. Int J Pharm, 1990, 58(1): 49-55.
9. New RRC. Influence of liposome characteristics on their properties and fate//Philippot JR, Schuber F. Liposomes as tools in basic research and industry. Boca Raton: CRC Press, 1995: 3-20.
10. 張淼, 于葉玲, 唐星. 阿糖胞苷多囊脂質體的制備及體外釋放度考察. 沈陽藥科大學學報, 2009, 26(1): 1-5.
11. 肖超菊, 齊憲榮, 艾尼瓦爾, 等. 順鉑緩釋多囊脂質體的制備和體外釋放性能研究. 藥學學報, 2003, 38(2): 133-137.
12. 馬濤, 尚北城, 徐貴麗, 等. 鹽酸萬古霉素陽離子脂質體的制備及其性質研究. 廣東藥學院報, 2010, 26(6): 551-555.

《中國修復重建外科雜志》

鹽酸萬古霉素陽離子多囊脂質體的制備及質量考察

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《中國修復重建外科雜志》

鹽酸萬古霉素陽離子多囊脂質體的制備及質量考察

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