Cytotoxicity of solid lipid nanoparticles and nanostructured lipid carriers containing the local anesthetic dibucaine designed for topical application

Barbosa, Raquel de Melo; Silva, C. M. G. da; Bella, T. S.; Araújo, Daniele Ribeiro de; Marcato, Priscyla D.; Durán, Nélson; Paula, Eneida de

doi:10.1088/1742-6596/429/1/012035

Cited by 32 publications

(38 citation statements)

References 33 publications

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“…Encapsulation of therapeutic agents is one of the most attractive areas in fashionable supramolecular host-guest chemistry and shows great potential in drug delivery. Materials used in encapsulation include liposomes (10,11), peptides (12), nanoparticles (13), chitosan (14,15), functional polymers (16), and host molecules such as cyclodextrins (17,18) and calix[n]arenes (6,(19)(20)(21)(22)(23).…”

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confidence: 99%

Benzocaine Complexation with p‐Sulfonic Acid Calix[n]arene: Experimental (¹H‐NMR) and Theoretical Approaches

et al. 2014

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The aim of this work was to study the interaction between the local anesthetic benzocaine and p-sulfonic acid calix[n]arenes using NMR and theoretical calculations and to assess the effects of complexation on cytotoxicity of benzocaine. The architectures of the complexes were proposed according to (1) H NMR data (Job plot, binding constants, and ROESY) indicating details on the insertion of benzocaine in the cavity of the calix[n]arenes. The proposed inclusion compounds were optimized using the PM3 semiempirical method, and the electronic plus nuclear repulsion energy contributions were performed at the DFT level using the PBE exchange/correlation functional and the 6-311G(d) basis set. The remarkable agreement between experimental and theoretical approaches adds support to their use in the structural characterization of the inclusion complexes. In vitro cytotoxic tests showed that complexation intensifies the intrinsic toxicity of benzocaine, possibly by increasing the water solubility of the anesthetic and favoring its partitioning inside of biomembranes.

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confidence: 99%

Benzocaine Complexation with p‐Sulfonic Acid Calix[n]arene: Experimental (¹H‐NMR) and Theoretical Approaches

et al. 2014

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“…Additionally, the safety behavior observed for XAN-NLC/LDC-PLC hydrogel was predictable, since NLC formulations were previously described as noncytotoxic for 3T3 and HaCat cells. 36,[46][47][48] Finally, the anesthesia duration was determined through tail-flick assay in mice. XAN-NLC/LDC-PLC exhibited an anesthetic effect two times higher than the control hydrogel (XAN/LDC-PLC) and four times higher than the commercially available cream.…”

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confidence: 99%

Nanohybrid hydrogels designed for transbuccal anesthesia

Ribeiro

Franz-Montan

Breitkreitz

et al. 2018

IJN

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BackgroundLocal anesthesia in dentistry is by far the most terrifying procedure for patients, causing treatment interruption. None of the commercially available topical formulations is effective in eliminating the pain and phobia associated to the needle insertion and injection.Materials and methodsIn this work we prepared a nanostructured lipid-biopolymer hydrogel for the sustained delivery of lidocaine–prilocaine (LDC-PLC) for transbuccal pre-anesthesia. The lipid was composed of optimized nanostructured lipid carriers (NLC) loaded with 5% LDC-PLC (NLC/LDC-PLC). The biopolymer counterpart was selected among alginate, xanthan (XAN), and chitosan matrices. The XAN-NLC hydrogel presented the most uniform aspect and pseudoplastic rheological profile, as required for topical use; therefore, it was selected for subsequent analyses. Accelerated stability tests under critical conditions (40°C; 75% relative humidity) were conducted for 6 months, in terms of drug content (mg/g), weight loss (%), and pH.ResultsIn vitro LDC-PLC release profile through Franz diffusion cells revealed a bimodal kinetics with a burst effect followed by the sustained release of both anesthetics, for 24 hours. Structural analyses (fourier transform infrared spectroscopy, differential scanning calorimetry and scanning electron microscopy) gave details on the molecular organization of the hybrid hydrogel, confirming the synergic interaction between the components. Safety and efficacy were evaluated through in vitro cell viability (3T3, HaCat, and VERO cells) and in vivo antinociceptive (tail-flick, in mice) tests, respectively. In comparison to a control hydrogel and the eutectic mixture of 5% LDC-PLC cream (EMLA®), the XAN-NLC/LDC-PLC hybrid hydrogel doubled and quadrupled the anesthetic effect (8 hours), respectively.ConclusionConsidering such exciting results, this multifaceted nanohybrid system is now ready to be further tested in clinical trials.

