title: The role of phospholipid as a solubility- and permeability-enhancing excipient for the improved delivery of the bioactive phytoconstituents of Bacopa monnieri.
abstract: 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.
authors: Department of Pharmaceutical Sciences, R.T.M. Nagpur University, Nagpur, India.
authors: Suprit D
authors: SD
authors: Saoji
authors: St. John Fisher College, Wegmans School of Pharmacy, Rochester, NY, USA.
authors: Vivek S
authors: VS
authors: Dave
authors: Department of Pharmaceutical Sciences, R.T.M. Nagpur University, Nagpur, India.
authors: Pradip W
authors: PW
authors: Dhore
authors: Department of Pharmaceutical Sciences, R.T.M. Nagpur University, Nagpur, India.
authors: Yamini S
authors: YS
authors: Bobde
authors: St. John Fisher College, Wegmans School of Pharmacy, Rochester, NY, USA.
authors: Connor
authors: C
authors: Mack
authors: Lake Erie College of Osteopathic Medicine, School of Pharmacy, Bradenton, FL, USA.
authors: Deepak
authors: D
authors: Gupta
authors: Department of Pharmaceutical Sciences, R.T.M. Nagpur University, Nagpur, India. Electronic address: nishikantraut29@gmail.com.
authors: Nishikant A
authors: NA
authors: Raut
mesh_terms: D000818:Animals; D000928:Antidepressive Agents / Q000008:administration & dosage; D034681:Bacopa / Q000737:chemistry*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D065546:Drug Liberation; D005079:Excipients / Q000737:chemistry*; D006801:Humans; D008297:Male; D051379:Mice; D010316:Particle Size; D010539:Permeability; D010743:Phospholipids / Q000737:chemistry*; D064209:Phytochemicals / Q000008:administration & dosage*; D010936:Plant Extracts / Q000008:administration & dosage*; D033362:Powder Diffraction; D012995:Solubility
chemical_list: D000928:Antidepressive Agents; D005079:Excipients; D010743:Phospholipids; D064209:Phytochemicals; D010936:Plant Extracts
keywords: Complexation; Excipients; Permeability; Phytoconstituents; Solubility