Neither too little nor too much: Finding the ideal proportion of excipients using confocal Raman and chemometrics

Mitsutake, Hery; Silva, Gustavo Henrique Rodrigues da; Breitkreitz, Márcia Cristina; Paula, Eneida de; Bordallo, H. N.

doi:10.1016/j.ejpb.2022.11.008

Cited by 2 publications

(4 citation statements)

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“…The determined ZP lied between |19.8 and 31.8| mV, what is compatible with good shelf stability. , Since BZC interacts differently with the solid and liquid lipids in the NLC core (see XRD, SANS, and Raman imaging data), we hypothesize that the more negative ZP values observed at higher lipid and BZC concentrations reflect the lipid displacement promoted by benzocaine. This results in a more superficial distribution of cetyl palmitate at the slipping plane of the NLC, as previously observed with the BZC analogue butamben …”

Section: Resultssupporting

confidence: 72%

“…The lamellar structures in the interior of the NLC agree with DSC and XRD data that revealed a decrease in the crystallinity of the lipid core (Figure ) and give clear evidence that BZC interacts differently with the solid and liquid lipids. Indeed, in a previous Raman imaging study with NLC composed of CP and propylene glycol monocaprylate, the interaction of butamben ( n -butyl- p -aminobenzoate) with the liquid lipid (but not CP) was demonstrated …”

Section: Resultsmentioning

confidence: 99%

“…This results in a more superficial distribution of cetyl palmitate at the slipping plane of the NLC, as previously observed with the BZC analogue butamben. 47 Based on the results for each response, the desirability region shown in Figure 1D was determined. The optimal formulation was composed of 25% TL, 60:40 SL/LL ratio, and 3% BZC plus 5% P68, and subsequent experiments were conducted with this selected composition.…”

Section: Resultsmentioning

confidence: 99%

“…Indeed, in a previous Raman imaging study with NLC composed of CP and propylene glycol monocaprylate, the interaction of butamben (n-butyl-p-aminobenzoate) with the liquid lipid (but not CP) was demonstrated. 47 Raman analyses were used to evaluate the miscibility of BZC with the NLC excipients in a preformulation. 59 Figure 5 shows the Raman spectrum of BZC and each NLC excipient.…”

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: 72%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

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

confidence: 99%

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