(+)-Limonene 1,2-Epoxide-Loaded SLNs: Evaluation of Drug Release, Antioxidant Activity, and Cytotoxicity in an HaCaT Cell Line

Abstract

In this work, we developed a solid lipid nanoparticle (SLN) formulation with (+)-limonene 1,2-epoxide and glycerol monostearate (Lim-SLNs), stabilized with Poloxamer® 188 in aqueous dispersion to modify the release profile of the loaded monoterpene derivative. We also evaluated the role of SLNs in lipid peroxidation and cytotoxicity in a spontaneously transformed aneuploid immortal keratinocyte cell line from adult human skin (the HaCaT cell line). For the cell viability assay, the colorimetric 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay was used. Lim-SLNs with a loading capacity and encapsulation efficiency of 0.39% and 63%, respectively, were produced by high pressure homogenization. A mean particle size of 194 ± 3.4 nm and polydispersity index of 0.244 were recorded for the loaded Lim-SLNs, as compared to 203 ± 1.5 nm (PI 0.213) for the non-loaded (blank) SLNs. The loading of the monoterpene derivative into glycerol monostearate SLNs fitted into the zero-order kinetics, and ameliorated both lipid peroxidation and cytotoxicity in a keratinocyte cell line. A promising formulation for antioxidant and anti-tumoral activities is here proposed.

Perillaldehyde 1,2-epoxide Loaded SLN-Tailored mAb: Production, Physicochemical Characterization and In Vitro Cytotoxicity Profile in MCF-7 Cell Lines

“…The capacity of cPa-SLN to neutralize ROS was also confirmed using the DPPH test, and as expected, was shown to be concentration-dependent ( Table 2). The absorbance decay of the sample test was correlated with the absorbance decay of the control test, resulting in the percentage scavenging of free radicals translated as the antioxidant activity [23]. For the positive control (BHT), 78.11% scavenging of DPPH radicals was recorded at the highest-tested concentration (6.0 µg/mL); similar results were previously reported [23,33].…”

“…The encapsulation efficiency (EE) of perillaldehyde 1,2-epoxide in cPa-SLN was determined as an indirect measure of the amount of drug quantified in supernatant [23]. Briefly, cPa-SLN was firstly ultra-centrifuged for 1 h at 100,000 g in a Beckman Optima™ Ultracentrifuge (Optima™ XL, Indianapolis, IN, USA) and the quantification of perillaldehyde 1,2-epoxide, determined in the supernatant in a UV spectrophotometer Shimadzu UV-1601 (Shimadzu Italy, Cornaredo, Italy), at 245 nm.…”

In Vitro Characterization, Modelling, and Antioxidant Properties of Polyphenon-60 from Green Tea in Eudragit S100-2 Chitosan Microspheres

“…Differences were shown to be statistically significant. For the positive control (BHT) 78.11% scavenging of DPPH radical was recorded at the highest tested concentration (6.0 µg/mL) [33,34]. For the Ch-PP60 8:1 , the linear regression of R 2 = 0.9941 (y = 4.2743x -1.45) was obtained and the IC 50 calculated as 212.3 µg/mL, which confirms the cross-linking of chitosan with glutaraldehyde did not compromise the antioxidant activity of catechin.…”

“…The release profile of epigallocatechin gallate (EGCG) from non-coated microspheres (Ch-PP60 8:1 ) and Eudragit S-100 coated microspheres (S100Ch-PP60) formulations were compared over the pH range from 1.2 (simulated gastric fluid) in acid buffer solution for 2 h, to pH 4.5 (simulated duodenum) for another 2 h, to pH 7.4 (simulated distal ileum and colon) for the remaining 20 h. The capacity of S100Ch-PP60 to neutralize reactive oxygen species (ROS) was evaluated using the DPPH scavenging assay, which was shown to be concentration dependent. The absorbance decay of the control test was compared with the recorded absorbance decay of Ch-PP60 8:1 versus S100Ch-PP60, resulting in the percentage scavenging of free radicals translated as the antioxidant activity (Table 3) [33]. Differences were shown to be statistically significant.…”

Ocular Cell Lines and Genotoxicity Assessment

“…Aging is a major risk factor for the onset of several chronic diseases, and any structural changes may end up in the loss of capacities, including vision. Besides, DNA is particularly sensitive to reactive oxygen species (ROS); these can be neutralized using nutraceuticals with antioxidant properties [11][12][13][14][15][16][17][18][19][20][21][22][23][24][25], which protect DNA, promote its repair, and reduce the risk of age-related diseases. Single-cell gel (SCG) electrophoresis is a sensitive genotoxicological test that evaluates DNA damage in individual cells and enables the quantification of tape breaks [26][27][28].…”