Miconazole nitrate (MIC) is an antifungal drug used for treatment of superficial fungal infections. However, it has low skin permeability. Hence, the objective of this study was to prepare miconazole nitrate using Transfersomes to overcome the barrier function of the skin. MIC Transfersomes were prepared using a thin lipid film hydration technique. The prepared Transfersomes were evaluated with respect to entrapment efficiency (EE%), particle size, and quantity of in vitro drug released to obtain an optimized formulation. The optimized formulation of MIC Transfersomes was incorporated into a Carbapol 934 gel base which was evaluated in comparison with a marketed product (Daktarin® cream 2%) for drug content, pH, spreadability, viscosity, in vitro permeation, and in vitro and in vivo antifungal activity. The prepared MIC Transfersomes had a high EE% ranging from (67.98 ± 0.66%) to (91.47 ± 1.85%), with small particle sizes ranging from (63.5 ± 0.604 nm) to (84.5 ± 0.684 nm). The in vitro release study suggested that there was an inverse relationship between EE% and in vitro release. The kinetic analysis of all release profiles was found to follow Higuchi’s diffusion model. All independent variables had a significant effect on the dependent variables (p-values < 0.05). The prepared MIC transfersomal gel showed higher antifungal activity than Daktarin® cream 2%. Therefore, miconazole nitrate in the form of Transfersomes has the ability to penetrate the skin, overcoming the stratum corneum barrier.
Liver cancer is considered one of the deadliest diseases with one of the highest disease burdens worldwide. Among the different types of liver cancer, hepatocellular carcinoma is considered to be the most common type. Multiple conventional approaches are being used in treating hepatocellular carcinoma. Focusing on drug treatment, regular agents in conventional forms fail to achieve the intended clinical outcomes. In order to improve the treatment outcomes, utilizing nanoparticles—specifically lipid based nanoparticles—are considered to be one of the most promising approaches being set in motion. Multiple forms of lipid based nanoparticles exist including liposomes, solid lipid nanoparticles, nanostructured lipid carriers, microemulsion, nanoemulsion, phytosomes, lipid coated nanoparticles, and nanoassemblies. Multiple approaches are used to enhance the tumor uptake as well tumor specificity such as intratumoral injection, passive targeting, active targeting, and stimuli responsive nanoparticles. In this review, the effect of utilizing lipidic nanoparticles is being discussed as well as the different tumor uptake enhancement techniques used. Graphical Abstract
Objectives: The study aimed to prepare carbamazepine in solid lipid nanoparticle form (CBZ-SLN) in order to enhance its anticonvulsant effect. Method: Eight formulations of CBZ-SLNs were prepared by homogenization and ultra-sonication techniques. Results: The prepared CBZ-SLN showed a high entrapment efficiency% (39.66 ± 2.42%–71.91 ± 1.21%), a small particle size (45.11 ± 6.72–760.7 ± 5.25 nm), and a negative zeta potential (from −21.5 ± 1.02 to −38.4 ± 1.32 mv). The in vitro release study showed the slow release of CBZ from SLNs compared to CBZ aqueous dispersion (p < 0.05). The infrared spectroscopy and the thermal analysis revealed the compatibility of the drug with other ingredients and the presence of drug in the more soluble amorphous estate, respectively. The in vivo study on mice revealed that the CBZ-SLN had a higher anticonvulsant efficacy than CBZ aqueous dispersion after a lethal and chronic dose of pentylenetetrazole (PTZ) (p < 0.05). The histopathological examination of the hippocampus revealed a decrease in the percentage of degeneration in mice treated with the CBZ-SLN compared to the PTZ and CBZ groups. Conclusion: CBZ can be formulated as SLN with higher anticonvulsant activity than free CBZ aqueous dispersion.
Paclitaxel (PTX) is an anticancer drug having poor aqueous solubility and low bioavailability. Formulation of PTX into Nanostructure lipid carriers (NLC) could be a potential way to enhance PTX aqueous solubility and bioavailability hence increases efficacy and decreases side effects. Eight PTX-NLC formulae were prepared using homogenization-ultrasonication technique. Characterization of the nanoparticles was done by transmission electron microscopy and by measurement of particle size, poly dispersibility index and zeta potential. Encapsulation efficiency, drug loading, and In Vitro release were measured. Particle size ranged between 172.8 ± 0.8 to 378.2 ± 1.8 nm and zeta potential between -18.6 ± 0.4 to -28.1 ± 1.2 mV. High EE and DL were obtained due to incorporation of liquid lipid and the In Vitro release showed prolonged time dependent release compared to Taxol ® . NLC-3 had the best results among the eight prepared formulae. In Vitro cytotoxicity of NLC-3 was evaluated on MCF-7 cell line and compared to pure PTX powder and Taxol ® . These findings show that NLC is a potential carrier to improve efficacy and enhance PTX delivery.
Drug absorption from the gastrointestinal tract (GIT) is one of the major problems affecting the bioavailability of orally absorbed drugs. This work aims to enhance Fexofenadine HCl oral bioavailability in vivo, the drug used for allergic rhinitis. In this study, novel spray-dried lactose-based enhanced in situ forming vesicles were prepared using different absorption enhancer by the slurry method. Full factorial design was used to obtain an optimized formulation, while central composite design was used to develop economic, environment-friendly analysis method of Fexofenadine HCl in plasma of rabbits. The optimized formulation containing Capryol 90 as absorption enhancer has a mean particle size 202.6 ± 3.9 nm and zeta potential −31.6 ± 0.9 mV. It achieved high entrapment efficiency of the drug 73.7 ± 1.7% and rapid Q3h release reaches 71.5 ± 2.7%. The design-optimized HPLC assay method in rabbit plasma could separate Fexofenadine HCl from endogenous plasma compounds in less than 3.7 min. The pharmacokinetic study and the pharmacological effect of the fexofenadine-loaded optimized formulation showed a significant increase in blood concentration and significantly higher activity against compound 48/80 induced systemic anaphylaxis-like reactions in mice. Therefore, enhanced in situ forming vesicles were effective nanocarriers for the entrapment and delivery of Fexofenadine HCl.
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