Abstract
The present study deals with the encapsulation and brain-specific targeting of Lycopene (LYC) as Polysorbate-80 (P-80) coated Phosphatidylserine-chitosan self-assembled nanoparticles (P-80-LYC-PSCNP), with an approach to reduce oxidative stress which is rationalized as a major cause of neurological disease. P-80-LYC-PSCNP was formulated by using the injection technique for self-assembly of Phosphatidylserine and chitosan, applying P-80 coating for surface modification and were assessed for their morphology and physicochemical attributes. The efficiency of LYC liberated from P-80-LYC-PSCNP was determined in Streptozotocin-induced Oxidative stress Model (SOSM); cognitively by behavioral despair-test and biochemically by enzymatic assays at 5 mg/kg LYC-equivalent dose. P-80-LYC-PSCNP were formulated as stable (ζ = 3.89 mV) spherical, regular (≈220 nm), and homogenous entities. It demonstrated a total 76.89% LYC in-vitro release during 28 hrs and shown efficacy for brain-specific delivery with a relative bioavailability of 20.4, Cmax 4.6 times, and 2.5 times swifter than normal LYC. After 28 days, it shortened immobility time by 72.57 ± 8.12 s (P < 0.01) against STZ-control (134.58 ± 13.85 s, P < 0.001). It also improved the antioxidant enzymatic functioning of CAT, SOD, and GPx by 7.90 ± 0.45 Δ240/min/mgP (P < 0.05), 32.50 ± 1.70 U/mgP (P < 0.01), and 59.40 ± 3.70 U/mgP (P < 0.01) respectively against STZ-control which showed 3.05 ± 0.80 Δ240/min/mgP (P < 0.05), 15.20 ± 3.10 U/mgP (P < 0.05), and 25.15 ± 3.05 U/mgP at 5 mg/kg LYC-equivalent dose respectively. P-80-LYC-PSCNP was successfully formulated, analyzed and had delivered Lycopene (5 mg/kg) by trespassing the BBB with improved pharmacokinetics. It alleviated the experimental Streptozotocin-induced Oxidative stress in turn improving behavioral and cognitive anomalies, while enhancing the antioxidant-related activity of enzymes.
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