Characterization of Articaine-Loaded Poly(ε-caprolactone) Nanocapsules and Solid Lipid Nanoparticles in Hydrogels for Topical Formulations

Abstract

This work describes the development of poly-ε-caprolactone nanocapsules (PCL-NC) and solid lipid nanoparticles (SLN) aiming delivery for articaine (ATC), in order to improve its chemical stability in semi-solid preparations looking forward their use for skin delivery. The nanoparticles were characterized by size, polydispersity index, and pH. Cellular viability was evaluated using the MTT test and the in vitro release kinetics was determined using a two-compartment model. The hydrogels with nanoparticle suspensions were characterized considering their rheological aspects and in vitro permeation across artificial membranes. Colloidal stability was satisfactory, since the formulations did not present major alterations during 120 days. High ATC encapsulation was achieved (78% for PCL-NC and 65% for SLN). The release profile of PCL-NC-ATC was slower, compared to the free molecule and SLN-ATC. MTT experiments showed the nanosystems were capable to increase cellular viability compared with free ATC. The hydrogels showed good consistency, homogeneity, and stability and presented pseudoplastic behavior with thixotropy, improving drug efficacy in clinical applications. The gel based on PCL-NC showed faster onset of activity and flux of 35.68 ± 1.98 μg/cm2/h, which then continued for up to 8 h. This study opens up prospects for employment of nanoparticulate systems for modified release of ATC.

Potential of mucoadhesive nanocapsules in drug release and toxicology in zebrafish

“…The drug release profile is vitally important in terms of effective therapy, providing information on release mechanisms and interaction between pharmaceuticals and nanocarriers [ 25 ]. The Fig 3 shows the release profiles of BENZ encapsulated in NPs and NPMAs, at room temperature (25°C) as a function of time.…”

“…Mathematical modeling was employed to elucidate the drug release from the nanoparticle systems. The Baker-Lonsdale model has been used previously by our group to evaluate the results of release curves involving nanoparticles [ 24 , 25 , 27 ]. Linear regression showed correlation coefficient ( r ) values of 0.978 and 0.988, and release constant ( k ) values of 4.24822 x 10 −5 (± 2.83661 x 10 −6 ) min -1 and 6.65378x 10 −5 (± 4.27674 x 10 −6 ) min -1 , for NPs and NPMAs, respectively.…”

“…The size distribution was given by the polydispersity index. Results were expressed as the average of three determinations [ 24 , 25 ].…”

“…The colloidal stability of the nanoparticles (NP) and NPMA suspensions was followed over time using measurements of particle size, polydispersity index, and zeta potential. The stability trials were continued for a period of 60 days, during which the formulations were stored at 25°C [ 25 ].…”

Nanohybrid hydrogels designed for transbuccal anesthesia

“…For the hybrid hydrogel, NLC formulations replaced the water used for dissolution of XAN. 26 The proportion of NLC/LDC-PLC and XAN in the hydrogel was 1:1 (w/w). In all types of prepared hydrogels, the final concentration of LDC-PLC was 25 mg/g.…”