Ligand-functionalized nanoliposomes for targeted delivery of galantamine
Abstract
The purpose of this study was to design ligand-functionalized nanoliposomes that are proficient in providing effective intracellular delivery of an alkaloid drug (galantamine) into PC12 neuronal cells in response to managing Alzheimer's disease (AD). Ligand-functionalized nanoliposomes were produced and validated for their physicochemical properties, in silico molecular mechanics energy relationships, ex vivo cytotoxicity, peptide coupling efficiency (PCE), drug entrapment efficiency (DEE), drug release, fluorometry and confocal microscopy. Particle sizes of the nanoliposomes ranged from 127 nm to 165 nm (PdI=0.39-0.03), zeta potential values of -18 mV to -36 mV, PCE from 40% to 78% while DEE ranged from 42% to 79%. The surface morphology of the nanoliposomes was stable, spherically and uniform in shape. Thermal behavior and Fourier transform infrared (FTIR) analyses confirmed that galantamine and the peptide-ligand were incorporated into the inner core and surface of the nanoliposomes, respectively. The optimized formulation showed sustained drug release (30% of drug released within 48 h). Fluorometry and confocal microscopy revealed that the ligand-functionalized nanoliposomes facilitated galantamine uptake into PC12 neuronal cells via the Serpin Enzyme Complex Receptor in a mediated manner. CytoTox-Glo™ cytotoxicity assay established the low cytotoxicity on PC12 neuronal cells when exposed to native nanoliposomes and the ligand-functionalized nanoliposomes. Response surface analysis demonstrated there was a high degree of correlation between the experimental and fitted values. Furthermore, ex vivo studies showed that the high galantamine accumulation into PC12 neuronal cells was influenced by the post-engineering of peptides on the surface of the galantamine-loaded nanoliposomes. MMER analysis aptly corroborated the experimental findings.
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PEGylated nanoliposomes and SLNs loaded with galantamine and memantine showed increased brain-targeted delivery with neuroprotective properties.
“PEGylated nanolipsomes and SLNs loaded with galantamine105 and memantine106 showed increased brain-targeted delivery with neuroprotective properties.106”
From Targeted therapy in chronic diseases using nanomaterial-based drug delivery vehicles (2019) · cites this paper as [105]
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Targeted therapy in chronic diseases using nanomaterial-based drug delivery vehicles
Singh, A. P., Biswas, A., Shukla, A., & Maiti, P. (2019) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-019-0068-3 · Cited by 645 · see citing works
Kochman, U., Sitka, H., Kuźniar, J., Czaja, M., Kozubek, P., Beszłej, J. A., & Leszek, J. (2026) · Molecular Neurobiology · doi:10.1007/s12035-025-05417-z · Cited by 60 · see citing works
- Authors
- Mufamadi, M. S., Choonara, Y. E., Kumar, P., Modi, G., Naidoo, D., van Vuuren, S., Ndesendo, V. M. K., Toit, L. C. D., Iyuke, S. E., & Pillay, V.
- Affiliations
- University of the Witwatersrand (ZA)
- St. John's University of Tanzania (TZ)
- Corresponding author
- Pillay, Viness
- ORCID
- Venue
- International Journal of Pharmaceutics
- Publisher
- Elsevier BV
- Published
- 2013-05
- Volume
- 448
- Issue
- 1
- Pages
- 267-281
- ISSN
- 0378-5173 (ISSN-L)
- OpenAlex
- W1986797776
- Cited by
- 51
- References
- 64
- Citations by year
- 2026: 3 · 2025: 3 · 2024: 4 · 2023: 2 · 2022: 4 · 2021: 6 · 2020: 5 · 2019: 7 · 2018: 2 · 2017: 4 · 2016: 6 · 2015: 5
- FWCI
- 1.40
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- International Journal of Pharmaceutics (publishedVersion)
- PubMed (publishedVersion)
- Nelson Mandela University Research Repository (submittedVersion)
- Funders
- National Research Foundation
- U.S. Food and Drug Administration
- Topics
- Physical Sciences › Materials Science › Biomaterials › Nanoparticle-Based Drug Delivery
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › RNA Interference and Gene Delivery
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Keywords
- galantamine, targeted drug delivery, Alzheimer's disease, intracellular drug delivery, sustained drug release, encapsulation efficiency, cytotoxicity, response surface optimization
- MeSH terms
- Animals, Galantamine, Ligands, Lipids, Liposomes, Oligopeptides, Surface Properties, PC12 Cells, Nootropic Agents, Microscopy, Electron, Transmission, Rats, Nanoparticles
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