Role of nanoparticle size, shape and surface chemistry in oral drug delivery

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• 作者：Amrita Banerjee^a ; ¹ ; Jianping Qi^a ; ^b ; ¹ ; Rohan Gogoi^c ; Jessica Wong^a ; Samir Mitragotri^a ; ^d ; ^{samir@engineering.ucsb.edu" class="auth_mail" title="E-mail the corresponding author}
• 关键词：BCA ; bicinchoninic acid ; CFSE ; carboxyfluorescein diacetate succinimidyl ester ; DAPI ; (4&prime ; 6-diamidino-2-phenylindole ; dihydrochloride) ; DMEM ; Dulbecco's Modified Eagle's Medium ; DPBS ; Dulbecco's phosphate-buffered saline ; EDC ; N-(3-dimethylaminopropyl)-N&prime ; -ethylcarbodiimide hydrochloride ; EDTA ; ethylene diamine tetra acetic acid ; FBS ; fetal bovine serum ; HBSS ; Hank's balanced salt solution ; GIT ; gastrointestinal tract ; Papp ; apparent permeability ; PBS ; phosphate buffered saline ; PEG
• 刊名：Journal of Controlled Release
• 出版年：2016
• 出版时间：28 September 2016
• 年：2016
• 卷：238
• 期：Complete
• 页码：176-185
• 全文大小：1491 K

文摘

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.