Supercritical fluid precipitation of ketoprofen in novel structured lipid carriers for enhanced mucosal delivery - a comparison with solid lipid particles

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• 作者：V.S.S. Gonç ; alves^a ; ^b ; ^c ; A.A. Matias^a ; ^b ; S. Rodrí ; guez-Rojo^c ; I.D. Nogueira^d ; C.M.M. Duarte^a ; ^b ; ^{cduarte@ibet.pt" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Structured lipid carriers ; Glyceryl monooleate ; Particles from gas saturated solutions® ; (PGSS® ; ) ; Supercritical fluids ; Ketoprofen ; Mucosal drug delivery
• 刊名：International Journal of Pharmaceutics
• 出版年：2015
• 出版时间：10 November 2015
• 年：2015
• 卷：495
• 期：1
• 页码：302-311
• 全文大小：1568 K

文摘

Structured lipid carriers based on mixture of solid lipids with liquid lipids are the second generation of solid lipid particles, offering the advantage of improved drug loading capacity and higher storage stability. In this study, structured lipid carriers were successfully prepared for the first time by precipitation from gas saturated solutions. Glyceryl monooleate (GMO), a liquid glycerolipid, was selected in this work to be incorporated into three solid glycerolipids with hydrophilic-lipophilic balance (HLB) ranging from 1 to 13, namely Gelucire 43/01™, Geleol™ and Gelucire 50/13™. In general, microparticles with a irregular porous morphology and a wide particle size distribution were obtained. The HLB of the individual glycerolipids might be a relevant parameter to take into account during the processing of solid:liquid lipid blends. As expected, the addition of a liquid lipid into a solid lipid matrix led to increased stability of the lipid carriers, with no significant modifications in their melting enthalpy after 6 months of storage. Additionally, Gelucire 43/01™:GMO particles were produced with different mass ratios and loaded with ketoprofen. The drug loading capacity of the structured lipid carriers increased as the GMO content in the particles increased, achieving a maximum encapsulation efficiency of 97% for the 3:1 mass ratio. Moreover, structured lipid carriers presented an immediate release of ketoprofen from its matrix with higher permeation through a mucous-membrane model, while solid lipid particles present a controlled release of the drug with less permeation capacity.