Colloids and Surfaces B: Biointerfaces 134 (2015) 47–58 Contents lists available at ScienceDirect Colloids and Surfaces B: Biointerfaces j o ur nal ho me pa ge: www.elsevier.com/locate/colsurfb Galactose engineered solid lipid nanoparticles for targeted delivery of doxorubicin Ashay Jain a,b , Prashant Kesharwani b,c,∗ , Neeraj K. Garg a,b , Atul Jain a,b , Som Akshay Jain b , Amit Kumar Jain b , Pradip Nirbhavane a , Raksha Ghanghoria b , Rajeev Kumar Tyagi d,e , Om Prakash Katare a,∗∗ a Drug Delivery Research Group, University Institute of Pharmaceutical Sciences, UGC Centre of Advanced Studies, Panjab University, Chandigarh 160014, India b Department of Pharmaceutical Sciences, Dr. Hari Singh Gour University, Sagar 470003, MP, India c Department of Pharmaceutical Sciences, Eugene Applebaum College of Pharmacy and Health Sciences, Wayne State University, Detroit, MI 48201, USA d Department of Periodontics, College of Dental Medicine Georgia Regents University, 1120 15th Street, Augusta, GA 30912, USA e Biosafety Support Unit, Regional Centre for Biotechnology-DBT, C.G.O. Complex, Lodhi Road, New Delhi 110003, India a r t i c l e i n f o Article history: Received 28 February 2015 Received in revised form 17 May 2015 Accepted 11 June 2015 Available online 19 June 2015 Keywords: Galactose Solid lipid nanoparticles Doxorubicin Cytotoxicity Lectin Targeting a b s t r a c t The present investigation reports the preparation, optimization, and characterization of surface engi- neered solid lipid nanoparticles (SLNs) encapsulated with doxorubicin (DOX). Salient features such as biocompatibility, controlled release, target competency, potential of penetration, improved physical sta- bility, low cost and ease of scaling-up make SLNs viable alternative to liposomes for effective drug delivery. Galactosylation of SLNs instructs some gratifying characteristic, which leads to the evolution of promising delivery vehicles. The impendence of lectin receptors on different cell surfaces makes the galactosylated carriers admirable for targeted delivery of drugs to ameliorate their therapeutic index. Active participa- tion of some lectin receptors in immune responses to antigen overlaid the application of galactosylated carriers in delivery of antigen and immunotherapy for treatment of maladies like cancer. These advan- tages revealed the promising potential of galactosylated carriers in each perspective of drug delivery. The developed DOX loaded galactosylated SLNs formulation was found to have particle size 239 ± 2.40 nm, PDI 0.307 ± 0.004, entrapment efficiency 72.3 ± 0.9%. Higher cellular uptake, cytotoxicity, and nuclear localization of galactosylated SLNs against A549 cells revealed higher efficiency of the formulation. In a nutshell, the galactosylation strategy with SLNs could be a promising approach in improving the delivery of DOX for cancer therapy. © 2015 Elsevier B.V. All rights reserved. 1. Introduction Neoplastic cells express the number of receptors on the surface which encompass very high empathy for carbohydrate molecules; these receptors are known as membrane lectins and because of these receptors different carbohydrates may be used as ligand to target the therapeutic agents [1–5]. Lectin receptors mediated targeting uses interaction of endogenous ligands with differ- ent sugar moieties like galactose, mannose, fucose, fructose and ∗ Corresponding author at: Department of Pharmaceutical Sciences, Dr. Hari Singh Gour University, Sagar 470003, India. Tel.: +91 7582 244432; fax: +91 7582 244432. ∗∗ Corresponding author. E-mail addresses: prashant pharmacy04@rediffmail.com, prashantdops@gmail.com (P. Kesharwani), drkatare@yahoo.com (O.P. Katare). lactose [5,6]. When these carbohydrate moieties are anchored to different drug vehicles the resultant glycosylated carriers having carbohydrate as stratum ligands are acknowledged and endocy- tosed by lectin receptors. Lectin receptors are highly expressed on the alveolar macrophages, liver endothelial Kupffer cells, splenic macrophages, peritoneal macrophages, macrophages of brain, illustrate a quick internalization of galactose-terminated glyco- proteins via receptor-mediated endocytosis [7–9]. Consequently, the expansion of polysaccharide galactose-tagged drug delivery vehicles may emerge as a prospective strategy for the selective delivery of anti-cancer agents to the tumor tissues [10]. In this sequel transport of anticancer bioactives upon encap- sulation in different delivery vehicles has been comprehensively investigated. Amidst of these vehicles vis a vis microspheres [11], micelles [12,13], liposomes [14,15], nanoparticles [16–18], and dendrimers [19–21]. SLNs have materialized as the most http://dx.doi.org/10.1016/j.colsurfb.2015.06.027 0927-7765/© 2015 Elsevier B.V. All rights reserved.