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Article

Lipidated Peptidomimetic Ligand-Functionalized HER2 Targeted Liposome as Nano-Carrier Designed for Doxorubicin Delivery in Cancer Therapy

1
School of Basic Pharmaceutical and Toxicological Sciences, College of Pharmacy, University of Louisiana at Monroe, Monroe, LA 71201, USA
2
Department of Pathology, Microbiology & Immunology (PMI), School of Medicine, USC, SC 6439 Garners Ferry Rd, Columbia, SC 29208, USA
3
Biotechnology Laboratory, LSU AgCenter, Louisiana State University, Baton Rouge, LA 70803, USA
*
Author to whom correspondence should be addressed.
Equally contributed to the work.
Academic Editor: Dimitris Tsiourvas
Pharmaceuticals 2021, 14(3), 221; https://0-doi-org.brum.beds.ac.uk/10.3390/ph14030221
Received: 28 December 2020 / Revised: 2 March 2021 / Accepted: 3 March 2021 / Published: 6 March 2021
(This article belongs to the Special Issue Lung Injury and Repair)
The therapeutic index of chemotherapeutic agents can be improved by the use of nano-carrier-mediated chemotherapeutic delivery. Ligand-targeted drug delivery can be used to achieve selective and specific delivery of chemotherapeutic agents to cancer cells. In this study, we prepared a peptidomimetic conjugate (SA-5)-tagged doxorubicin (Dox) incorporated liposome (LP) formulation (SA-5-Dox-LP) to evaluate the targeted delivery potential of SA-5 in human epidermal growth factor receptor-2 (HER2) overexpressed non-small-cell lung cancer (NSCLC) and breast cancer cell lines. The liposome was prepared using thin lipid film hydration and was characterized for particle size, encapsulation efficiency, cell viability, and targeted cellular uptake. In vivo evaluation of the liposomal formulation was performed in a mice model of NSCLC. The cell viability studies revealed that targeted SA-5-Dox-LP showed better antiproliferative activity than non-targeted Dox liposomes (Dox-LP). HER2-targeted liposome delivery showed selective cellular uptake compared to non-targeted liposomes on cancer cells. In vitro drug release studies indicated that Dox was released slowly from the formulations over 24 h, and there was no difference in Dox release between Dox-LP formulation and SA-5-Dox-LP formulation. In vivo studies in an NSCLC model of mice indicated that SA-5-Dox-LP could reduce the lung tumors significantly compared to vehicle control and Dox. In conclusion, this study demonstrated that the SA-5-Dox-LP liposome has the potential to increase therapeutic efficiency and targeted delivery of Dox in HER2 overexpressing cancer. View Full-Text
Keywords: epidermal growth factor receptor (EGFR); liposome; doxorubicin; HER2; NSCLC epidermal growth factor receptor (EGFR); liposome; doxorubicin; HER2; NSCLC
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MDPI and ACS Style

Naik, H.; Sonju, J.J.; Singh, S.; Chatzistamou, I.; Shrestha, L.; Gauthier, T.; Jois, S. Lipidated Peptidomimetic Ligand-Functionalized HER2 Targeted Liposome as Nano-Carrier Designed for Doxorubicin Delivery in Cancer Therapy. Pharmaceuticals 2021, 14, 221. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14030221

AMA Style

Naik H, Sonju JJ, Singh S, Chatzistamou I, Shrestha L, Gauthier T, Jois S. Lipidated Peptidomimetic Ligand-Functionalized HER2 Targeted Liposome as Nano-Carrier Designed for Doxorubicin Delivery in Cancer Therapy. Pharmaceuticals. 2021; 14(3):221. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14030221

Chicago/Turabian Style

Naik, Himgauri, Jafrin J. Sonju, Sitanshu Singh, Ioulia Chatzistamou, Leeza Shrestha, Ted Gauthier, and Seetharama Jois. 2021. "Lipidated Peptidomimetic Ligand-Functionalized HER2 Targeted Liposome as Nano-Carrier Designed for Doxorubicin Delivery in Cancer Therapy" Pharmaceuticals 14, no. 3: 221. https://0-doi-org.brum.beds.ac.uk/10.3390/ph14030221

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