Solid lipid nanoparticles for trans-resveratrol incorporation: development, physico-chemical characterization, stability study and in vitro release

• Grant number: 17/05566-3
• Support Opportunities: Scholarships in Brazil - Scientific Initiation
• Effective date (Start): September 01, 2017
• Effective date (End): December 31, 2018
• Field of knowledge: Health Sciences - Pharmacy - Pharmaceutical Technology
• Principal Investigator: Marlus Chorilli
• Grantee: Andressa Tardim Cruz
• Host Institution: Faculdade de Ciências Farmacêuticas (FCFAR). Universidade Estadual Paulista (UNESP). Campus de Araraquara. Araraquara , SP, Brazil
• Associated scholarship(s): 17/24365-9 - In vitro cutaneous permeation study of trans-resveratrol incorporated into solid lipid nanoparticles, BE.EP.IC

Abstract

Solid lipid nanoparticles (SLN) are dispersions formed by nanometric particles that have high physiological stability and a matrix composed of solid lipids. Drugs encapsulated in NLS present an increase stability, such as possibility of prolonged, controlled, and specific release of drugs, and another advantages over other release systems like reduced toxicity of the components, non-use of solvents organic production, large-scale production and sterilization facility, among others. However, one of the major problems found in the development of NLS is the instability for long periods of time; and drug expulsion from the lipid matrix during the storage period was reported. Trans-resveratrol (RES) is a substance naturally found in water, has low solubility in water and high membrane permeability. Although there are several studies demonstrating the benefits of RES for melanoma treatment, others demonstrate a low bioavailability of this oral substance in humans, which may be circumvented by its dermal administration. In this context, the aim of this work is to develop and study the stability of NLSs with RES after being prepared using different methodologies, including Ultra Turrax at 11,000 to 24,000 rpm or magnetic stirrer. After homogenates for particle size reduction, the pre-emulsion formed will be sonicated and different storage conditions will be evaluated, and their influence on the RES encapsulation efficiency and the stability of formulations prepared with the following components: stearic acid (5%), soybean phosphatidylcholine (1.2%), poloxamer 407 (0.1%), polysorbate (0.1%) and polysorbate 80 (3.5%), glycerin (0.15%), phenonip (0.75%), ethanol PA (1.25%), milli-Q water (sufficient quantity to reach the total amount of formulation) added or not of cetyltrimethylammonium bromide (0.45%). The formulations will be analyzed at the times 24 hours, 7, 15, 30, 60 and 90 days after the preparation. They will be stored in a refrigerator (4 ± 2° C) throughout the analysis period, and will be analyzed organoleptic characteristics, determination of pH, conductivity, the mean hydrodynamic diameter, and zeta potential. It is expected to see the influence of the NLS preparation technique on stability, encapsulation efficiency and on the release profile of RES. (AU)