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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

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

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Author(s):
Fachinetti, Naiara [1] ; Rigon, Roberta Balansin [1] ; Eloy, Josimar O. [1] ; Sato, Mariana Rillo [1] ; dos Santos, Karen Cristina [1] ; Chorilli, Marlus [1]
Total Authors: 6
Affiliation:
[1] UNESP Sao Paulo State Univ, Dept Drugs & Med, Sch Pharmaceut Sci, Campus Araraquara, Rodovia Araraquara Jau, Km 1, BR-14800903 Sao Paulo - Brazil
Total Affiliations: 1
Document type: Journal article
Source: AAPS PHARMSCITECH; v. 19, n. 3, p. 1401-1409, APR 2018.
Web of Science Citations: 6
Abstract

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. (AU)

FAPESP's process: 13/21500-1 - Solid lipid nanoparticles for incorporation of trans-resveratrol in the topical treatment of melanoma: in vitro and in vivo evaluation and the elucidation of the mechanism of uptake cellular
Grantee:Roberta Balansin Rigon
Support type: Scholarships in Brazil - Doctorate
FAPESP's process: 11/19018-1 - Evaluation of the potential of nanostructured lipid carriers for cutaneous administration of trans-resveratrol
Grantee:Naiara Fachinetti
Support type: Scholarships in Brazil - Scientific Initiation
FAPESP's process: 12/19568-4 - Evaluation of the potential of nanostructured lipid systems for cutaneous administration of trans-resveratrol
Grantee:Marlus Chorilli
Support type: Regular Research Grants
FAPESP's process: 11/16888-5 - Development and characterization of solid lipid nanoparticles for dermal administration of trans-resveratrol
Grantee:Roberta Balansin Rigon
Support type: Scholarships in Brazil - Master