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Published on: April 26, 2016
Antineoplastics Encapsulated in Nanostructured Lipid Carriers
Gustavo Henrique Rodrigues da Silva1, Ludmilla David de Moura1, Fabíola Vieira de Carvalho1
1Department of Biochemistry and Tissue Biology, Institute of Biology, University of Campinas-UNICAMP, Campinas 13083-862, Brazil.
Abstract:
Ideally, antineoplastic treatment aims to selectively eradicate cancer cells without causing systemic toxicity. A great number of antineoplastic agents (AAs) are available nowadays, with well-defined therapeutic protocols. The poor bioavailability, non-selective action, high systemic toxicity, and lack of effectiveness of most AAs have stimulated the search for novel chemotherapy protocols, including technological approaches that provide drug delivery systems (DDS) for gold standard medicines. Nanostructured lipid carriers (NLC) are DDS that contain a core of solid and lipid liquids stabilised by surfactants. NLC have high upload capacity for lipophilic drugs, such as the majority of AAs. These nanoparticles can be prepared with a diversity of biocompatible (synthetic or natural) lipid blends, administered by different routes and functionalised for targeting purposes. This review focused on the research carried out from 2000 to now, regarding NLC formulations for AAs (antimetabolites, antimitotics, alkylating agents, and antibiotics) encapsulation, with special emphasis on studies carried out in vivo. NLC systems for codelivery of AAs were also considered, as well as those for non-classical drugs and therapies (natural products and photosensitisers). NLC have emerged as powerful DDS to improve the bioavailability, targeting and efficacy of antineoplastics, while decreasing their toxic effect in the treatment of different types of cancer.
Insights
Nanostructured lipid carriers (NLC) offer improved cancer treatment by enhancing antineoplastic agent (AA) delivery. These advanced drug delivery systems (DDS) boost efficacy and targeting while reducing systemic toxicity in chemotherapy.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Pharmacology
Background:
- Current antineoplastic agents (AAs) often suffer from poor bioavailability, systemic toxicity, and lack of selectivity.
- Novel drug delivery systems (DDS) are crucial for improving chemotherapy efficacy and patient outcomes.
- Nanostructured lipid carriers (NLC) are promising DDS with high drug loading capacity for lipophilic AAs.
Purpose of the Study:
- To review research on NLC formulations for antineoplastic agents (AAs) from 2000 to the present.
- To evaluate the in vivo efficacy and safety of NLC-based DDS for cancer therapy.
- To explore NLC applications in codelivery and for non-classical anticancer therapies.
Main Methods:
- Systematic literature review of NLC formulations for AAs (antimetabolites, antimitotics, alkylating agents, antibiotics).
- Focus on in vivo studies assessing efficacy, biodistribution, and toxicity.
- Inclusion of studies on NLC for codelivery and alternative anticancer agents.
Main Results:
- NLC demonstrate high encapsulation efficiency for various lipophilic AAs.
- In vivo studies show enhanced tumor targeting, improved bioavailability, and increased efficacy of AAs delivered via NLC.
- NLC formulations have shown reduced systemic toxicity compared to conventional AA administration.
- NLC are effective for codelivery of multiple AAs and for delivering natural products and photosensitizers.
Conclusions:
- Nanostructured lipid carriers (NLC) represent a powerful drug delivery system (DDS) for enhancing antineoplastic agent (AA) therapy.
- NLC improve the bioavailability, targeting, and efficacy of AAs while mitigating their toxic side effects.
- NLC hold significant potential for advancing cancer treatment through improved drug delivery strategies.

