Abstract
Methotrexate (MTX) is a folic acid antagonist used as an effective drug to treat various kinds of cancers. However, MTX has limited use in cancer chemotherapy due to its adverse effects such as poor bioavailability, low specificity, drug resistance, and dose-dependent side effects. To improve lymphatic delivery and reduce toxicity of MTX, MTX-loaded nanoparticles (NPs) were prepared in the present study. NPs were prepared with double emulsion solvent evaporation method using poly(lactide-co-glycolide) (PLGA). NPs were assessed for size, encapsulation efficiency, morphology, Fourier-transform infrared spectroscopy, X-ray diffraction, and thermal characterization. In vitro release profiles and cytotoxicity of these NPs were also evaluated. Prepared NPs and free MTX were administered orally or intravenously (5 mg/kg as MTX) to rats to evaluate their pharmacokinetic characteristics and lymphatic delivery effects. Mean particle size and encapsulation efficiency of NPs were 163.7 ± 10.25 nm and 93.3 ± 0.5%, respectively. Prepared NPs showed a sustained release profile of MTX in vitro and may be effective to cancer cells. Area under the blood concentration-time curve, total clearance, half-life, and lymphatic targeting efficiency were significantly different (p < 0.05) between prepared NPs and free MTX. These results demonstrate that MTX-loaded PLGA NPs are good candidates for targeted delivery of MTX to the lymphatic system.
Highlights
Nanomedicines have recently become an object of great interest in the area of drug delivery systems
Between prepared NPs and free MTX. These results demonstrate that MTX-loaded PLGA NPs are good candidates for targeted delivery of MTX to the lymphatic system
These results suggest that prepared MTX-loaded PLGA NPs are effective for lymphatic delivery of MTX
Summary
Nanomedicines have recently become an object of great interest in the area of drug delivery systems. Nanoparticles (NPs) are tiny materials of nanometer scale and have unique properties in the body in relation to their size. NPs can have a relatively large loading capacity due to their high surface area-to-volume ratio [1]. NPs lead to improve therapeutic efficiency and decrease side effects [2]. These systems can reduce drug doses by preventing rapid degradation or metabolism of drug and increasing drug concentration in the target tissue [3,4]. Using the properties of NPs, various attempts to nanoparticulate drugs have continued from the past to the present. Drugs with many physicochemical barriers have been studied to overcome their limitations using nanocarrier drug delivery system
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