PEGylated polypeptide lipid nanocapsules to enhance the anticancer efficacy of erlotinib in non-small cell lung cancer
- Authors
- Kim, Jeonghwan; Ramasamy, Thiruganesh; Choi, Ju Yeon; Kim, Ssang Tae; Youn, Yu Seok; Choi, Han-Gon; Yong, Chul Soon; Kim, Jong Oh
- Issue Date
- Feb-2017
- Publisher
- ELSEVIER
- Keywords
- Erlotinib; Polypeptide; Nanocapsules; Antitumor efficacy; Lung cancer
- Citation
- COLLOIDS AND SURFACES B-BIOINTERFACES, v.150, pp.393 - 401
- Indexed
- SCIE
SCOPUS
- Journal Title
- COLLOIDS AND SURFACES B-BIOINTERFACES
- Volume
- 150
- Start Page
- 393
- End Page
- 401
- URI
- https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/10184
- DOI
- 10.1016/j.colsurfb.2016.11.002
- ISSN
- 0927-7765
- Abstract
- In this study, a core-shell type polypeptide-based lipid nanocapsule was developed to enhance anticancer efficacy of erlotinib in non-small cell lung cancers. Mean particle size of PEGylated polypeptide-lipid nanocapsules (PLN) for erlotinib (ERL) delivery was similar to 200 nm with an effective surface charge of -20 mV. Protective PEGylated polypeptide layer acted as a molecular fence and effectively controlled the diffusion of erlotinib from the lipid nanocapsule core, whereas pH-responsiveness of poly(L-aspartic acid) accelerated the release of erlotinib in acidic conditions. Blank lipid nanocapsules showed excellent bio-compatibility. ERL-loaded PLN (ERL-PLN) showed dose-dependent cytotoxicity in NCl-H358 and HCC-827 lung cancer cells. ERL-PLN treatment resulted in a superior tumor regression profile in a xenograft tumor model, compared to free ERL and control, suggesting high therapeutic efficacy. ERL-PLN-treated mice showed 5- and 2-fold smaller tumor volume compared to control and free ERL groups, respectively. Based on these results, PLN provide a promising drug delivery approach for lung cancer therapy. (C) 2016 Elsevier B.V. All rights reserved.
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