ABSTRACT
Objective: Solid lipid nanoparticles (SLNs) are at the forefront of the rapidly developing field of nanotechnology with several potential applications in drug delivery and research. The aim of this study was to develop and characterize SLNs formulae of Terbinafine HCl (TFH) for topical drug delivery applications. Methods: SLNs were prepared using the solvent injection technique. Glyceryl Monostearate (GMS) served as the lipid base. Three stabilizers; Tween 80, Cremophor RH40, and Poloxamer 188, were used. The effect of stabilizer type and concentration, as well as the lipid concentration, were studied, factorial design of 32*21was applied. The prepared SLNs were characterized regarding their particle size, zeta potential, polydispersity index (PDI), entrapment efficiency percent (EE %), and physicochemical stability. The selected formulae were subjected to further investigations such as morphological studies, in vitro release studies, and Infrared (IR) spectroscopy. They were compared with the marketed cream Lamifen® in term of their antifungal activity against Candida albicans. Results: Lipid concentration, together with the type and concentration of stabilizer, appeared to be the main cornerstones which affect the formation of SLNs. Smaller particle size was observed when increasing the stabilizer concentration and decreasing the lipid concentration. Higher EE% was observed when increasing both the stabilizer and the lipid concentrations. Formulae (F6, F12 andF19) were selected as the most suitable SLNs with optimum particle size of 480.2±18.89, 458.6±12.45 and 246.7±10.5 nm, respectively as well as the highest EE% of 87.13±0.19, 93.69±0.7 and 95.06±0.25, respectively. In vitro microbiological screening of their antifungal activity showed significantly larger zones of inhibition of diameters 25.9±0.25, 25±0.35 and 24.67±0.36 mm, respectively in comparison with the marketed Lamifen® cream which showed a zone of 11.2±0.44 mm diameter. Conclusion: Applying SLNs containing TFH as topical antifungal preparations may be considered as a very promising option as they show good physicochemical characterization with high antifungal activity, which delineates them as a promising dosage form for topical antifungal treatment.
ABSTRACT
Objective: To evaluate the efficacy of combined ABZ and PZQ and their solid lipid nanoparticles in chemoprophylaxis of cystic echinococcosis (CE). Methods: ABZ and PZQ loaded solid lipid nanoparticles (SLNs) were prepared by high shear homogenization and microemulsion congealing techniques with some minor modification. Nanoparticles average size, polydispersity index (PDI), and particle size distribution were determined by scanning electron microscopy (SEM) and photon cor-relation spectroscopy. Forty females BALB/c were experimentally infected by proto-scoleces (PSC) and randomly divided into four equal groups of 10 mice. After the end of the 3 months treatment period and 2 months rest, mice were sacrificed and the peritoneal cavity was opened for removal, counting, measuring, and histological analysis of hydatid cyst. Results: The results indicated that ABZ and PZQ chemoprophylaxis treatment reduced the wet weight and size of developed cysts 77.3% and 79%, respectively. The corre-sponding result for the ABZ and PZQ loaded SLNs was 83%and 85%, respectively. Conclusions: This study for the first time demonstrated that ABZ and PZQ loaded SLNs is superior to free ABZ and PZQ for the chemoprophylaxis of CE in mice.
ABSTRACT
Objective To evaluate the efficacy of combined ABZ and PZQ and their solid lipid nanoparticles in chemoprophylaxis of cystic echinococcosis (CE). Methods ABZ and PZQ loaded solid lipid nanoparticles (SLNs) were prepared by high shear homogenization and microemulsion congealing techniques with some minor modification. Nanoparticles average size, polydispersity index (PDI), and particle size distribution were determined by scanning electron microscopy (SEM) and photon correlation spectroscopy. Forty females BALB/c were experimentally infected by protoscoleces (PSC) and randomly divided into four equal groups of 10 mice. After the end of the 3 months treatment period and 2 months rest, mice were sacrificed and the peritoneal cavity was opened for removal, counting, measuring, and histological analysis of hydatid cyst. Results The results indicated that ABZ and PZQ chemoprophylaxis treatment reduced the wet weight and size of developed cysts 77.3% and 79%, respectively. The corresponding result for the ABZ and PZQ loaded SLNs was 83% and 85%, respectively. Conclusions This study for the first time demonstrated that ABZ and PZQ loaded SLNs is superior to free ABZ and PZQ for the chemoprophylaxis of CE in mice.
ABSTRACT
AIM:Surfactants and their blend play important roles in the preparation of solid lipid nanoparticles (SLNs).In this study,four types of surfactant were employed to investigate the influence of the surfactants on properties of SLNs in the absence of model drugs thereby avoiding the interaction between the surfactant and the drug.METHODS:The physicochemical properties of the colloidal systems,such as mean particle size,distribution range and Zeta potential,were investigated by laser diffractometry and the DSC analysis was performed as well.RESULTS:It was found that ionic surfactants,such as sodium deoxycholate, increased the Zeta potential of nanoparticles leading to improve the physical stability of the system.But it showed obviously relative low emulsification efficiency in the preparation.Non-ionic emulsifier,especially Pluronic F-68, offered additional steric stabilization effect avoiding aggregation of the fine particles in the colloidal system.CONCLUSION:The formulation in the study for the first time combined four types of additives including ionic surfactant (sodium deoxycholate),non-ionic emulsifier (Pluronic F-68 and Tween-80),and lecithin to obtain favorably stable nanosuspension,which could stabilize for more than six months without creaming.
ABSTRACT
Objective The paclitaxel loaded solid lipid nanoparticles (PTX-SLNs) were prepared by an ultrasonic-dispersion emulsification technique. The stability of PTX-SLNs was investigated in this study. Methods The technology was preferenced by stability, Zeta potential, particle diameter, and entrapment efficiency as indexes. The doses of lipid materials and coemulsifier, the ultrasonic time, and the ultrasonic power were investigated in detail. Results The optimum prescriptions were definited by one-factor and orthogonal test. The adjuvant: glyceryl monostearate (100/150 mg), Fabaceous Lecithin (100 mg), coemulsifier Pluronic F68∶Tween 80 (2∶1). The samples were sonicated with an energy output of 300 W in 20 min after emulsified at (75?5) ℃. Conclusion The PTX-SLNs are successfully prepared and PTX-SLNs with high stability are fairly dispersed in colloidal solution. This technology has a nice prospect with safety and reliability.