Surface-Modified Multifunctional Thymol-Loaded Biodegradable Nanoparticles for Topical Acne Treatment

Abstract

The present work is focused on the development of novel surface-functionalized poly(lactic-co-glycolic acid) nanoparticles loaded with thymol (TH-NPs) for topical administration enhancing thymol anti-inflammatory, antioxidant and wound healing activities against acne. TH-NPs were prepared by solvent evaporation method using different surface functionalization strategies and obtaining suitable physicochemical parameters and a good short-term stability at 4 °C. Moreover, TH-NPs skin penetration and antioxidant activity were assessed in ex vivo pig skin models. Skin penetration of TH-NPs followed the follicular route, independently of the surface charge and they were able to enhance antioxidant capacity. Furthermore, antimicrobial activity against Cutibacterium acnes was evaluated in vitro by the suspension test showing improved antibacterial performance. Using human keratinocyte cells (HaCat), cytotoxicity, cellular uptake, antioxidant, anti-inflammatory and wound healing activities were studied. TH-NPs were non-toxic and efficiently internalized inside the cells. In addition, TH-NPs displayed significant anti-inflammatory, antioxidant and wound healing activities, which were highly influenced by TH-NPs surface modifications. Moreover, a synergic activity between TH-NPs and their surface functionalization was demonstrated. To conclude, surface-modified TH-NPs had proven to be suitable to be used as anti-inflammatory, antioxidant and wound healing agents, constituting a promising therapy for treating acne infection and associated inflammation.

Development of Peptide Targeted PLGA-PEGylated Nanoparticles Loading Licochalcone-A for Ocular Inflammation

“…As can be observed in Figure 3, Lico-A PLGA NPs were stable at 4 °C and 25 °C even after 3 months of storage. However, at 38 °C, the formulations were clearly unstable obtaining variations of the BS superior to 10% [55,56]. These results correlate with other obtained by previous authors using PLGA nanocarriers [43].…”

“…Although all of the formulations were very similar, as can be observed in Table 4, Moreover, release profiles of all the formulations were very similar, being able to release Lico-A within the first 24 h after their application. In addition, this release from biodegradable nanocarriers is usually governed by a diffusion process since it is much faster than the matrix degradation [55]. Release data were fitted to a hyperbola equation [60][61][62].…”

Investigations of pectin nanostructures for enhanced percutaneous delivery of fusidic acid

“…To examine in vitro the cytotoxicity of GBE‐PEC NS against HaCaT cells at varying concentrations from 1 to 3 mg/ml, an MTT assay was carried out with PBS serving as a control. The cell line was chosen since it has been utilized as a substitute for human keratinocytes in numerous cytotoxicity investigations of percutaneous drug formulations 52,53 . In comparison to the PBS control, GBE‐PEC NS displayed >85% cell viability over the entire concentration range studied, the findings (Figure 10) revealed that cytotoxicity was dose‐dependent and minimal under application‐relevant conditions.…”

Enhanced Transdermal Delivery of Pranoprofen Using a Thermo-Reversible Hydrogel Loaded with Lipid Nanocarriers for the Treatment of Local Inflammation

“…The short-term stability of the PF-NLCs-F127 hydrogel (Figure 6) did not detect signs of destabilization over 60 days at 25 • C since the BS profile revealed variations of less than ±10%, indicating that the formulation was stable [34,35].…”