2021
DOI: 10.1038/s41598-021-99743-6
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A pre-formulation study of tetracaine loaded in optimized nanostructured lipid carriers

Abstract: Tetracaine (TTC) is a local anesthetic broadly used for topical and spinal blockade, despite its systemic toxicity. Encapsulation in nanostructured lipid carriers (NLC) may prolong TTC delivery at the site of injection, reducing such toxicity. This work reports the development of NLC loading 4% TTC. Structural properties and encapsulation efficiency (%EE > 63%) guided the selection of three pre-formulations of different lipid composition, through a 23 factorial design of experiments (DOE). DLS and TEM analy… Show more

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Cited by 18 publications
(5 citation statements)
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“…FE-SEM images of NLC/CAN and NLC control showed that both formulations presented nanoparticles with spherical morphology and with well-defined contours, as expected for this type of system ( Figure 4 ). In addition, the images revealed spherical monodisperse distributed nanoparticles, compatible with the morphology of NLC composed of synthetic and traditional lipids excipients ( Ribeiro et al., 2016 ; Calixto et al., 2021 ; Castro et al., 2021 ; Moura et al., 2021 ).…”
Section: Resultssupporting
confidence: 56%
“…FE-SEM images of NLC/CAN and NLC control showed that both formulations presented nanoparticles with spherical morphology and with well-defined contours, as expected for this type of system ( Figure 4 ). In addition, the images revealed spherical monodisperse distributed nanoparticles, compatible with the morphology of NLC composed of synthetic and traditional lipids excipients ( Ribeiro et al., 2016 ; Calixto et al., 2021 ; Castro et al., 2021 ; Moura et al., 2021 ).…”
Section: Resultssupporting
confidence: 56%
“…MM showed three sharp peaks at 2,848.39, 2,915.88, and 2,954.45 cm −1 , attributed to asymmetric, symmetric stretching of C-H bonds on −CH 2 and C-H bond asymmetric stretching on −CH 3 groups respectively. Another relevant sharp peak was found at 1731.8 cm −1 , corresponding to ester carbonyl stretching vibrations ( Castro et al, 2021 ). Finally, both 3D meshes showed a complex broad peak between 1,150 and 900 cm −1 , from overlapping P188, HPMC, and Chi peaks in that band of the spectrum, and broadband between 3,000 and 3,500 cm −1 from O-H and N-H vibrations in HPMC and Chi.…”
Section: Resultsmentioning
confidence: 99%
“…In the preformulation phase, physiochemical properties and the compatibility of the drug with excipients of the formulation are regulating the nano-system behavioural selected for the final formulation design. Preformulation studies are conducted to create an appropriate dosage form by establishing the pharmacokinetics and pharmacodynamic profile parameters [79,80]. Moreover, the dissolution profile, polymorphic forms, the pharmacokinetics of the drug, and its bioavailability, details on the drug's deterioration process, undesirable drug-related conditions, and pharmacodynamic effects are also an important part of preformulation studies which are provided by physicochemical properties of the drug.…”
Section: Preformulation Studies For Nano-based Therapeuticsmentioning
confidence: 99%