Flaxseed oil is a rich source of polyunsaturated fatty acids (PUFA). It contains up to 57% of linolenic acid (omega-3 fatty acid) and up to 17% of linoleic acid. Due to such high content of PUFA, it is a potential skin permeation enhancer. Moreover, it has anti-proliferative activity against breast cancer.
Tamoxifen is an anti-cancer agent that binds to estrogen receptors in breast cancer cells and inhibits cell proliferation. However the systemic administration of tamoxifen is associated with severe side effects including endometrial cancer. To this end the topical delivery of tamoxifen to the breast tissue is a promising strategy for localized therapy. The topical delivery of tamoxifen is limited by its poor skin penetration characteristics.
We have developed a formulation that can harness the multifunctional properties of multiple therapeutic agents. Several oil in water emulsion formulations (nano and micro emulsions) were developed using alpha santalol or flaxseed oil as the oil phase. Alpha santalol is known to have anti-cancer properties (skin, breast and prostate cancers, among others). It also has skin penetration enhancing properties. Alpha santalol or sandalwood oil can be used as the oil phase of the emulsion. Flaxseed oil is a rich source of PUFA and is known to have beneficial effects in prevention and treatment of cancer, cardiovascular, diabetes and inflammatory disorders. The components of PUFA (i.e., linolenic acid and linoleic acid) are known to have skin penetration enhancing properties. Further, the flaxseed oil can be used as the oil phase in the emulsion. In a further modification of the formulation, both alpha santalol (or sandalwood oil) and PUFA were used as the oil phase in the emulsion. This formulation in addition to synergistically increasing the skin penetration may also lead to enhanced anti-cancer or anti-inflammatory activity. Further, it can be used to deliver other therapeutic agents.
The multifunctional property of sandalwood oil/santalol and flaxseed oil offers a number of unique advantages for the delivery of drugs for prevention and treatment of cancer and other diseases.