Solid lipid nanoparticles optimized by 22 factorial design for skin administration: Cytotoxicity in NIH3T3 fibroblasts

Rigon, Roberta Balansin; Gonçalez, Maíra Lima; Severino, Patrícia; Alves, Dilson Amancio; Santana, Maria Helena Andrade; Souto, Eliana B.; Chorilli, Marlus

doi:10.1016/j.colsurfb.2018.07.065

Cited by 57 publications

(32 citation statements)

References 23 publications

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“…Sucupira oil-loaded NLC were produced by hot HPH technique which, besides the advantages of smaller particle sizes and higher loading capacity for lipophilic bioactives, the appropriate combination of lipids and surfactants will have to be found. Experimental factorial design is well-established as a standard approach to reach the most suitable parameters allowing the production of stable sucupira oil-loaded NLC formulations [40,49,[62][63][64][65][66]. Factorial design sets independent variables, either quantitative or qualitative factors, at given levels and evaluates them in a predefined number of experiments to understand their direct effect on the dependent variables and to determine if some factor interaction occurs.…”

Section: Resultsmentioning

confidence: 99%

“…Aiming to maximize the experimental efficiency with a minimum number of experiments to optimize the sucupira oil-loaded NLC produced by HPH, a full factorial design approach gathering all the possible combinations between the factors and their levels was applied. A 2 2 factorial design consisting of two factors, each one set at 2-levels [49], was used to evaluate surfactant (TPGS) and solid lipid (Kollivax ® GMS II) concentrations influence on the produced NLC. As dependent variables, mean particle size, PI and ZP were considered.…”

Section: Experimental Factorial Designmentioning

confidence: 99%

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Sucupira Oil-Loaded Nanostructured Lipid Carriers (NLC): Lipid Screening, Factorial Design, Release Profile, and Cytotoxicity

et al. 2020

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Essential oils are odorant liquid oily products consisting of a complex mixture of volatile compounds obtained from a plant raw material. They have been increasingly proven to act as potential natural agents in the treatment of several human conditions, including diabetes mellitus (DM). DM is a metabolic disorder characterized by chronic hyperglycemia closely related to carbohydrate, protein and fat metabolism disturbances. In order to explore novel approaches for the management of DM our group proposes the encapsulation of sucupira essential oil, obtained from the fruits of the Brazilian plants of the genus Pterodon, in nanostructured lipid carriers (NLCs), a second generation of lipid nanoparticles which act as new controlled drug delivery system (DDS). Encapsulation was performed by hot high-pressure homogenization (HPH) technique and the samples were then analyzed by dynamic light scattering (DLS) for mean average size and polydispersity index (PI) and by electrophoretic light scattering (ELS) for zeta potential (ZP), immediately after production and after 24 h of storage at 4 °C. An optimal sucupira-loaded NLC was found to consist of 0.5% (m/V) sucupira oil, 4.5% (m/V) of Kollivax® GMS II and 1.425% (m/V) of TPGS (formulation no. 6) characterized by a mean particle size ranging from 148.1 ± 0.9815 nm (0 h) to 159.3 ± 9.539 nm (at 24 h), a PI from 0.274 ± 0.029 (0 h) to 0.305 ± 0.028 (24 h) and a ZP from −0.00236 ± 0.147 mV (at 0 h) to 0.125 ± 0.162 (at 24 h). The encapsulation efficiency and loading capacity were 99.98% and 9.6%, respectively. The optimized formulation followed a modified release profile fitting the first order kinetics, over a period of 8 h. In vitro cytotoxicity studies were performed against Caco-2 cell lines, for which the cell viability above 90% confirmed the non-cytotoxic profile of both blank and sucupira oil-loaded NLC.

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Section: Resultsmentioning

confidence: 99%

Section: Experimental Factorial Designmentioning

confidence: 99%

Sucupira Oil-Loaded Nanostructured Lipid Carriers (NLC): Lipid Screening, Factorial Design, Release Profile, and Cytotoxicity

et al. 2020

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“…Consumables for cell culture were obtained from Sigma Chemical Co. (St. Louis, MO, USA). For the 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) assay [54], cells were incubated in 96-well plates (0.1 × 10 6 cells/mL, 100 µL/well in culture medium) for 24 h. Solutions of SLNs (blank) and Lim-SLNs in dimethyl sulfoxide (DMSO 0.7%) at increasing concentrations (1, 2, 5, and 10 µg/mL) were prepared in fetal bovine serum (FBS)-free culture medium, added to each well, and then incubated for more 72 h at 37 • C in a 5% CO 2 atmosphere. A solution of DMSO 1% was set as the negative control and doxorubicin at 100 µg/mL as the positive control (doxorubicin: purity > 98%; Sigma Chemical Co., St. Louis, MO, USA).…”

Section: Cell Culture and Mtt Assaymentioning

confidence: 99%

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

Souto

Zielińska

Souto

et al. 2020

IJMS

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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.

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“…(Figure 1). Cell viability above 70 wt% were recorded (91.12 wt% for non-loaded and 89.45 wt% for BZP3-loaded NCs), which demonstrated the NCs to be noncytotoxic [26][27][28]. No statistical difference was observed using the ANOVA test.…”

Section: Resultsmentioning

confidence: 85%

Development, Cytotoxicity and Eye Irritation Profile of a New Sunscreen Formulation Based on Benzophenone-3-poly(ε-caprolactone) Nanocapsules

Barbosa

Nascimento

Bani

et al. 2019

Toxics

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The objective of this work was to characterize the toxicological profile of a newly developed sunscreen formulation based on polymeric nanocapsules (NCs) loading benzophenone-3 (BZP3). NCs composed of poly(ε-caprolactone) carrot oil and Pluronic® F68 were produced by emulsification-diffusion method. Their mean particle size (Z-Ave) ranged from 280 to 420 nm, polydispersity index (PDI) was below 0.37, while zeta potential (ZP) reached about |+11 mV|. No cytotoxic effects were observed in L929 fibroblast cell line for the blank (i.e., non-loaded) NCs and BZP3-loaded NCs (BZP3-NCs). The semi-solid sunscreen formulation was stable over time (centrifugation testing) and exhibited non-Newtonian pseudoplastic behavior, which is typical of products for topical application onto the skin. The sun protection factor (SPF) value reached 8.84, when incorporating BZP3-NCs (SPF of 8.64) into the semi-solid formulation. A synergistic effect was also observed when combining the formulation ingredients of nanocapsules, i.e., SPF of carrot oil was 6.82, blank NCs was 6.84, and BZP3-loaded NCs was 8.64. From the hen’s egg-chorioallantoic membrane test (HET-CAM) test, the non-irritation profile of the developed formulations could also be confirmed. The obtained results show a promising use of poly(ε-caprolactone) nanocapsules to be loaded with lipophilic sunscreens as benzophenone-3.

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Solid lipid nanoparticles optimized by 22 factorial design for skin administration: Cytotoxicity in NIH3T3 fibroblasts

Cited by 57 publications

References 23 publications

Sucupira Oil-Loaded Nanostructured Lipid Carriers (NLC): Lipid Screening, Factorial Design, Release Profile, and Cytotoxicity

Sucupira Oil-Loaded Nanostructured Lipid Carriers (NLC): Lipid Screening, Factorial Design, Release Profile, and Cytotoxicity

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

Development, Cytotoxicity and Eye Irritation Profile of a New Sunscreen Formulation Based on Benzophenone-3-poly(ε-caprolactone) Nanocapsules

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