title: Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents.
abstract: In the present study, a phospholipid-based complex of standardized Centella extract (SCE) was developed with a goal of improving the bioavailability of its phytoconstituents. The SCE-phospholipid complex was prepared by solvent evaporation method and characterized for its physicochemical and functional properties. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), photomicroscopy, and powder x-ray diffraction (PXRD) were used to confirm the formation of Centella naturosome (CN). The prepared complex was functionally evaluated by apparent solubility, in vitro drug release, ex vivo permeation, and in vivo efficacy studies. The prepared CN exhibited a significantly higher (12-fold) aqueous solubility (98.0 ± 1.4 μg/mL), compared to the pure SCE (8.12 ± 0.44 μg/mL), or the physical mixture of SCE and the phospholipid (13.6 ± 0.4 μg/mL). The in vitro dissolution studies revealed a significantly higher efficiency of CN in releasing the SCE (99.2 ± 4.7, % w/w) in comparison to the pure SCE (39.2 ± 2.3, % w/w), or the physical mixture (42.8 ± 2.09, % w/w). The ex vivo permeation studies with the everted intestine method showed that the prepared CN significantly improved the permeation of SCE (82.8 ± 3.7, % w/w), compared to the pure SCE (26.8 ± 2.4, % w/w), or the physical mixture (33.0 ± 2.7, % w/w). The in vivo efficacy studies using the Morris Water Maze test indicated a significant improvement of the spatial learning and memory in aged mice treated with CN. Thus, drug-phospholipid complexation appears to be a promising strategy to improve the aqueous solubility and bioavailability of bioactive phytoconstituents.
authors.affiliation: Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur, India.
authors.forename: Suprit D
authors.initials: SD
authors.lastname: Saoji
authors.affiliation: Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur, India.
authors.forename: Nishikant A
authors.initials: NA
authors.lastname: Raut
authors.affiliation: Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur, India.
authors.forename: Pradip W
authors.initials: PW
authors.lastname: Dhore
authors.affiliation: Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University, Nagpur, India.
authors.forename: Chandrashekhar D
authors.initials: CD
authors.lastname: Borkar
authors.affiliation: Wegmans School of Pharmacy, St. John Fisher College, Rochester, New York, 14534, USA.
authors.forename: Michael
authors.initials: M
authors.lastname: Popielarczyk
authors.affiliation: Wegmans School of Pharmacy, St. John Fisher College, Rochester, New York, 14534, USA. viveksdave@gmail.com.
authors.forename: Vivek S
authors.initials: VS
authors.lastname: Dave
mesh_terms: D000375:Aging / Q000523:psychology; D000818:Animals; D001682:Biological Availability; D028041:Centella / Q000737:chemistry*; D007408:Intestinal Absorption; D008297:Male; D018782:Maze Learning / Q000187:drug effects; D008568:Memory / Q000187:drug effects; D051379:Mice; D010743:Phospholipids / Q000737:chemistry*; D008517:Phytotherapy / Q000379:methods*; D010936:Plant Extracts / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013028:Space Perception / Q000187:drug effects; D014315:Triterpenes / Q000737:chemistry / Q000493:pharmacokinetics
chemical_list: D010743:Phospholipids; D010936:Plant Extracts; D014315:Triterpenes
keywords: drug-phospholipid complex; permeability; phytoconstituents; solubility