Comparative Study of Glyceryl Behenate or Polyoxyethylene 40 Stearate-Based Lipid Carriers for Trans-Resveratrol Delivery: Development, Characterization and Evaluation of the In Vitro Tyrosinase Inhibition
Trans-resveratrol (RSV) is a natural compound with several properties, such as the ability to inhibit the tyrosinase enzyme, with potential application as a skin-lightning agent and for the treatment of skin disorders associated with hyperpigmentation and melanogenesis. However, the drug faces several drawbacks which altogether limit its therapeutic application. Thus, drug loading into nanocarriers emerge as an alternative to circumvent these problems. Herein, nanostructured lipid carriers (NLCs) have been employed for RSV encapsulation, with comparison of two different lipids, glyceryl behenate (more hydrophobic), and polyoxyethylene 40 (PEG 40) stearate. PEG 40 stearate-containing NLCs presented smaller particle size and polydispersity compared with glyceryl behenate, attributed to better emulsification and nanoparticle formation, resulting in higher RSV encapsulation efficiency. Drug was loaded in both carriers as a molecular dispersion. Furthermore, the formulations had very low RSV release, which occurred due to the crystallinity degree of lipid matrix, in accordance with the DSC data. Moreover, RSV cytotoxicity against L-929 cells was not increased when loaded into nanocarriers. Interestingly, RSV-loaded formulation prepared with PEG-40 stearate resulted on greater tyrosinase inhibition than RSV solution and formulation containing glyceryl behenate, equivalent to 1.31 and 1.83 times higher, respectively, demonstrating that the incorporation of RSV into NLC allowed an enhanced tyrosinase inhibitory activity. Overall, the results obtained herein evidence potential for future in vivo evaluation of RSV-loaded NLCs.
Williams KA, Kolappswamy K, DeTolla LJ, Vucenik I. Effect of inositol hexaphosphate against UVB damage in HaCaT cells and skin carcinogenesis in SKH1 hairless mice. Comp Med. 2011;61:39–44.Google Scholar
Gokce EH, Korkmaz E, Dellera E, Sandri G, Cristina Bonferoni M, Ozer O. Resveratrol-loaded solid lipid nanoparticles versus nanostructured lipid carriers: evaluation of antioxidant potential for dermal applications. Int J Nanomedicine. 2012;7:1841–50. https://doi.org/10.2147/IJN.S29710.CrossRefGoogle Scholar
Cassano R, Ferrarelli T, Mauro MV, Cavalcanti P, Picci N, Trombino S. Preparation, characterization and in vitro activities evaluation of solid lipid nanoparticles based on PEG-40 stearate for antifungal drugs vaginal delivery. Drug Deliv. 2014;7544:1–10.CrossRefGoogle Scholar
Eloy JO, Petrilli R, Fernando J, Marcelo H, Antonio R, Palma J, et al. Biointerfaces co-loaded paclitaxel/rapamycin liposomes: development, characterization and in vitro and in vivo evaluation for breast cancer therapy. Colloids and Surfaces B Biointerfaces [Internet]. 2016;141:74–82. https://doi.org/10.1016/j.colsurfb.2016.01.032.CrossRefGoogle Scholar
Krause B, Mende M, Pötschke P, Petzold G. Dispersability and particle size distribution of CNTs in an aqueous surfactant dispersion as a function of ultrasonic treatment time. Carbon NY. 2010;48:2746–54.CrossRefGoogle Scholar
Omwoyo WN, Ogutu B, Oloo F, Swai H, Kalombo L, Melariri P, et al. Preparation, characterization, and optimization of primaquine-loaded solid lipid nanoparticles. Int J Nanomedicine. 2014;9:3865–74. https://doi.org/10.2147/IJN.S62630.Google Scholar
Sanna V, Siddiqui IA, Sechi M, Mukhtar H. Resveratrol-loaded nanoparticles based on poly(epsilon-caprolactone) and poly(d,l-lactic-co-glycolic acid)–poly(ethylene glycol) blend for prostate cancer treatment. Mol Pharm. 2013;10:3871–81. Available from: http://www.ncbi.nlm.nih.gov/pubmed/23968375CrossRefGoogle Scholar
Souza SD. A review of in vitro drug release test methods for nano-sized dosage forms. Adv Pharmaceutics. 2014.Google Scholar
Singh R, Lillard W. Nanoparticle-based targeted drug delivery. Exp Mol Pathol. 2009;86:215–23.CrossRefGoogle Scholar
Juère E, Florek J, Bouchoucha M, Jambhrunkar S, Wong KY, Popat A, et al. In vitro dissolution, cellular membrane permeability and anti-inflammatory response of resveratrol-encapsulated mesoporous silica nanoparticles. Mol Pharm [Internet]. 2017; acs.molpharmaceut.7b00529; https://doi.org/10.1021/acs.molpharmaceut.7b00529.
Costa P, Lobo JMS. Modelling and comparison of dissolution profile. Eur J Pharm Sci. 2001;13:123–33.CrossRefGoogle Scholar
Schmolka IR. Artificial skin. I. Preparation and properties treatment of burns. J Biomed Mater Res. 1972;6:571–82.CrossRefGoogle Scholar
Rodrigues F, Gaspar C, Palmeira-de-Oliveira A, Sarmento B, Helena Amaral M, Oliveira MB. Application of coffee silverskin in cosmetic formulations: physical/antioxidant stability studies and cytotoxicity effects. Drug Dev Ind Pharm [Internet]. 2015;0:1–8. https://doi.org/10.3109/03639045.2015.1035279.Google Scholar