Phytolipid delivery of Pentaclethra macrophylla (Fabaceae) extract: In vitro and in vivo activities

Purpose: To investigate the physicochemical properties and in vivo anti-inflammatory activity of phytosome complexes prepared from Pentaclethra macrophylla seeds. Method: Pentaclethra macrophylla seeds were extracted using Petroleum ether. Wavelength of maximum absorption (λ) of bioactive compounds (BCs) was determined. Phytochemical constituents were quantified and formulated as phytosome complexes in different ratios of lipid-based phospholipon complexes (LPCs; 1:1, 1:2, and 2:1 as LPC1, LPC2, and LPC3, respectively). Formulated phytosome complexes were evaluated for percentage yield, encapsulation efficiency (EE), and Fourier transform infrared spectroscopy (FTIR). In vitro drug release was done using 10 mg LPCs in simulated intestinal fluid (SIF, pH 6.8). A total of 40 female Wistar rats, randomized into 5 groups (n = 8 per group), were used. Group 1 (received 100 mg/kg of pure lipid bioactive compounds), group 2 (received 100 mg/kg LPC formulation (LPC3 optimized complex, (selected because it has the highest EE), group 3 (received 10 mg/kg of Indomethacin (positive standard), group 4 (received distilled water equivalent to 70 mg/kg (0.64 mL), and group 5 (received no treatment (negative control). Anti-inflammatory effect was evaluated using rat paw oedema model. Results: Yield was 33.43 %, alkaloid was high (2.80 %), λ was 234 nm, EE in LP3 was 93 ± 0.09 %. In vitro drug release of all LPCs demonstrated a gradual and retarded drug release within 22 – 38 % after 1 h. Also, LPC3 has significantly higher anti-inflammatory activity (98 %) compared to controls (p < 0.05). Conclusion: Formulating Pentaclethra macrophylla as a lipid-based phospholipid complex improves entrapment efficiency, retards drug release, and significantly increases anti-inflammatory activity.