title: Role of nanoparticle size, shape and surface chemistry in oral drug delivery.
abstract: Nanoparticles find intriguing applications in oral drug delivery since they present a large surface area for interactions with the gastrointestinal tract and can be modified in various ways to address the barriers associated with oral delivery. The size, shape and surface chemistry of nanoparticles can greatly impact cellular uptake and efficacy of the treatment. However, the interplay between particle size, shape and surface chemistry has not been well investigated especially for oral drug delivery. To this end, we prepared sphere-, rod- and disc-shaped nanoparticles and conjugated them with targeting ligands to study the influence of size, shape and surface chemistry on their uptake and transport across intestinal cells. A triple co-culture model of intestinal cells was utilized to more closely mimic the intestinal epithelium. Results demonstrated higher cellular uptake of rod-shaped nanoparticles in the co-culture compared to spheres regardless of the presence of active targeting moieties. Transport of nanorods across the intestinal co-culture was also significantly higher than spheres. The findings indicate that nanoparticle-mediated oral drug delivery can be potentially improved with departure from spherical shape which has been traditionally utilized for the design of nanoparticles. We believe that understanding the role of nanoparticle geometry in intestinal uptake and transport will bring forth a paradigm shift in nanoparticle engineering for oral delivery and non-spherical nanoparticles should be further investigated and considered for oral delivery of therapeutic drugs and diagnostic materials.
authors.affiliation: Department of Chemical Engineering, University of California, Santa Barbara, Santa Barbara, CA 93106, USA.
authors.forename: Amrita
authors.initials: A
authors.lastname: Banerjee
authors.affiliation: Department of Chemical Engineering, University of California, Santa Barbara, Santa Barbara, CA 93106, USA; School of Pharmacy, Fudan University, Shanghai 201203, PR China.
authors.forename: Jianping
authors.initials: J
authors.lastname: Qi
authors.affiliation: College of Letters and Science, University of California, Santa Barbara, Santa Barbara, CA 93106, USA.
authors.forename: Rohan
authors.initials: R
authors.lastname: Gogoi
authors.affiliation: Department of Chemical Engineering, University of California, Santa Barbara, Santa Barbara, CA 93106, USA.
authors.forename: Jessica
authors.initials: J
authors.lastname: Wong
authors.affiliation: Department of Chemical Engineering, University of California, Santa Barbara, Santa Barbara, CA 93106, USA; Center for Bioengineering, University of California, Santa Barbara, Santa Barbara, CA 93106, USA. Electronic address: samir@engineering.ucsb.edu.
authors.forename: Samir
authors.initials: S
authors.lastname: Mitragotri
mesh_terms: D018938:Caco-2 Cells; D002460:Cell Line; D018920:Coculture Techniques; D004337:Drug Carriers / Q000032:analysis / Q000737:chemistry* / Q000493:pharmacokinetics; D016503:Drug Delivery Systems; D006801:Humans; D007408:Intestinal Absorption; D053758:Nanoparticles / Q000032:analysis / Q000737:chemistry* / Q000648:ultrastructure; D010316:Particle Size; D013499:Surface Properties
chemical_list: D004337:Drug Carriers
keywords: Nanoparticle; Oral delivery; Shape; Size; Surface chemistry; Triple co-culture