Characterization and cytotoxicity of a benzocaine inclusion complex

Torres, Liliane Henrique; Carvalho, Mohana Zorkot; Melo, Patrı́cia da Silva; Paula, Eneida de; Saczk, Adelir Aparecida; Pinto, Luciana Rossini

doi:10.1007/s10847-018-0791-3

Cited by 10 publications

(6 citation statements)

References 22 publications

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“…When BZC was added, there was a slight decrease in this transition temperature (from 53.0 °C in NLC to 52.9 °CNLC BZC ) and enthalpy (from 190.8 to 164.7 J/g). These data also show that the fraction of BZC encapsulated in the NLC (96%, according to %EE) decreased the crystallinity of the lipid core (NLC BZC vs NLC), as observed previously, with other local anesthetics encapsulated in NLC. − The absence of the melting point of pure BZC in the NLC BZC sample is another indicator of BZC dissolution into the lipid matrix of the NLC.…”

Section: Resultssupporting

confidence: 78%

“…11 No replections from BZC were noticeable in the optimized NLC formulation sample (Figure 3D), and there was a loss in intensity (from the physical mixture to NLC BZC ) compatible with the insertion of BZC into the lipid matrix. 54 Small-angle neutron scattering has become a routine technique for the structural characterization of macromolecular assemblies of polymers, micelles, and even NLC 35 in the spatial range of a few to hundreds of nanometers. SANS measurements were performed to probe the structural organization of the optimized NLC, with and without benzocaine (Figure 4).…”

Section: Calorimetric X-ray Diffraction Small-angle Neutron Scatterin...mentioning

confidence: 99%

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Fresh Carrier for an Old Topical Local Anesthetic: Benzocaine in Nanostructured Lipid Carriers

Souza,

Rodrigues da Silva,

Ribeiro

et al. 2024

ACS Biomater. Sci. Eng.

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Nanostructured lipid carriers (NLC) have emerged as innovative drug delivery systems, offering distinct advantages over other lipid-based carriers, such as liposomes and solid lipid nanoparticles. Benzocaine (BZC), the oldest topical local anesthetic in use, undergoes metabolism by pseudocholinesterase, leading to the formation of p-aminobenzoic acid, a causative agent for allergic reactions associated with prolonged BZC usage. In order to mitigate adverse effects and enhance bioavailability, BZC was encapsulated within NLC. Utilizing a 2 3 factorial design, formulations comprising cetyl palmitate (solid lipid), propylene glycol monocaprylate (liquid lipid), and Pluronic F68 as surfactants were systematically prepared, with variations in the solid/liquid lipid mass ratios (60:40−80:20%), total lipid contents (15−25%), and BZC concentrations (1−3%). The optimized formulation underwent characterization by dynamic light scattering, differential scanning calorimetry, Raman imaging, X-ray diffraction, small-angle neutron scattering, nanotracking analysis, and transmission electron microscopy (TEM)/cryo-TEM, providing insights into the nanoparticle structure and the incorporation of BZC into its lipid matrix. NLC BZC exhibited a noteworthy encapsulation efficiency (%EE = 96%) and a 1 year stability when stored at 25 °C. In vitro kinetic studies and in vivo antinociceptive tests conducted in mice revealed that NLC BZC effectively sustained drug release for over 20 h and prolonged the anesthetic effect of BZC for up to 18 h. We therefore propose the use of NLC BZC to diminish the effective anesthetic concentration of benzocaine (from 20 to 3% or less), thus minimizing allergic reactions that follow the topical administration of this anesthetic and, potentially, paving the way for new routes of BZC administration in pain management.

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Section: Resultssupporting

confidence: 78%

Section: Calorimetric X-ray Diffraction Small-angle Neutron Scatterin...mentioning

confidence: 99%

Fresh Carrier for an Old Topical Local Anesthetic: Benzocaine in Nanostructured Lipid Carriers

Souza,

Rodrigues da Silva,

Ribeiro

et al. 2024

ACS Biomater. Sci. Eng.

