Investigation of the factors influencing the incorporation of clotrimazole in SLN and NLC prepared by hot high-pressure homogenization

被引:107
作者
Souto, E. B. [1 ]
Mueller, R. H. [1 ]
机构
[1] Free Univ Berlin, Dept Pharmaceut Technol Biotechnol & Qual Managem, D-12169 Berlin, Germany
关键词
clotrimazole; solid lipid nanoparticles (SLN); nanostructured lipid carriers (NLC); x-ray diffraction; differential scanning calorimetry (DSC);
D O I
10.1080/02652040500435295
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
Clotrimazole, a fungicidal effective for the local treatment of cutaneous and mucosal infections, was incorporated into solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC). The aim was to increase its dermal bioavailability and to control drug release, thereby potentially reducing its side effects. Prior to the release studies, the carrier was optimized and characterized by using different techniques. Laser diffractometry (LD), photon correlation spectroscopy (PCS) and scanning electron microscopy (SEM) indicated that SLN were spherical in shape with a mean size of similar to 400nm. Some aggregation phenomena occurred during preparation of SEM samples due to the lipid character of the carriers. No physico-chemical instability of the drug-loaded lipid nanoparticles was detected during 2 years of storage at different temperatures. X-ray and DSC results suggested that during storage time the drug remained molecularly dispersed in the lipid matrix. Drug associated to SLN and NLC in its crystal form could be excluded.
引用
收藏
页码:377 / 388
页数:12
相关论文
共 26 条
[1]  
BOISTELLE R, 1988, SURFACTANT SCI SERIE, P189
[2]   Effect of particle size on colloidal solid triglycerides [J].
Bunjes, H ;
Koch, MHJ ;
Westesen, K .
LANGMUIR, 2000, 16 (12) :5234-5241
[3]  
BUNJES H, 1998, SUBMICRON EMULSIONS, P175
[4]   Scanning electron microscopy and atomic force microscopy imaging of solid lipid nanoparticles derived from amphiphilic cyclodextrins [J].
Dubes, A ;
Parrot-Lopez, H ;
Abdelwahed, W ;
Degobert, G ;
Fessi, H ;
Shahgaldian, P ;
Coleman, AW .
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS, 2003, 55 (03) :279-282
[5]   Interfacial interactions between amphiphilic cyclodextrins and physiologically relevant cations [J].
Dubes, A ;
Parrot-Lopez, H ;
Shahgaldian, P ;
Coleman, AW .
JOURNAL OF COLLOID AND INTERFACE SCIENCE, 2003, 259 (01) :103-111
[6]   POLYMORPHIC BEHAVIOR OF SPRAYED LIPID MICROPELLETS AND ITS EVALUATION BY DIFFERENTIAL SCANNING CALORIMETRY AND SCANNING ELECTRON-MICROSCOPY [J].
ELDEM, T ;
SPEISER, P ;
ALTORFER, H .
PHARMACEUTICAL RESEARCH, 1991, 8 (02) :178-184
[7]   OPTIMIZATION OF SPRAY-DRIED AND SPRAY-CONGEALED LIPID MICROPELLETS AND CHARACTERIZATION OF THEIR SURFACE-MORPHOLOGY BY SCANNING ELECTRON-MICROSCOPY [J].
ELDEM, T ;
SPEISER, P ;
HINCAL, A .
PHARMACEUTICAL RESEARCH, 1991, 8 (01) :47-54
[8]  
GARTI N, 1988, SURFACTANT SCI SERIE, P267
[9]   Clotrimazole/betamethasone diproprionate: A review of costs and complications in the treatment of common cutaneous fungal infections [J].
Greenberg, HL ;
Shwayder, TA ;
Bieszk, N ;
Fivenson, DP .
PEDIATRIC DERMATOLOGY, 2002, 19 (01) :78-81
[10]   Preparation of solid lipid nanoparticles with clobetasol propionate by a novel solvent diffusion method in aqueous system and physicochemical characterization [J].
Hu, FQ ;
Yuan, H ;
Zhang, HH ;
Fang, M .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 2002, 239 (1-2) :121-128