title: Biodegradable Poly (Lactic-co-Glycolic Acid)-Polyethylene Glycol Nanocapsules: An Efficient Carrier for Improved Solubility, Bioavailability, and Anticancer Property of Lutein.
abstract: Lutein bioavailability is limited because of its poor aqueous solubility. In this study, lutein-poly (lactic-co-glycolic acid) (PLGA)-polyethylene glycol (PEG) nanocapsules were prepared to improve the solubility, bioavailability, and anticancer property of lutein. The scanning electron microscopy and dynamic light scattering examination revealed that the nanocapsules are smooth and spherical with size ranging from 80 to 500 nm (mean = 200 nm). In vitro lutein release profile from nanocapsules showed controlled sustainable release (66%) up to 72 h. Aqueous solubility of lutein nanocapsules was much higher by 735-fold than the lutein. Fourier transform infrared spectroscopy analyses showed no chemical interaction among PLGA, PEG, and lutein, indicating possible weak intermolecular forces like hydrogen bonds. X-ray diffraction revealed lutein is distributed in a disordered amorphous state in nanocapsules. Postprandial plasma kinetics (area under the curve) of an oral dose of lutein from nanocapsules was higher by 5.4-fold compared with that of micellar lutein (control). The antiproliferative effect of lutein from nanocapsules (IC50 value, 10.9 μM) was higher (43.6%) than the lutein (IC50 value, 25 μM). Results suggest that PLGA-PEG nanocapsule is an efficient carrier for enhancing hydrophilicity, bioavailability, and anticancer property of lipophilic molecules such as lutein.
authors.affiliation: Department of Molecular Nutrition, CSIR - Central Food Technological Research Institute, Mysore 570 020, Karnataka, India.
authors.forename: Ranganathan
authors.initials: R
authors.lastname: Arunkumar
authors.affiliation: Department of Meat and Marine Science, CSIR - Central Food Technological Research Institute, Mysore 570 020, Karnataka, India.
authors.forename: Keelara Veerappa Harish
authors.initials: KVH
authors.lastname: Prashanth
authors.affiliation: Division of Applied Biosciences, Graduate School of Agriculture, Kyoto University, Kyoto 606-8502, Japan.
authors.forename: Yuki
authors.initials: Y
authors.lastname: Manabe
authors.affiliation: Division of Applied Biosciences, Graduate School of Agriculture, Kyoto University, Kyoto 606-8502, Japan.
authors.forename: Takashi
authors.initials: T
authors.lastname: Hirata
authors.affiliation: Division of Applied Biosciences, Graduate School of Agriculture, Kyoto University, Kyoto 606-8502, Japan.
authors.forename: Tatsuya
authors.initials: T
authors.lastname: Sugawara
authors.affiliation: Department of Biochemistry and Nutrition, CSIR-Central Food Technological Research Institute, Mysore 570 020, Karnataka, India.
authors.forename: Shylaja Mallaiah
authors.initials: SM
authors.lastname: Dharmesh
authors.affiliation: Department of Molecular Nutrition, CSIR - Central Food Technological Research Institute, Mysore 570 020, Karnataka, India. Electronic address: baskaranv@cftri.res.in.
authors.forename: Vallikannan
authors.initials: V
authors.lastname: Baskaran
mesh_terms: D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D001682:Biological Availability; D049109:Cell Proliferation / Q000187:drug effects; D004355:Drug Stability; D056945:Hep G2 Cells; D006801:Humans; D019344:Lactic Acid / Q000737:chemistry*; D014975:Lutein / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics* / Q000494:pharmacology; D008297:Male; D051379:Mice; D053769:Nanocapsules / Q000737:chemistry*; D009369:Neoplasms / Q000188:drug therapy; D011092:Polyethylene Glycols / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D012995:Solubility; D031686:Tagetes / Q000737:chemistry
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D053769:Nanocapsules; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D011092:Polyethylene Glycols; D014975:Lutein
keywords: X-ray powder diffractometry; antioxidants; bioavailability; biodegradable polymers; nanocapsules; pharmacokinetics; poly(lactic/glycolic) acid (PLGA or PLA); polymeric drug carrier; poorly water-soluble drugs