Using Chitosan-Coated Polymeric Nanoparticles-Thermosensitive Hydrogels in association with Limonene as Skin Drug Delivery Strategy

Abstract

Topical delivery of local anesthetics (LAs) is commonly used to decrease painful sensations, block pain throughout procedures, and alleviate pain after surgery. Dermal and/or transdermal delivery of LAs has other advantages, such as sustained drug delivery and decreased systemic adverse effects. This study reports the development of poly(D,L-lactide-co-glycolide) (PLGA) nanoparticles coated with chitosan for the sustained release and topicality of benzocaine (BZC) and topical delivery. BZC PLGA nanoparticles or nonencapsulated drugs were further incorporated into Poloxamer hydrogels (Pluronic™ F-127). The nanoparticles showed a mean diameter of 380 ± 4 nm, positive zeta potential after coating with chitosan ( 23.3 ± 1.7 mV), and high encapsulation efficiency ( 96.7 ± 0.02 % ). Cellular viability greater than 70% for both fibroblasts and keratinocytes was observed after treatment with nanoparticles, which is in accordance with the preconized guidelines for biomedical devices and delivery systems. Both the nanoparticles and hydrogels were able to modulate BZC delivery and increase drug permeation when compared to the nonencapsulated drug. Furthermore, the incorporation of limonene into hydrogels containing BZC-loaded nanoparticles increased the BZC permeation rates. Non-Newtonian and pseudoplastic behaviors were observed for all hydrogel nanoformulations with or without nanoparticles. These results demonstrate that the hydrogel-nanoparticle hybrids could be a promising delivery system for prolonged local anesthetic therapy.

Thermo-Responsive Gel Containing Hydroxytyrosol-Chitosan Nanoparticles (Hyt@tgel) Counteracts the Increase of Osteoarthritis Biomarkers in Human Chondrocytes

“…As shown in Figure 2 A, the addition of different concentrations of Hyt-NPs (1, 5, and 10 mg) did not significantly affect the Hyt@tgel gelation temperature, suggesting that hydrogel structure organization was maintained after nanoparticles dispersion. These results are in agreement with previous studies at the same Pluronic concentrations [ 48 , 49 ]. The gelation time of the Hyt@tgel at 35 °C was slightly increased by Hyt NPs incorporation ( Figure 2 B).…”

Tocopherol succinate‐loaded ethosomal gel synthesized by cold method technique: Deeper biophysical characterizations for translational application on human skin

“…In this method, the aqueous phase was added dropwise carefully into the nonaqueous phase to produce ethosomes 13,14 . Then, the size of developed ethosomal vesicles was further reduced by sonicating at RT, Nano sized vesicles are more stable and showed good release behavior from the developed formulation 17,40,3 . TSEG6 was used for further in‐vitro (e.g., physical characterizations.…”

Fabrication of Ethosomes Containing Tocopherol Acetate to Enhance Transdermal Permeation: In Vitro and Ex Vivo Characterizations

“…Suspended NPs were characterized for their average PS and electrostatic potential of charge, which are important features for stability studies [ 33 , 34 ]. The PS and ZP of the dH 2 O diluted TA-5 formulation were assessed by dynamic light scattering (DLS) using a Zeta Sizer Nano ZS90, Malvern, UK at 25 °C.…”

“…The drug entrapment efficiency calculated how much amount of the drug was entrapped into developed spherical vesicles. The % EE was calculated by simple indirect analysis technique [ 23 , 33 , 34 ]. First, 1 mL ethosomal suspension was centrifuged for 30 min to obtain a clear supernatant solution.…”