Tocosome: Novel drug delivery system containing phospholipids and tocopheryl phosphates

Abstract

The potential of two derivatives of vitamin E, i.e. α-tocopheryl phosphate (TP) and di-α-tocopheryl phosphate (T₂P), for the protection and delivery of therapeutics is being investigated in our laboratory and some promising results have been obtained so far. Novel nanocarrier systems containing TP, T₂P and different lipids/phospholipids (phosphatidylcholine, stearyl amine, Phospholipon 90H, Phospholipon 100H) with and without cholesterol were prepared using Mozafari method. The preparation method did not require utilization of potentially toxic solvents, detergents or employment of harsh treatments such as sonication or high-shear force homogenization. Tocosomes, containing 5-fluorouracil (as a model drug), were shown to possess narrow size distribution, acceptable encapsulation efficiency and long-term stability (more than two years).

Keywords: 5-Fluorouracil (PubChem CID: 3385); Cholesterol (PubChem CID: 5997); Drug delivery; Encapsulation; Mozafari method; Phosphatidylcholine (PubChem CID: 5287971); Phospholipid; Stearyl amine (PubChem CID: 15793); Tocopherol phosphate; α-Tocopheryl phosphate (PubChem CID: 94493).