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Micelleplexes as nucleic acid delivery systems for cancer-targeted therapies
Miguel Pereira-Silva1, Ivana Jarak1, Carmen Alvarez-Lorenzo2
1Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra, Univ. Coimbra, Portugal.
Abstract:
Cancer remains one of the leading causes of death worldwide despite significant therapeutic advancements and improved detection methods. Nucleic acid (NA) therapeutics are receiving increasing attention for cancer management and cure. Indeed, ribonucleic acid (RNA) oligonucleotides (such as small interfering RNA (siRNA) and micro RNA (miRNA)), messenger RNA (mRNA) and deoxyribonucleic acid (DNA) (such as plasmidic DNA (pDNA) and minicircle DNA (mcDNA)), have demonstrated potential as novel therapeutic agents. The imposing prospects of NA-based therapeutics reside in their ability to act as key-players mediating cellular pathways and bestowing potent gene silencing properties, as in the case of RNA interference (RNAi) agents, or by promoting the expression of specific required proteins for disease management (pDNA, mcDNA and mRNA, for instance). However, efficient NA therapeutics delivery is seriously hampered by NA physicochemical features, low in vivo serum stability and compromised cellular internalization, which swiftly reduce their biological activities. Recently, nano-based systems emerged as suitable vehicles for NA delivery. This review covers NA-carrying micelleplexes as robust and multifunctional polymer-based NA delivery systems, as well as the specific in vivo challenges for successful NA delivery to cancer cells and their prospects to become clinical reality, followed by a critical analysis of the major in vivo micelleplex-based cancer-targeted strategies accomplished till the present day.
Insights
Nucleic acid therapeutics offer promising cancer treatments by silencing genes or expressing proteins. However, effective delivery to cancer cells remains a challenge, with nano-based micelleplexes showing potential to overcome these hurdles.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Molecular Biology
Background:
- Cancer is a leading cause of death globally, driving the need for novel therapeutic strategies.
- Nucleic acid (NA) therapeutics, including RNA and DNA, show great promise for cancer management due to their gene-modulating capabilities.
- Challenges in NA delivery, such as poor stability and cellular uptake, limit their clinical application.
Purpose of the Study:
- To review the potential of NA-based therapeutics for cancer treatment.
- To explore nano-based systems, specifically micelleplexes, as advanced delivery vehicles for NA therapeutics.
- To critically analyze in vivo micelleplex-based cancer-targeting strategies and their clinical prospects.
Main Methods:
- Review of current literature on nucleic acid therapeutics and delivery systems.
- Focus on micelleplexes as polymer-based nanocarriers for NA delivery.
- Analysis of in vivo challenges and targeted strategies for cancer therapy.
Main Results:
- NA therapeutics demonstrate potent gene silencing or protein expression for cancer management.
- Micelleplexes are identified as robust and multifunctional systems for overcoming NA delivery barriers.
- Various in vivo micelleplex-based cancer-targeting strategies have been developed.
Conclusions:
- Nano-based micelleplexes represent a promising approach to enhance the efficacy of NA therapeutics in cancer treatment.
- Addressing in vivo delivery challenges is crucial for translating these NA-based strategies into clinical reality.
- Further research into micelleplex-mediated cancer targeting holds significant potential for advancing oncology.
