title: Solid self-nanoemulsifying drug delivery system (S-SNEDDS) containing phosphatidylcholine for enhanced bioavailability of highly lipophilic bioactive carotenoid lutein.
abstract: The objectives of this study was to prepare solid self-nanoemulsifying drug delivery system (S-SNEDDS) containing phosphatidylcholine (PC), an endogenous phospholipid with excellent in vivo solubilization capacity, as oil phase for the delivery of bioactive carotenoid lutein, by spray drying the SNEDDS (liquid system) containing PC using colloidal silica (Aerosil® 200 VV Pharma) as the inert solid carrier, and to evaluate the enhanced bioavailability (BA) of lutein from S-SNEDDS. The droplet size analyses revealed droplet size of less than 100 nm. The solid state characterization of S-SNEDDS by SEM, DSC, and XRPD revealed the absence of crystalline lutein in the S-SNEDDS. The bioavailability study performed in rabbits resulted in enhanced values of C(max) and AUC for S-SNEDDS. The enhancement of C(max) for S-SNEDDS was about 21-folds and 8-folds compared with lutein powder (LP) and commercial product (CP), respectively. The relative BA of S-SNEDDS compared with CP or LP was 2.74-folds or 11.79-folds, respectively. These results demonstrated excellent ability of S-SNEDDS containing PC as oil phase to enhance the BA of lutein in rabbits. Thus, S-SNEDDS containing PC as oil phase could be a useful lipid drug delivery system for enhancing the BA of lutein in vivo.
authors.affiliation: College of Pharmacy, Yeungnam University, Kyungsan, South Korea.
authors.forename: Srinivasan
authors.initials: S
authors.lastname: Shanmugam
authors.forename: Rengarajan
authors.initials: R
authors.lastname: Baskaran
authors.forename: Prabagar
authors.initials: P
authors.lastname: Balakrishnan
authors.forename: Pritam
authors.initials: P
authors.lastname: Thapa
authors.forename: Chul Soon
authors.initials: CS
authors.lastname: Yong
authors.forename: Bong Kyu
authors.initials: BK
authors.lastname: Yoo
mesh_terms: D000818:Animals; D001682:Biological Availability; D002338:Carotenoids / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D045703:Emulsifying Agents / Q000737:chemistry; D014975:Lutein / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D008297:Male; D009821:Oils / Q000737:chemistry; D010316:Particle Size; D010713:Phosphatidylcholines / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D010743:Phospholipids / Q000737:chemistry; D011817:Rabbits; D012822:Silicon Dioxide / Q000737:chemistry; D012995:Solubility
chemical_list: D004337:Drug Carriers; D045703:Emulsifying Agents; D009821:Oils; D010713:Phosphatidylcholines; D010743:Phospholipids; D002338:Carotenoids; D012822:Silicon Dioxide; D014975:Lutein