Dual Nanostructured Lipid Carriers/Hydrogel System for Delivery of Curcumin for Topical Skin Applications

This work focuses on the development and evaluation of a dual nanostructured lipid carrier (NLC)/Carbopol^®-based hydrogel system as a potential transporter for the topical delivery of curcumin to the skin. Two populations of different sized negatively charged NLCs (P1, 70–90 nm and P2, 300–350 nm) were prepared and characterized by means of dynamic light scattering. NLCs presented an ovoid platelet shape confirmed by transmission electron microscopy techniques. Curcumin NLC entrapment efficiency and release profiles were assessed by HPLC (high pressure liquid chromatography) and spectrophotometric methods. Preservation and enhancement of curcumin (CUR) antioxidant activity in NLCs (up to 7-fold) was established and cell viability assays on fibroblasts and keratinocytes indicated that CUR-NLCs are non-cytotoxic for concentrations up to 10 μM and exhibited a moderate anti-migration/proliferation effect (20% gap reduction). CUR-NLCs were then embedded in a Carbopol^®-based hydrogel without disturbing the mechanical properties of the gel. Penetration studies on Franz diffusion cells over 24 h in CUR-NLCs and CUR-NLCs/gels demonstrated an accumulation of CUR in Strat-M^® membranes of 22% and 5%, respectively. All presented data support the use of this new dual CUR-NLC/hydrogel system as a promising candidate for adjuvant treatment in topical dermal applications.

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Chemicals:

Precirol^® ATO5 (gliceryl palmitostearate) and Labrafac^® lipophile WL 1349 (caprylic/capric triglycerides) were kindly provided by Gattefosse (Nanterre, France). Curcumin (CUR, purity ≥75% HPLC), Tween^® 80 (polyoxyethylene 20 sorbitan monooleate), poloxamer 407 (polyoxyethylene-polyoxypropylene copolymer), (±)-α-tocopherol (purity ≥ 75% HPLC), 2,2′-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS), potassium persulfate (K₂S₂O₈, purity ≥ 99%), triethanolamine (TEA, purity ≥ 99%), 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide (MTT), tert-butyl hydroperoxide (Luperox^®), 2′,7′-dichlorofluorescin diacetate (DCFH-DA) and Trolox (purity ≥ 98%) were purchased from Sigma-Aldrich (Saint-Quentin-Fallavier, France). Acetonitrile (ACN) and trifluoroacetic acid (TFA, purity ≥ 99%) were purchased from Sigma-Aldrich (Milan, Italy). Dichloromethane (DCM, purity ≥ 99.8%), ethanol (EtOH, purity ≥ 99.8%) and isopropanol (purity ≥ 98%) were purchased from VWR Chemicals (Fontenay-sous-Bois, France). Carbopol^® 980 NF (polyacrylic acid polymer crosslinked with allyl pentaerythritol) was kindly provided by Lubrizol (Rouen, France).

Calderon-Jacinto, R.; Matricardi, P.; Gueguen, V.; Pavon-Djavid, G.; Pauthe, E.; Rodriguez-Ruiz, V. Dual Nanostructured Lipid Carriers/Hydrogel System for Delivery of Curcumin for Topical Skin Applications. Biomolecules 2022, 12, 780. https://doi.org/10.3390/biom12060780