Beclomethasone-Loaded Lipidic Nanocarriers for Pulmonary Drug Delivery: Preparation, Characterization and In Vitro Drug Release

被引:38
作者
Jaafar-Maalej, Chiraz [1 ,2 ]
Andrieu, Veronique [3 ,4 ]
Elaissari, Abdelhannid [1 ,2 ]
Fessi, Hatem [1 ,2 ]
机构
[1] Univ Lyon, F-69622 Villeurbanne, France
[2] CNRS, Lab Automat & Genie Procedes, UMR 5007, F-69622 Villeurbanne, France
[3] Fac Med Marseille, CNRS IRD, URMITE UMR 6236, F-13385 Marseille 05, France
[4] Fac Pharm Marseille, Dept Pharm Galen, F-13385 Marseille 05, France
关键词
High-Shear Homogenization; Lipid Nanoparticles; Beclomethasone Dipropionate; Pulmonary Drug Delivery; Aerosol; Nebulization; SOLVENT DIFFUSION METHOD; NANOPARTICLES SLN; TOPICAL DELIVERY; PHYSICOCHEMICAL CHARACTERIZATION; LIPOSOME AEROSOL; BINARY-MIXTURES; CARRIER SYSTEM; AQUEOUS SYSTEM; SOLID LIPIDS; OIL CONTENT;
D O I
10.1166/jnn.2011.3119
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The purpose of this research paper was the development of lipid nanoparticles (LN) formulation suitable for beclomethasone dipropionate (BDP) administration via the pulmonary route. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) were prepared by high-shear homogenization method; the effects of process and formulation parameters on nanoparticles characteristics were investigated. LN were characterized in terms of morphology, size, encapsulation efficiency, in vitro drug release and aerosol aerodynamic properties. Nano-sized BDP-loaded LN with high entrapment efficiency values reaching 99% were successfully obtained. Application of in vitro drug release data to the Higuchi kinetic equation indicated a diffusion-controlled release from the lipidic matrix. Aerosolisation and subsequent cascade impaction measurements proved that SLN and NLC were efficiently nebulized yielding aerosols of a suitable particle size for BDP deep lung delivery. Results demonstrate that LN are promising nebulized carriers for BDP opening the way for lipophilic drug-targeting strategies by nebulization.
引用
收藏
页码:1841 / 1851
页数:11
相关论文
共 68 条
[1]  
Ahlin Pegi, 1998, Acta Pharmaceutica (Zagreb), V48, P259
[2]  
[Anonymous], 2014, [No title captured], P5236
[3]   Experimental study of the GAS process for producing microparticles of beclomethasone-17,21-dipropionate suitable for pulmonary delivery [J].
Bakhbakhi, Y ;
Charpentier, PA ;
Rohani, S .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2006, 309 (1-2) :71-80
[4]   Pulmonary drug delivery with aerosolizable nanoparticles in an ex vivo lung model [J].
Beck-Broichsitter, Moritz ;
Gauss, Julia ;
Packhaeuser, Claudia B. ;
Lahnstein, Kerstin ;
Schmehl, Thomas ;
Seeger, Werner ;
Kissel, Thomas ;
Gessler, Tobias .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2009, 367 (1-2) :169-178
[5]   Solid Lipid Nanoparticles as Insulin Inhalation Carriers for Enhanced Pulmonary Delivery [J].
Bi, Ru ;
Shao, Wei ;
Wang, Qun ;
Zhang, Na .
JOURNAL OF BIOMEDICAL NANOTECHNOLOGY, 2009, 5 (01) :84-92
[6]   Nano-emulsion formulation using spontaneous emulsification:: solvent, oil and surfactant optimisation [J].
Bouchemal, K ;
Briançon, S ;
Perrier, E ;
Fessi, H .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2004, 280 (1-2) :241-251
[7]   An investigation of some of the factors influencing the jet nebulisation of liposomes [J].
Bridges, PA ;
Taylor, KMG .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2000, 204 (1-2) :69-79
[8]   Characterization of indomethacin-loaded lipid nanoparticles by differential scanning calorimetry [J].
Castelli, F ;
Puglia, C ;
Sarpietro, MG ;
Rizza, L ;
Bonina, F .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2005, 304 (1-2) :231-238
[9]   Nebulization of biodegradable nanoparticles: impact of nebulizer technology and nanoparticle characteristics on aerosol features [J].
Dailey, LA ;
Schmehl, T ;
Gessler, T ;
Wittmar, M ;
Grimminger, F ;
Seeger, W ;
Kissel, T .
JOURNAL OF CONTROLLED RELEASE, 2003, 86 (01) :131-144
[10]   Nebulisation of rehydrated freeze-dried beclomethasone dipropionate liposomes [J].
Darwis, Y ;
Kellaway, IW .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2001, 215 (1-2) :113-121