1Assistant Professor, Vels Institute of Science Technology and Advanced Studies, Velan Nagar, PV. Vaithiyalingam Road, Pallavaram, Chennai 600117; Email: nivearaj96@gmail.com
2Associate Professor, IIMT College of Medical Sciences (IIMT University); Email: namratasingh_pharma@iimtindia.net; ORCID: 0009-0003-3282-6253
3Assistant Professor, IIMT University, College of Medical Sciences (Pharmacy), 'O' Pocket Ganga Nagar, Meerut, U.P, India; Email: afsha1837@gmail.com; ORCID: 0000-0002-6814-5826
4Assistant Professor, Department of Food Technology, JAIN (Deemed-to-be University) Bangalore - 562112
5Associate Professor, School of Pharmacy, Dhamma Dipa International Buddhist University, Manu Bankul, Sabroom, South Tripura, India, Pin No. - 799143; Email: bimald32@gmail.com
6Professor and Head, Department of Pharmaceutics, School of Pharmaceutical Sciences, Faculty of Pharmacy, IFTM University, Moradabad, Uttar Pradesh, India; Email: p23upadhyay@yahoo.com, prashantupadhyay@iftmuniversity.ac.in
7Assistant Professor (SG), Department of Computer Science and Engineering, School of Computing, Vel Tech Rangarajan Dr. Sagunthala R&D Institute of Science and Technology, Avadi, Chennai, Tamilnadu, India – 600062; Email: spsanthoshkumar16@gmail.com; ORCID ID: https://orcid.org/0000-0001-8531-759X
8Professor, Department of Pharmaceutics, Danteswari College of Pharmacy, Jagdalpur, Chattisgarh - 494221; Email: bbasantareddy1@gmail.com
*Corresponding author: Dr. Boi Basanta Kumar Reddy, Professor, Department of Pharmaceutics, Danteswari College of Pharmacy, Jagdalpur, Chattisgarh - 494221; Email: bbasantareddy1@gmail.com
The traditional chemotherapy has weaknesses on non-specific biodistribution, severe systemic toxicity, and optimum tumor accumulation. In a bid to overcome these obstacles, the present research was aimed at developing and in vitro assessing PEGylated liposomes as a core system to target cancer therapy, where Irinotecan hydrochloride, a prototype chemotherapeutic agent, was used in the study. The liposomes were prepared successfully through the thin-film hydration and sonication technique using egg phosphatidylcholine, cholesterol and methylated polyethylene glycol (MPEG). The prepared vesicles had ideal nanoscale properties with a mean particle size of 152.3 ± 4.7 nm, polydispersity index of 0.18 ± 0.02, and zeta potential of -12.5 ±1.8 mV that are favorable to passive tumor targeting through Enhanced Permeability and Retention (EPR) effect. Efficiency of drug entrapment of 85.4 ± 2.1 percent was attained. The in vitro drug release studies indicated a sustained profile of up to 48 hours and stability studies showed that storage at 4°C was essential to the maintenance of integrity of formulation during a period of one month. A comparative cellular uptake study was modeled as a demonstration of active targeting using the HER2-positive (MCF-7/HER2+) and the HER2-negative (MDA-MB-231) breed cancer cell lines. The flow cytometry and confocal microscopy were performed to observe low and non-specific uptake of the non-targeted PEGylated liposomes in both cell lines, which demonstrates the property of stealthiness of the liposomes and the need to functionalize their surface. Finally, an Irinotecan liposomal nanocarrier characterized and stable was established. These findings support the platform as an emerging basis of future conjugation with any desired targeting ligand (e.g. anti-HER2 antibodies) to undergo receptor-mediated active targeting, which is a key step to improving therapeutic efficacy and specificity in oncology.
Keywords: Targeted drug delivery, Liposomes, Irinotecan hydrochloride, PEGylation, Nanomedicine, Cancer therapy
How to cite this article: Nivathra V, Singh N, Khan A, Jha P, Debbarma B, Upadhyay P, Santhoshkumar SP, Reddy BBK. Formulation and in vitro and in vivo evaluation of ligand-functionalized liposomes for targeted cancer therapy. Int J Drug Deliv Technol. 2026;16(11s): 367-378. DOI: 10.25258/ijddt.16.11s.35
Source of support: Nil.
Conflict of interest: None