Abstract
The aim of present study was to develop radiolabeled NPs to overcome the limitations of fluorescence with theranostic potential. Synthesis of PLGA-NPs loaded with technetium-99m was based on a Dean-Vortex-Bifurcation Mixer (DVBM) using an innovative microfluidic technique with high batch-to-batch reproducibility and tailored-made size of NPs. Eighteen different formulations were tested and characterized for particle size, zeta potential, polydispersity index, labeling efficiency, and in vitro stability. Overall, physical characterization by dynamic light scattering (DLS) showed an increase in particle size after radiolabeling probably due to the incorporation of the isotope into the PLGA-NPs shell. NPs of 60 nm (obtained by 5:1 PVA:PLGA ratio and 15 mL/min TFR with 99mTc included in PVA) had high labeling efficiency (94.20 ± 5.83%) and >80% stability after 24 h and showed optimal biodistribution in BALB/c mice. In conclusion, we confirmed the possibility of radiolabeling NPs with 99mTc using the microfluidics and provide best formulation for tumor targeting studies.
Highlights
The design of targeted drug delivery systems using nanomaterials has rapidly spread in medicine, due to the possibility of improving the targeting and release of drugs from these nano-systems, avoiding their premature biodegradation, off-target and systemic toxicity [1]
The polylactide-co-glycolic acid (PLGA) are polymeric NPs already approved by Food and Drug Administration (FDA) and European
dynamic light scattering (DLS) results confirmed that particle size is affected by both total flow ratio (TFR) and flow rate ratio (FRR) as already published by others [24]
Summary
The ideal delivery system should satisfy several requirements like biodegradability, biocompatibility, non-immunogenicity and non-toxicity in a biological system They should have the capability of a high load of drugs and administer them to the target with controlled release and distribution, with minimal losses and a prolonged release in the desired site [2,3]. Nanomaterials match these characteristics as they can be used to fabricate several types of nanoparticles (NPs), formulated with organic, inorganic, or hybrid core. The polylactide-co-glycolic acid (PLGA) are polymeric NPs already approved by Food and Drug Administration (FDA) and European
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