Exploitation of amaranth oil fractions enriched in squalene for dual delivery of hydrophilic and lipophilic actives

• Co-encapsulation of water and lipid-soluble drugs in the same delivery system.
• Multiscaled squalene based-nanocarriers with nanoconfinements less than 15 nm.
• Co-encapsulation effect with values of about 90% for both kinds of drugs.
• Nanocarriers that assure a successful dual release of hydrophilic and lipophilic drugs.
• Antioxidant activity was observed to the extent of 98% scavenged free-oxygen radicals.

The study describes an ideal approach to increase the co-encapsulation of two water and lipid-soluble drugs in the same delivery system. The main purpose is represented by the exploitation of oil fractions isolated from amaranth seeds for the development of squalene-based nanocarriers able for a dual release of one antitumor drug, pemetrexed and one bio-flavonoid, hesperidin. The co-encapsulated nanocarriers presented unique nanoassembly morphology and showed excellent stability against aggregation. A delimited repartition of both actives, mainly in oily nanoconfinements of lipid nanocariers has been indicated by scanning calorimetry. The entrapment efficiency study revealed a great encapsulation effect with values reaching 94% for hesperidin and 89% for pemetrexed. These values are associated with a high ability of squalene-nanocarriers to capture free radicals. The greatest antioxidant activity was determined for nanocarriers that co-encapsulate 1.4% drugs, e.g., 97.3 and 98.2%. In vitro co-release tests demonstrated that pemetrexed and hesperidin were gradually released despite of their different lipophilicity. The most concentrated squalene fraction assures a slower release of both actives. The cumulative results showed that the applied strategy is a promising approach to improve the performance of medical treatments used to prevent and treat diseases associated with tumor and oxidative stress.

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