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“…The surface morphology and size of the blank and NLC/Co‐Q10 nanoparticles were observed under transmission electron microscopy. The samples were negatively stained with 2% uranyl acetate and dried after applying to a copper grid . The dried slides were observed under transmission electron microscope (LEO 906, 100 kv, Zeiss, Germany) operating at 100 kv.…”

Section: Methodsmentioning

confidence: 99%

Therapeutic Anti-Inflammatory Potential of Different Formulations Based on Coenzyme Q10-Loaded Nanostructured Lipid Carrier: In Vitro, Ex Vivo, and In Vivo Evaluations

Ahmadi¹,

Rostamizadeh

Modarresi‐Alam³

2018

Eur. J. Lipid Sci. Technol.

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An attempt is made to study skin anti‐inflammatory activity for different formulations of Co‐Q10 loaded nanostructured lipid carriers (NLC) including NLC, NLC‐based gel, and W/O cream. NLCs are prepared by a hot high speed homogenization method using cetylpalmitate as solid lipid, coconut oil as liquid lipid, and tween 80 as surfactant. NLCs are characterized by different techniques including dynamic light scattering, transmission electron microscopy, and FT‐IR. Stable formulation with a mean size range of 118.7 ± 6.9 nm and zeta potential of −29.1 ± 1.96 mV is developed. Drug loading content for NLC/Co‐Q10, NLC‐based gel, and W/O cream formulations is 7.945 ± 0.035%, 4.79 ± 0.052%, and 2.39 ±0.041%, respectively. All formulations show high entrapment efficiency (EE) (>96% w/w). The formulations are prepared and characterized in terms of rheology, pH, anti‐radical activity, ex vivo skin permeation, and in vivo anti‐inflammatory activity. A drug release study exhibits that the maximum attainable drug release after 48 h for NLC/Co‐Q10 is 11.94% versus 14.4% for NLC‐based gel and 41.56% for W/O cream. Ex vivo studies on rat skin reveals that Co‐Q10 contained in the W/O cream formulation penetrates into the stratum corneum more readily than that in the NLC/Co‐Q10 and NLC‐based gel formulations. In vivo studies of acute anti‐inflammatory activity of NLC‐based formulations show significant difference between inhibition effect of W/O cream and NLC/Co‐Q10 compared to betamethasone. Practical Applications: The findings indicate that formulation based on NLC/Co‐Q10 is suitable not only in skin penetration but also in dermatology. Anti‐inflammatory activity for different formulations of Co‐Q10 loaded NLC including NLC, NLC‐based gel, and W/O cream is investigated. All formulations show suitable physicochemical properties and high drug loading capacity for being used as dermatological formulations. The order of drug release after 48 h is NLC/Co‐Q10 < NLC‐based gel < W/O cream. In ex vivo study, the fastest penetration rate into the stratum corneum is obtained for W/O cream. W/O cream and NLC/Co‐Q10 formulations show significant acute anti‐inflammatory activity compared to betamethasone in in vivo study.

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Cytotoxicity of solid lipid nanoparticles and nanostructured lipid carriers containing the local anesthetic dibucaine designed for topical application

Cited by 32 publications

References 33 publications

Benzocaine Complexation with p‐Sulfonic Acid Calix[n]arene: Experimental (¹H‐NMR) and Theoretical Approaches

Benzocaine Complexation with p‐Sulfonic Acid Calix[n]arene: Experimental (¹H‐NMR) and Theoretical Approaches

Nanohybrid hydrogels designed for transbuccal anesthesia

Therapeutic Anti-Inflammatory Potential of Different Formulations Based on Coenzyme Q10-Loaded Nanostructured Lipid Carrier: In Vitro, Ex Vivo, and In Vivo Evaluations

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Cytotoxicity of solid lipid nanoparticles and nanostructured lipid carriers containing the local anesthetic dibucaine designed for topical application

Cited by 32 publications

References 33 publications

Benzocaine Complexation with p‐Sulfonic Acid Calix[n]arene: Experimental (1H‐NMR) and Theoretical Approaches

Benzocaine Complexation with p‐Sulfonic Acid Calix[n]arene: Experimental (1H‐NMR) and Theoretical Approaches

Nanohybrid hydrogels designed for transbuccal anesthesia

Therapeutic Anti-Inflammatory Potential of Different Formulations Based on Coenzyme Q10-Loaded Nanostructured Lipid Carrier: In Vitro, Ex Vivo, and In Vivo Evaluations

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Benzocaine Complexation with p‐Sulfonic Acid Calix[n]arene: Experimental (¹H‐NMR) and Theoretical Approaches

Benzocaine Complexation with p‐Sulfonic Acid Calix[n]arene: Experimental (¹H‐NMR) and Theoretical Approaches