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Retinoids Delivery Systems in Cancer: Liposomal Fenretinide for Neuroectodermal-Derived Tumors
Veronica Bensa1, Enzo Calarco1, Elena Giusto1
1Laboratory of Experimental Therapies in Oncology, IRCCS Istituto Giannina Gaslini, 16147 Genoa, Italy.
Abstract:
Retinoids are a class of natural and synthetic compounds derived from vitamin A. They are involved in several biological processes like embryogenesis, reproduction, vision, growth, inflammation, differentiation, proliferation, and apoptosis. In light of their important functions, retinoids have been widely investigated for their therapeutic applications. Thus far, their use for the treatment of several types of cancer and skin disorders has been reported. However, these therapeutic agents present several limitations for their widespread clinical translatability, i.e., poor solubility and chemical instability in water, sensitivity to light, heat, and oxygen, and low bioavailability. These characteristics result in internalization into target cells and tissues only at low concentration and, consequently, at an unsatisfactory therapeutic dose. Furthermore, the administration of retinoids causes severe side-effects. Thus, in order to improve their pharmacological properties and circulating half-life, while minimizing their off-target uptake, various retinoids delivery systems have been recently developed. This review intends to provide examples of retinoids-loaded nano-delivery systems for cancer treatment. In particular, the use and the therapeutic results obtained by using fenretinide-loaded liposomes against neuroectodermal-derived tumors, such as melanoma, in adults, and neuroblastoma, the most common extra-cranial solid tumor of childhood, will be discussed.
Insights
Retinoids, vitamin A derivatives, show therapeutic promise but face delivery challenges. Novel nanodelivery systems, like fenretinide-loaded liposomes, improve treatment for cancers such as melanoma and neuroblastoma.
Area of Science:
- Biochemistry and Molecular Biology
- Pharmacology and Pharmaceutical Sciences
- Oncology
Background:
- Retinoids, derived from vitamin A, regulate critical biological processes including cell differentiation and apoptosis.
- Retinoids exhibit therapeutic potential in treating cancers and skin disorders.
- Current retinoid therapies are limited by poor solubility, chemical instability, low bioavailability, and severe side effects.
Purpose of the Study:
- To review retinoid-loaded nanodelivery systems for enhanced cancer treatment.
- To highlight the therapeutic efficacy of fenretinide-loaded liposomes against neuroectodermal tumors.
Main Methods:
- Literature review of retinoid applications and nanodelivery systems.
- Focus on liposomal formulations of fenretinide for targeted cancer therapy.
- Analysis of therapeutic outcomes in preclinical and clinical studies.
Main Results:
- Nanodelivery systems significantly improve retinoid solubility, stability, and bioavailability.
- Fenretinide-loaded liposomes demonstrate promising therapeutic results against melanoma and neuroblastoma.
- Reduced off-target effects and improved drug concentration at tumor sites were observed.
Conclusions:
- Retinoid-loaded nanodelivery systems offer a viable strategy to overcome limitations of conventional retinoid therapy.
- Liposomal fenretinide represents a promising approach for treating neuroectodermal-derived cancers in adults and children.
- Further research into nanodelivery systems can optimize retinoid-based cancer treatments.
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