Abstract
Background: Boldine, is an aporphine alkaloid that possesses potent antioxidant activity. Despite having enormous potential, the clinical application of boldine was restricted because of its poor bioavailability attributed to its poor aqueous solubility and rapid clearance from the body. The drug phospholipid complexation techniques were frequently employed to overcome the limitation of low bioavailability of phytoconstituents/herbal extract.
Objective: The boldine phospholipid complex (BOL-PC) formulation was developed for enhancing antioxidant potential of boldine by preparing its phospholipid complex.
Methods: Boldine loaded phospholipid (BOL-PC) complex was prepared by refluxing followed by solvent evaporation method and subjected to various physicochemical and spectral analysis. Further, the in-vitro antioxidant activity was evaluated by DPPH free radical scavenging method.
Results: The formation of the complex was confirmed by 1H NMR and thermal analysis. SEM and PXRD revealed partial amorphization of drug in complex formed. The BOL-PC dissolution rate and solubility were significantly improved compared to the parent compound. The maximum % yield and % EE were found to be 95.92± 0.01732 and 95.89±0.3502 respectively in the optimized formulation (F3), which exhibited concentration-dependent antioxidant property.
Conclusion: It was concluded from the study that the phospholipid complexation of boldine has better antioxidant potential and improved the solubility, dissolution profile which may facilitate its oral absorption and enhances its chances for clinical application.
Keywords: Phyto-phospholipid complex, boldine, PXRD, solubility, antioxidant activity, DSC.
Graphical Abstract
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