The role of phospholipid as a solubility- and permeability-enhancing excipient for the improved delivery of the bioactive phytoconstituents of Bacopa monnieri

• Published in: European journal of pharmaceutical sciences Vol. 108; pp. 23 - 35
• Main Authors: Saoji, Suprit D., Dave, Vivek S., Dhore, Pradip W., Bobde, Yamini S., Mack, Connor, Gupta, Deepak, Raut, Nishikant A.
• Format: Journal Article
• Language: English
• Published: Netherlands Elsevier B.V 15-10-2017
• Subjects: Animals; Antidepressive Agents - administration & dosage; Bacopa - chemistry; Biological Availability; Chemistry, Pharmaceutical; Complexation; Drug Delivery Systems; Drug Liberation; Excipients; Excipients - chemistry; Humans; Male; Mice; Particle Size; Permeability; Phospholipids - chemistry; Phytochemicals - administration & dosage; Phytoconstituents; Plant Extracts - administration & dosage; Powder Diffraction; Solubility; Complexation; Excipients; Permeability; Phytoconstituents; Solubility
• ISSN: 0928-0987; 1879-0720
• DOI: 10.1016/j.ejps.2016.08.056

In an attempt to improve the solubility and permeability of Standardized Bacopa Extract (SBE), a complexation approach based on phospholipid was employed. A solvent evaporation method was used to prepare the SBE-phospholipid complex (Bacopa Naturosome, BN). The formulation and process variables were optimized using a central-composite design. The formation of BN was confirmed by photomicroscopy, Scanning Electron Microscopy (SEM), Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), and Powder X-ray Diffraction (PXRD). The saturation solubility, the in-vitro dissolution, and the ex-vivo permeability studies were used for the functional evaluation of the prepared complex. BN exhibited a significantly higher aqueous solubility compared to the pure SBE (20-fold), or the physical mixture of SBE and the phospholipid (13-fold). Similarly, the in-vitro dissolution revealed a significantly higher efficiency of the prepared complex (BN) in releasing the SBE (>97%) in comparison to the pure SCE (~42%), or the physical mixture (~47%). The ex-vivo permeation studies showed that the prepared BN significantly improved the permeation of SBE (>90%), compared to the pure SBE (~21%), or the physical mixture (~24%). Drug-phospholipid complexation may thus be a promising strategy for solubility enhancement of bioactive phytoconstituents.
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