Liposomes, a nanoscale carrier, plays an important role in the delivery of drug, affects the in vivo efficacy of drugs. In this paper, silymarin(SM)-loaded liposomes was optimized using the response surface method (RSM), with entrapment efficiency (EE%) as an index. The formulation was optimized as follow: lecithin (7.8mg/mL), SM/lecithin (1/26) and lecithin/cholesterol (10/1). The optimized SM liposomes had a high EE (96.58 ±3.06%), with a particle size of 290.3 ±10.5nm and a zeta potential of +22.98 ±1.73mV. In vitro release tests revealed that SM was released in a sustained-release manner, primarily via diffusion mechanism. In vitro cytotoxicity studies demonstrated that the prepared SM liposomes had stronger inhibitory effects than the model drug. Overall, these results indicate that this liposome system is suitable for intravenous delivery to enhance the antitumor effects of SM.
Lecithins , Liposomes , Particle Size , Silymarin , Silymarin/pharmacology , Silymarin/chemistry , Silymarin/administration & dosage , Humans , Lecithins/chemistry , Antineoplastic Agents/pharmacology , Antineoplastic Agents/chemistry , Antineoplastic Agents/administration & dosage , Drug Liberation , Cell Line, Tumor , Cell Survival/drug effects , Cholesterol/chemistry , Chemistry, Pharmaceutical , Drug Compounding
The aim of this study was to develop a gambogic acid-loaded mixed micelles (GA-M) system, using Kolliphor HS15 and lecithin, for enhancement of oral bioavailability. GA-M was prepared using the thin film hydration method, and particle size and zeta potential indexes were used to determine the optimized formulation was optimized with taking particle size, zeta potential as indexes. The optimal GA-M system had a mean particle size in the nanometer range (87.22 ± 0.68 nm) and zeta potential greater than 20 mV in magnitude (-21.63 ± 1.69 mV) at a 1:1 proportion of HS15: lecithin. Additionally, the carriers had a high entrapment efficiency (98.32 ± 3.52%) and drug loading (4.68 ± 0.17%). Furthermore, the in vitro GA release characteristics followed first-order kinetics, suggesting that the release of the molecule was achieved both by medium diffusion and structural erosion. Transport elucidation in Caco-2 cells demonstrated that the efflux ratio of encapsulated GA was dramatically decreased from 1.42 to 0.76, and pharmacokinetic studies showed that the oral bioavailability of GA-M was 2.3 times higher than that of free GA, indicating that HS15/lecithin mixed micelles could promote absorption in the gastrointestinal tract. Overall, these results present a micelle system suitable for oral delivery, with increased solubility and oral bioavailability of GA.
Lecithins , Micelles , Administration, Oral , Biological Availability , Caco-2 Cells , Drug Carriers/chemistry , Humans , Particle Size , Solubility , Xanthones
The fluoride-free fabrication of superhydrophobic materials for the separation of oil/water mixtures has received widespread attention because of frequent offshore oil exploration and chemical leakage. In recent years, oil/water separation materials, based on metal meshes, have drawn much attention, with significant advantages in terms of their high mechanical strength, easy availability, and long durability. However, it is still challenging to prepare superhydrophobic metal meshes with high-separation capacity, low costs, and high recyclability for dealing with oil-water separation. In this work, a superhydrophobic and super oleophilic stainless steel mesh (SSM) was successfully prepared by anchoring Fe2O3 nanoclusters (Fe2O3-NCs) on SSM via the in-situ flame synthesis method and followed by further modification with octadecyltrimethoxysilane (OTS). The as-prepared SSM with Fe2O3-NCs and OTS (OTS@Fe2O3-NCs@SSM) was confirmed by a field emission scanning electron microscope (FESEM), transmission electron microscope (TEM), energy dispersive spectrometer (EDS), X-ray photoelectron spectrometer (XPS), and X-ray diffractometer (XRD). The oil-water separation capacity of the sample was also measured. The results show that the interlaced and dense Fe2O3-NCs, composed of Fe2O3 nanoparticles, were uniformly coated on the surface of the SSM after the immerging-burning process. Additionally, a compact self-assembled OTS layer with low surface energy is coated on the surface of Fe2O3-NCs@SSM, leading to the formation of OTS@Fe2O3-NCs@SSM. The prepared OTS@Fe2O3-NCs@SSM shows excellent superhydrophobicity, with a water static contact angle of 151.3°. The separation efficiencies of OTS@Fe2O3-NCs@SSM for the mixtures of oil/water are all above 98.5%, except for corn oil/water (97.5%) because of its high viscosity. Moreover, the modified SSM exhibits excellent stability and recyclability. This work provides a facile approach for the preparation of superhydrophobic and super oleophilic metal meshes, which will lead to advancements in their large-scale applications on separating oil/water mixtures.
