Preparation and Crystal Modification of Ibuprofen-Loaded Solid Lipid Microparticles

Abstract

Abstract: An emulsion-congealing technique is used to prepare solid lipid microparticles (SLM) containing ibuprofen with glyceryl behenate, tripalmitin and beewax as excipients. The difference of the solubility parameters between the excipients and ibuprofen are used to analyze their compatibility. Both the solubility parameter analysis and the experimental results show that glyceryl behenate is the best among the three excipients. The solid particles disperse well in aqueous phase when the drug loading reaches 10% (relative to lipid only). Glycerides exhibit marked polymorphism and their rapid rates of crystallization accelerate the formation of metastable crystal modification. The metastable crystal modification characterizes high drug loading capacity but less stability. Increasing the content of lipophilic drug in a lipid matrix facilitates the transformation of excipients to more stable polymorphic forms.

Key words: solid lipid microparticles, crystal modification, solubility parameter, drug loading capacity, ibuprofen

摘要： An emulsion-congealing technique is used to prepare solid lipid microparticles (SLM) containing ibuprofen with glyceryl behenate, tripalmitin and beewax as excipients. The difference of the solubility parameters between the excipients and ibuprofen are used to analyze their compatibility. Both the solubility parameter analysis and the experimental results show that glyceryl behenate is the best among the three excipients. The solid particles disperse well in aqueous phase when the drug loading reaches 10% (relative to lipid only). Glycerides exhibit marked polymorphism and their rapid rates of crystallization accelerate the formation of metastable crystal modification. The metastable crystal modification characterizes high drug loading capacity but less stability. Increasing the content of lipophilic drug in a lipid matrix facilitates the transformation of excipients to more stable polymorphic forms.

关键词: solid lipid microparticles;crystal modification;solubility parameter;drug loading capacity;ibuprofen

LONGChunxia, ZHANGLijuan, QIANYu. Preparation and Crystal Modification of Ibuprofen-Loaded Solid Lipid Microparticles[J]. .

龙春霞, 章莉娟, 钱宇. 布洛芬固体脂质微颗粒的制备及其晶体构型研究[J]. CIESC Journal.

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Preparation and Crystal Modification of Ibuprofen-Loaded Solid Lipid Microparticles

布洛芬固体脂质微颗粒的制备及其晶体构型研究

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