Lipid nanocarriers for dermal delivery of lutein: Preparation, characterization, stability and performance

• Published in: International journal of pharmaceutics 2011-07, Vol.414 (1), p.267-275
• Main Authors: Mitri, Khalil, Shegokar, Ranjita, Gohla, Sven, Anselmi, Cecilia, Müller, Rainer H.
• Format: Article
• Language: English
• Subjects: absorption; Administration, Cutaneous; Administration, Topical; Animals; Antioxidant; antioxidants; Antioxidants - chemistry; Biological and medical sciences; blue light; cellulose; corn oil; Dermal delivery; Drug Carriers - analysis; Drug Carriers - chemistry; Drug Compounding; Drug Delivery Systems; Drug Stability; ears; Emulsions; erythema; Excipients - chemistry; General pharmacology; Glucans - chemistry; homogenization; irradiation; lipid content; Lipids - chemistry; Lutein; Lutein - analysis; Lutein - chemistry; Medical sciences; Membranes, Artificial; nanocarriers; nanoemulsions; nanoparticles; Nanoparticles - analysis; Nanoparticles - chemistry; Nanostructured lipid carriers; Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Photo stability; Skin; Solid lipid nanoparticles; Solubility; Surface-Active Agents - chemistry; Swine; temperature; topical application; Triglycerides - chemistry; water potential; zeta potential
• ISSN: 0378-5173; 1873-3476
• DOI: 10.1016/j.ijpharm.2011.05.008

Topical application of lutein as an innovative antioxidant, anti-stress and blue light filter, which is able to protect skin from photo damage, has got a special cosmetic and pharmaceutical interest in the last decade. Lutein is poorly soluble, and was therefore incorporated into nanocarriers for dermal delivery: solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC) and a nanoemulsion (NE). Nanocarriers were produced by high pressure homogenization. The mean particle size was in the range of about 150 nm to maximum 350 nm, it decreased with increasing oil content of the carriers. The zeta potential in water was in the range −40 to −63 mV, being in agreement with the good short term stability at room temperature monitored for one month. In vitro release was studied using a membrane free model. Highest release in 24 h was observed for the nanoemulsion (19.5%), lowest release (0.4%) for the SLN. Release profiles were biphasic (lipid nanoparticles) or triphasic (NE). In vitro penetration study with a cellulose membrane showed in agreement highest values for the NE (60% in 24 h), distinctly lower values for the solid nanocarriers SLN and NLC (8–19%), lowest values for lutein powder (5%). Permeation studies with fresh pig ear skin showed that no (SLN, NLC) or very little lutein (0.4% after 24 h) permeated, that means the active remains in the skin and is not systemically absorbed. The nanocarriers were able to protect lutein against UV degradation. In SLN, only 0.06% degradation was observed after irradiation with 10 MED (Minimal Erythema Dose), in NLC 6–8%, compared to 14% in the NE, and to 50% as lutein powder suspended in corn oil. Based on size, stability and release/permeation data, and considering the chemical protection of the lutein prior to its absorption into the skin, the lipid nanoparticles are potential dermal nanocarriers for lutein.