Evaluation of the digestibility of solid lipid nanoparticles of glyceryl dibehenate produced by two techniques: Ultrasonication and spray-flash evaporation

被引:15
作者
Jannin, Vincent [1 ]
Blas, Lucia [2 ]
Chevrier, Stepnie [1 ]
Miolane, Cedc [1 ]
Demarne, Frederic [1 ]
Spitzer, Denis [2 ]
机构
[1] Gattefosse SAS, 36 Chemin Genas, F-69804 St Priest, France
[2] UNISTRA, Lab NS3E, CNRS, UMR ISL 3208, 5 Rue Gen Cassagnou, F-68301 St Louis, France
关键词
Ultrasonication; SLN; Spray-flash evaporation; Lipolysis; Glyceryl dibehenate; DRUG-DELIVERY SYSTEMS; IN-VITRO DIGESTION; FORMULATIONS; RELEASE; TESTS; ESTABLISHMENT; PERFORMANCE; PARTICLES; LIPOLYSIS; IIIA;
D O I
10.1016/j.ejps.2017.09.049
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Objective: To evaluate the digestibility of Solid Lipid Nanoparticles (SLN) of glyceryl dibehenate prepared either with surfactants by ultrasonication or without surfactant by spray-flash evaporation. Methods: SLN of glyceryl dibehenate (Compritol (R) 888 ATO) were produced by two processes: (i) high-shear homogenization with a solution of water-soluble surfactants followed by ultrasonication (ii) and Spray-Flash Evaporation (SFE) of the pure lipid. The digestibility of these nanoparticles was then tested by in vitro lipolysis using a pH-stat apparatus and the assay of glycerides by gel phase chromatography. Results: SLN of glyceryl dibehenate prepared by ultrasonication exhibited a mean particle size of 180 nm and showed a limited digestion of the lipid excipient. SLN comprising only glyceryl dibehenate produced by SFE have a mean particle size between 235 and 411 nm depending on process parameters. These nanoparticles were not digested by lipases. The presence of surfactant at the lipid/water interface of the SLN seems to be mandatory to allow the adsorption of the lipase and degradation of glyceryl behenate. Conclusions: Glyceryl dibehenate as a solid particle - even as a SLN - is not digested by pancreatin during in vitro lipolysis test.
引用
收藏
页码:91 / 95
页数:5
相关论文
共 18 条
[1]   Size characterization of commercial micelles and microemulsions by Taylor dispersion analysis [J].
Chamieh, Joseph ;
Davanier, Florian ;
Jannin, Vincent ;
Demarne, Frederic ;
Cottet, Herve .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2015, 492 (1-2) :46-54
[2]   Solid lipid particles for oral delivery of peptide and protein drugs I - Elucidating the release mechanism of lysozyme during lipolysis [J].
Christophersen, P. C. ;
Zhang, L. ;
Yang, M. ;
Nielsen, H. Morck ;
Mullertz, A. ;
Mu, H. .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2013, 85 (03) :473-480
[3]   Does the commonly used pH-stat method with back titration really quantify the enzymatic digestibility of lipid drug delivery systems? A case study on solid lipid nanoparticles (SLN) [J].
Heider, Martha ;
Hause, Gerd ;
Maeder, Karsten .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2016, 109 :194-205
[4]   Influence of poloxamers on the dissolution performance and stability of controlled-release formulations containing Precirol® ATO 5 [J].
Jannin, V ;
Pochard, E ;
Chambin, O .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2006, 309 (1-2) :6-15
[5]   Development of self emulsifying lipid formulations of BCS class II drugs with low to medium lipophilicity [J].
Jannin, Vincent ;
Chevrier, Stephanie ;
Michenaud, Matthieu ;
Dumont, Camille ;
Belotti, Silvia ;
Chavant, Yann ;
Demarne, Frederic .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2015, 495 (01) :385-392
[6]   In vitro lipolysis tests on lipid nanoparticles: comparison between lipase/co-lipase and pancreatic extract [J].
Jannin, Vincent ;
Dellera, Eleonora ;
Chevrier, Stephanie ;
Chavant, Yann ;
Voutsinas, Christophe ;
Bonferoni, Cristina ;
Demarne, Frederic .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2015, 41 (10) :1582-1588
[7]   Continuous twin screw melt granulation of glyceryl behenate: Development of controlled release tramadol hydrochloride tablets for improved safety [J].
Keen, Justin M. ;
Foley, Connor J. ;
Hughey, Justin R. ;
Bennett, Ryan C. ;
Jannin, Vincent ;
Rosiaux, Yvonne ;
Marchaud, Delphine ;
McGinity, James W. .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2015, 487 (1-2) :72-80
[8]   Understanding the lipid-digestion processes in the GI tract before designing lipid-based drug-delivery systems [J].
N'Goma, Jean-Claude Bakala ;
Amara, Sawsan ;
Dridi, Kaouthar ;
Jannin, Vincent ;
Carriere, Frederic .
THERAPEUTIC DELIVERY, 2012, 3 (01) :105-124
[9]   Innovation of novel 'Tab in Tab' system for release modulation of milnacipran HCl: optimization, formulation and in vitro investigations [J].
Parejiya, Punit B. ;
Barot, Bhavesh S. ;
Patel, Hetal K. ;
Shelat, Pragna K. ;
Shukla, Arunkumar .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 2013, 39 (11) :1851-1863
[10]  
Patel K, 2015, J DRUG DELIV THER, V5, P19