title: Comparative real-time study of cellular uptake of a formulated conjugated linolenic acid rich nano and conventional macro emulsions and their bioactivity in ex vivo models for parenteral applications.
abstract: The objective of the present study was to fabricate and monitor real-time, impact of a stable conjugated linolenic acid, α-eleostearic acid (ESA) rich nanoemulsion (NE) formulation (d < 200 nm) vis-à-vis ESA conventional emulsion (CE) system in ex vivo systems against both endogenous and exogenous reactive oxygen species (ROS). Accordingly, stable nanoemulsion formulation of ESA was engineered with the aid of bitter melon seed oil and non-toxic excipients. Morphology and particle size of the emulsion formulations were studied to validate stability. The real-time rapid uptake of the ESA NE and its increased prophylactic efficacy against induced endogenous and exogenous ROS in terms of cell viability and membrane integrity was evaluated flow-cytometrically and with fluorescence microscopic analysis of different primary cells. It was found that the fabricated non-toxic ESA NE had stable parameters (hydrodynamic mean diameter, particle size distribution and zeta potential) for over 12 weeks. Further, ESA NE at a concentration of ∼ 70 μM exhibited maximum efficacy in protecting cells from oxidative damage against both endogenous and exogenous ROS in lymphocytes and hepatocytes as compared to its corresponding presence in the CE formulation. This study provides a real-time empirical evidence on the influence of nano formulation in enhancing bioavailability and antioxidative properties of ESA.
authors.affiliation: Laboratory of Food Science & Technology, Food & Nutrition Division, University of Calcutta, 20 B Judges Court Road, Kolkata, West Bengal 700027,India; Centre for Research in Nanoscience & Nanotechnology, University of Calcutta, JD 2, Sector III, Salt Lake City, Kolkata, West Bengal 700098, India.
authors.forename: Debjyoti
authors.initials: D
authors.lastname: Paul
authors.affiliation: Laboratory of Food Science & Technology, Food & Nutrition Division, University of Calcutta, 20 B Judges Court Road, Kolkata, West Bengal 700027,India; Centre for Research in Nanoscience & Nanotechnology, University of Calcutta, JD 2, Sector III, Salt Lake City, Kolkata, West Bengal 700098, India.
authors.forename: Sayani
authors.initials: S
authors.lastname: Mukherjee
authors.affiliation: Department of Biochemistry, University of Calcutta, 35, Ballygunge Circular Road, Kolkata, West Bengal 700019, India.
authors.forename: Rajarshi
authors.initials: R
authors.lastname: Chakraborty
authors.affiliation: Centre for Research in Nanoscience & Nanotechnology, University of Calcutta, JD 2, Sector III, Salt Lake City, Kolkata, West Bengal 700098, India.
authors.forename: Sanjaya K
authors.initials: SK
authors.lastname: Mallick
authors.affiliation: Laboratory of Food Science & Technology, Food & Nutrition Division, University of Calcutta, 20 B Judges Court Road, Kolkata, West Bengal 700027,India; Centre for Research in Nanoscience & Nanotechnology, University of Calcutta, JD 2, Sector III, Salt Lake City, Kolkata, West Bengal 700098, India. Electronic address: pubalighoshdhar@yahoo.co.in.
authors.forename: Pubali
authors.initials: P
authors.lastname: Dhar
mesh_terms: D016923:Cell Death / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004655:Emulsions / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007963:Leukocytes, Mononuclear / Q000737:chemistry* / Q000166:cytology / Q000378:metabolism; D046911:Macromolecular Substances / Q000737:chemistry / Q000494:pharmacology; D049329:Nanostructures / Q000737:chemistry*; D010316:Particle Size; D017382:Reactive Oxygen Species / Q000378:metabolism; D013329:Structure-Activity Relationship; D013499:Surface Properties; D013997:Time Factors; D017962:alpha-Linolenic Acid / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D004655:Emulsions; D046911:Macromolecular Substances; D017382:Reactive Oxygen Species; D017962:alpha-Linolenic Acid
keywords: Flow cytometry; Nanoemulsion; Reactive oxygen species; Transmission electron microscopy; α-Eleostearic acid