Herceptin-functionalized pure paclitaxel nanocrystals for enhanced delivery to HER2-postive breast cancer cells

[Display omitted] The objective of this study was to prepare Herceptin (HCT)-functionalized paclitaxel nanocrystals and evaluated their cell-specific interactions, cellular accumulation, and growth inhibition in HER2-positve breast cancer cells as a tumor-targeted delivery module. Paclitaxel (PTX) w...

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Bibliographic Details
Published in:International journal of pharmaceutics 2016-11, Vol.513 (1-2), p.543-553
Main Authors: Noh, Jin-Ki, Naeem, Muhammad, Cao, Jiafu, Lee, Eun Hee, Kim, Min-Soo, Jung, Yunjin, Yoo, Jin-Wook
Format: Article
Language:English
Subjects:
Adsorption
Antineoplastic Agents - administration & dosage
Antineoplastic Agents - chemistry
Breast Neoplasms
Cell Cycle - drug effects
Cell Line, Tumor
Cell Survival - drug effects
Drug Delivery Systems
Drug Liberation
HER2-positve breast cancer
Herceptin
Humans
Nanocrystals
Nanoparticles - administration & dosage
Nanoparticles - chemistry
Paclitaxel
Paclitaxel - administration & dosage
Paclitaxel - chemistry
Particle Size
Receptor, ErbB-2
Trastuzumab - administration & dosage
Trastuzumab - chemistry
Tumor-targeting
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Summary:[Display omitted] The objective of this study was to prepare Herceptin (HCT)-functionalized paclitaxel nanocrystals and evaluated their cell-specific interactions, cellular accumulation, and growth inhibition in HER2-positve breast cancer cells as a tumor-targeted delivery module. Paclitaxel (PTX) was fabricated in the form of nanocrystals (PNCs) by a sono-precipitation method, and HCT were coated using a facile non-covalent method (PNCs-HCT). Our results showed that the PNCs-HCT were stable for at least 1month at 4°C with no noticeable desorption of HCT. The release test showed that PNCs-HCT exhibited sustained drug release similar to only PNCs but with a higher release rate than only PTX powder. Cellular uptake, cytotoxicity, and cell cycle arrest studies revealed that PNCs-HCT exhibit greater binding affinity and higher cell-specific internalization to HER2-positive breast cancer cell lines as compared to PNCs, followed by enhanced cell growth inhibition. HCT-functionalized PNCs presented in this study offer a promising strategy for targeted pure drug nanocrystal delivery and enhancing the efficiency of anticancer therapy.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2016.09.067