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Int J Pharm. 2015 Feb 1;479(1):77-87. doi: 10.1016/j.ijpharm.2014.12.044. Epub 2014 Dec 26.

Cellular interactions and photoprotective effects of idebenone-loaded nanostructured lipid carriers stabilized using PEG-free surfactant.

Author information

1
Department of Pharmaceutics, Poona College of Pharmacy, Bharati Vidyapeeth University, Erandwane, Pune 411038, Maharashtra, India; National Centre for Cell Science, NCCS Complex, Pune University Campus, Ganeshkhind, Pune 411007, Maharashtra, India.
2
National Centre for Cell Science, NCCS Complex, Pune University Campus, Ganeshkhind, Pune 411007, Maharashtra, India.
3
Department of Pharmaceutics, Poona College of Pharmacy, Bharati Vidyapeeth University, Erandwane, Pune 411038, Maharashtra, India. Electronic address: vbpokharkar@yahoo.co.in.

Abstract

In past years, nanostructured lipid carriers (NLCs) have emerged as novel topical antioxidant delivery systems because of combined positive features of liposomes and polymeric nanoparticles. Here, we seek to unlock the possibility of idebenone (IDB; an antioxidant)-loaded NLCs (IDB-NLCs) cellular interactions such as, viability and uptake, and its photoprotective effects against Ultraviolet-B (UVB)-mediated oxidative stress in immortal human keratinocyte cell line (HaCaT). The two-step preformulation strategy followed by three-level, three-variable, L9 (3(3)) Taguchi robust orthogonal design employed was important in improving IDB-NLCs key physicochemical aspects such as, entrapment efficiency, drug release (sustained), occlusion, skin deposition and physical stability. UV crosslinker, confocal microscopy and flow cytometry techniques were used to (1) mediate oxidative stress in HaCaT cells, (2) study a qualitative cellular uptake, (3) measure intracellular reactive oxygen species (ROS), and mitochondrial membrane potential, respectively. NLCs markedly improved biocompatibility of IDB under normal as well as stress conditions. Quantitative and qualitative cell uptake studies demonstrated a significant uptake of IDB-NLCs (3-fold increase) and nile red-labeled IDB-NLCs (NR-IDB-NLCs) at 2 h, respectively, hence exerted improved photoprotective effects.

KEYWORDS:

Biocompatibility; Nanostructured lipid carriers; Oxidative stress; PEG-free surfactant; Photoprotection; Taguchi design

PMID:
25545795
DOI:
10.1016/j.ijpharm.2014.12.044
[Indexed for MEDLINE]

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