Stabilization of retinol through incorporation into liposomes.
Chemical and photochemical processes during storage and preparation rapidly degrade retinol, the most active form of vitamin A. Therefore, the efficacy of incorporation into liposomes in order to modulate the kinetics of retinol degradation was investigated. Retinol was readily incorporated into multilamellar liposomes that were prepared from soybean phosphatidylcholine; the extent of the incorporation was 98.14 +/- 0.93% at pH 9.0 at a ratio of 0.01 : 1 (wt : wt) retinol : phospholipid. It was only marginally lower at higher retinol concentrations. The pH of the hydration buffer had a small effect. The incorporation efficiency ranged from 99.25 +/- 0.47% at pH 3 to 97.45 +/- 1.13% at pH 11. The time course of the retinol degradation in the aqueous solution in liposomes was compared to that of free retinol and free retinol with alpha-tocopherol under a variety of conditions of pH (3, 7, and 11), temperature (4, 25, 37, and 50 degrees ), and light exposure (dark, visible, and UV). The retinol that was incorporated into the liposomes degraded significantly slower than the free retinol or retinol with alpha-tocopherol at pH 7 and 11. At pH 3, where the free retinol degrades rapidly, the degradation kinetics were similar in liposomes and the presence of alpha-tocopherol. At pH 7.0 and 4 degrees in the light, for example, free aqueous retinol was completely degraded within 2 days, while only 20% of the retinol in the liposomes were degraded after 8 days. In general, the protective effect of the liposome incorporation was greater at low temperatures, at neutral and high pH, and in the dark. The results suggest that protection is greater in the solid, gel phase than in the fluid liquid crystalline phase lipids. These results indicate that the incorporation into liposomes can extend the shelf-life of retinol under a variety of conditions of temperature, pH, and ambient light conditions.
Lee
Seung-Cheol
SC
Department of Food Science and Biotechnology, Division of Life Sciences, Kyungnam University, Masan 631-701, Korea. sclee@kyungnam.ac.kr
Yuk
Hyun-Gyun
HG
Lee
Dong-Hoon
DH
Lee
Kyung-Eun
KE
Hwang
Yong-Il
YI
Ludescher
Richard D
RD
D004355:Drug Stability; D004356:Drug Storage; D005527:Food, Fortified / Q000032:analysis; D006801:Humans; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D008027:Light; D008081:Liposomes; D010713:Phosphatidylcholines; D013696:Temperature; D014466:Ultraviolet Rays; D014801:Vitamin A / Q000008:administration & dosage* / Q000737:chemistry* / Q000528:radiation effects
D008081:Liposomes; D010713:Phosphatidylcholines; D014801:Vitamin A