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“…Being more acidic than water and coming into contact with alkaline hydroxides in aqueous solution at basic pH levels, thymol reacts with alkaline hydroxides to form salts or phenoxide ions, more stable than thymol itself (at neutral pH), due to the net effect of the resonance of the aromatic ring. The formation of thymol inclusion complexes with CDs determines a decrease in the enthalpy and an increase in the entropy of the system, thus reducing the free energy, which causes an increase in the stability of the complex. Although there are many factors that contribute to the complexation thermodynamics, the extent of favorable entropy change (data not shown) indicates that the desolvation process accompanying complex formation rather than conformational changes was related with enthalpic gain.…”

Section: Resultsmentioning

confidence: 99%

Thorough characterization and stability of HP‐β‐cyclodextrin thymol inclusion complexes prepared by microwave technology: A required approach to a successful application in food industry

et al. 2018

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“…The PXRD results of BZN and TIB revealed crystallographic patterns with sharp narrow characteristic peaks (Figure 7a,b) [35]. This cluster pattern was distinguishable for drugs in pure form and is indicative of crystal pattern [39]. However, the PXRD pattern of the optimized formulation clearly revealed reduction in intensity of incorporated drugs in the physical mixture (Figure 7c), [40].…”

Section: Pxrd Analysismentioning

confidence: 96%

Evaluating Novel Agarose-Based Buccal Gels Scaffold: Mucoadhesive and Pharmacokinetic Profiling in Healthy Volunteers

et al. 2022

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Agarose (AG) forms hydrocolloid in hot water and possesses a noteworthy gel strength. However, no reasonable scientific work on investigating the mucoadhesive character of AG has been reported. Therefore, the current study was designed to develop AG and carbopol (CP) based buccal gel scaffold for simultaneous release of benzocaine (BZN) and tibezonium iodide (TIB). Gels’ scaffold formulations (F1–F12) were prepared with varied concentrations (0.5–1.25% w/v) of AG and CP alone or their blends (AG-CP) using homogenization technique. The prepared formulations were characterized for solid-state, physicochemical, in vitro, ex vivo, and in vivo mucoadhesive studies in healthy volunteers. The results showed that mucoadhesive property of AG was concentration dependent but improved by incorporating CP in the scaffolds. The ex vivo mucoadhesive time reached >36 h when AG was used alone or blended with CP at 1% w/v concentration or above. The optimized formulation (F10) depicted >98% drugs release within 8 h and was also storage stable up to six months. The salivary concentration of BZN and TIB from formulation F10 yielded a Cmax value of 9.97 and 8.69 µg/mL at 2 and 6 h (tmax), respectively. In addition, the FTIR, PXRD, and DSC results confirmed the presence of no unwanted interaction among the ingredients. Importantly, the mucoadhesive study performed on healthy volunteers did not provoke any signs of inflammation, pain, or swelling. Clearly, it was found from the results that AG-CP scaffold provided better mucoadhesive properties in comparison to pure AG or CP. Conclusively, the developed AG based mucoadhesive drug delivery system could be considered a potential alternative for delivering drugs through the mucoadhesive buccal route.

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Characterization and cytotoxicity of a benzocaine inclusion complex

Cited by 10 publications

References 22 publications

Fresh Carrier for an Old Topical Local Anesthetic: Benzocaine in Nanostructured Lipid Carriers

Fresh Carrier for an Old Topical Local Anesthetic: Benzocaine in Nanostructured Lipid Carriers

Thorough characterization and stability of HP‐β‐cyclodextrin thymol inclusion complexes prepared by microwave technology: A required approach to a successful application in food industry

Evaluating Novel Agarose-Based Buccal Gels Scaffold: Mucoadhesive and Pharmacokinetic Profiling in Healthy Volunteers

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