Herceptin-functionalized pure paclitaxel nanocrystals for enhanced delivery to HER2-postive breast cancer cells.
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.
College of Pharmacy, Pusan National University, Busan, South Korea.
Jin-Ki
JK
Noh
College of Pharmacy, Pusan National University, Busan, South Korea.
Muhammad
M
Naeem
College of Pharmacy, Pusan National University, Busan, South Korea.
Jiafu
J
Cao
College of Pharmacy, Korea University, Sejong, South Korea.
Eun Hee
EH
Lee
College of Pharmacy, Pusan National University, Busan, South Korea.
Min-Soo
MS
Kim
College of Pharmacy, Pusan National University, Busan, South Korea.
Yunjin
Y
Jung
College of Pharmacy, Pusan National University, Busan, South Korea. Electronic address: jinwook@pusan.ac.kr.
Jin-Wook
JW
Yoo
D000327:Adsorption; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry; D001943:Breast Neoplasms; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D016503:Drug Delivery Systems; D065546:Drug Liberation; D006801:Humans; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D017239:Paclitaxel / Q000008:administration & dosage* / Q000737:chemistry; D010316:Particle Size; D018719:Erb-b2 Receptor Tyrosine Kinases; D000068878:Trastuzumab / Q000008:administration & dosage* / Q000737:chemistry
D000970:Antineoplastic Agents; D017239:Paclitaxel; D018719:Erb-b2 Receptor Tyrosine Kinases; D000068878:Trastuzumab; C508053:ERBB2 protein, human
HER2-positve breast cancer; Herceptin; Nanocrystals; Paclitaxel; Tumor-targeting