ABSTRACT
Objective: The main purpose of this work was to prepare tolnaftate (TOL) loaded nanostructured lipid carriers (NLCs), Evaluate its characteristics and in vitro release study. Methods: Tolnaftate loaded Nanostructured lipid carriers were prepared by the high shear homogenization method using different liquid lipids types (DERMAROL DCO® and DERMAROL CCT®) and concentrations, different concentration ratios of tween80® to span20® and different homogenization speeds. All the formulated nanoparticles were subjected to particle size (PS), zeta potential (ZP), polydispersity index (PI), drug entrapment efficiency (EE), Differential Scanning Calorimetry (DSC), Transmission Electron microscopy (TEM), release kinetics and in vitro release study was determined. Results: The results revealed that NLC dispersions had spherical shapes with an average size between 154.966±1.85 nm and 1078.4±103.02 nm. High entrapment efficiency was obtained with negatively charged zeta potential with PDI value ranging from 0.291±0.02 to 0.985±0.02. The release profiles of all formulations were characterized by a sustained release behavior over 24 h and the release rates increased as the amount of surfactant decreased. The release rate of TOL is expressed following the theoretical model by Higuchi. Conclusion: From this study, It can be concluded that NLCs are a good carrier for tolnaftate delivery
ABSTRACT
Objective: To prepare and optimize tilianin loaded solid lipid nanoparticles (T-SLNs), and investigate the physicochemical properties, absorption and transport behavour of T-SLNs in vitro. Methods: T-SLNs were prepared by high shear homogenization followed by ultrasonication and optimized by central composite design and response surface methodology. In the study, the physicochemical properties of T-SLNs including size, polydispersity (PDI), Zeta potential, shape, entrapment efficiency and release profile in vitro were investigated, the absorption and transport behavour of T-SLNs in Caco-2 cell model were also measured. Results: The optimum formulation of T-SLNs consisted of: drug/lipid of 0.11, soy lecithin/lipid of 1.26, and content of tween-80 was 5.05%. The prepared T-SLNs were spherical and uniform with the mean particle diameter at (86.40 ± 0.62) nm, PDI (0.165 ± 0.080) and Zeta potential of (-24.2 ± 0.6) mV, respectively. The average EE was (89.81 ± 1.07)%, and the release in vitro showed that tilianin was released about (98.72 ± 1.57)% in 48 h. Besides, the absorption and transport assays of T-SLNs in Caco-2 cells model indicated that T-SLNs had a higher absorption and transport than tilianin. Conclusion: The method of high shear homogenization followed by ultrasonication is suitable for T-SLNs preparation. The optimal T-SLNs have a smaller particle size and high EE. Moreover, in the same concentration of tilianin, the absorption and transport amounts of T-SLNs in Caco-2 cell model were higher than tilianin.
ABSTRACT
Aims: The aim of this study was to explore the practicability of preparation of solid lipid nanoparticles of Glyceryl monostearate containing Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide as model drugs. The physicochemical properties of the prepared formulae like particle size, drug entrapment efficiency, drug loading capacity, yield content and in-vitro drug release behavior were also measured. Methodology: Solid lipid nanoparticles loaded with three model lipophilic drugs were prepared by high shear hot homogenization method. The model drugs used are Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide. Glyceryl monostearate was used as lipid core; Tween 20 and Tween 80 were employed as surfactants and lecithin as co-surfactant. Many formulation parameters were controlled to obtain high quality nanoparticles. The prepared solid lipid nanoparticles were evaluated by different standard physical and imaging methods. The efficiency of drug release form prepared formulae was studied using in vitro technique with utilize of dialysis bag technique. The stability of prepared formulae was studied by thermal procedures and infrared spectroscopy. Results: The mean particle diameter measured by laser diffraction technique was (194.6±5.03 to 406.6±15.2 nm) for Dibenzoyl peroxide loaded solid lipid nanoparticles, (220±6.2 to 328.34±2.5) nm for Erythromycin loaded solid lipid nanoparticles and (227.3±2.5 to 480.6±24) nm for Triamcinolone acetonide loaded solid lipid nanoparticles. The entrapment efficiency and drug loading capacity, determined with ultraviolet spectroscopy, were 80.5±9.45% and 0.805±0.093%, for Dibenzoyl peroxide, 96±11.5 and 0.96±0.012 for Triamcinolone acetonide and 94.6±14.9 and 0.946±0.012 for Erythromycin base respectively. It was found that model drugs showed significant faster release patterns when compared with commercially available formulations and pure drugs (p˂0.05). Thermal analysis of prepared solid lipid nanoparticles gave indication of solubilization of drugs within lipid matrix. Fourier Transformation Infrared Spectroscopy (FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating no interaction between drugs and lipid matrix and being only dissolved in it. Electron microscope of scanning and transmission techniques indicated sphere form of prepared solid lipid nanoparticles with smooth surface with size below 100 nm. Conclusions: Solid lipid nanoparticles with small particle size have high encapsulation efficiency, and relatively high loading capacity for Dibenzoyl peroxide, Erythromycin base, and Triamcinolone acetonide as model drugs can be obtained by this method.