Folic acid conjugated chitosan nanoparticles for tumor targeting of therapeutic and imaging agents

Anticancer drugs are typically distributed non-specifically in the body, where they affect both cancerous and normal cells. This limits the drug level achievable within the tumor, compromising the therapeutic efficacy, and results in potential toxic effects on normal tissues. Targeted delivery of chemotherapeutics exclusively to cancer cells is the focus of intensive research for improvement of anticancer therapy. Various drug delivery systems have been investigated for this purpose, with therapeutic-carrying polymeric nanoparticulate systems designed for specific targeting of tumor cells receiving special interest. Chitosan, a natural polymer derived from crustacean shells, has attracted particular attention as a drug carrier. The simple and mild preparation methods, low toxicity, good stability, controlled drug release and the ability to overcome biological barriers has made chitosan-based nanoparticles popular in drug and gene delivery applications. Chitosan nanoparticles have been fabricated with optimal size and surface characteristics in order to tailor the behavior within the biological system, including circulation time, as well as passive and active cancer targeting. Folic acid is widely employed as a ligand targeting cancerous cells as its receptor which 'shuttles' folic acid into the cells via endocytosis is over-expressed on the surface of many human epithelial cancer cells. Incorporating folic acid into chitosan-based drug and gene delivery formulations renders the systems with an efficient targeting capacity. Furthermore, it is possible to formulate chitosan nanocarriers that display multiple useful characteristics extending beyond targeted delivery. The versatility of these systems is also being exploited in nanotheranostics.</p

Folic acid conjugated chitosan nanoparticles for tumor targeting of therapeutic and imaging agents

Anticancer drugs are typically distributed non-specifically in the body, where they affect both cancerous and normal cells. This limits the drug level achievable within the tumor, compromising the therapeutic efficacy, and results in potential toxic effects on normal tissues. Targeted delivery of chemotherapeutics exclusively to cancer cells is the focus of intensive research for improvement of anticancer therapy. Various drug delivery systems have been investigated for this purpose, with therapeutic-carrying polymeric nanoparticulate systems designed for specific targeting of tumor cells receiving special interest. Chitosan, a natural polymer derived from crustacean shells, has attracted particular attention as a drug carrier. The simple and mild preparation methods, low toxicity, good stability, controlled drug release and the ability to overcome biological barriers has made chitosan-based nanoparticles popular in drug and gene delivery applications. Chitosan nanoparticles have been fabricated with optimal size and surface characteristics in order to tailor the behavior within the biological system, including circulation time, as well as passive and active cancer targeting. Folic acid is widely employed as a ligand targeting cancerous cells as its receptor which 'shuttles' folic acid into the cells via endocytosis is over-expressed on the surface of many human epithelial cancer cells. Incorporating folic acid into chitosan-based drug and gene delivery formulations renders the systems with an efficient targeting capacity. Furthermore, it is possible to formulate chitosan nanocarriers that display multiple useful characteristics extending beyond targeted delivery. The versatility of these systems is also being exploited in nanotheranostics.</p

Correlation among chemical structure, surface properties and cytotoxicity of N-acyl alanine and serine surfactants

Toxicity is one of the main concern limiting the use of surfactants. Many efforts have been devoted to the development of new amphiphilic molecules characterized by a lower toxicological profile and environmental impact. N-acyl amino acids are a class of anionic surfactants that can find applications in different technological fields as an alternative to sulphate-based surfactants (e.g., sodium dodecyl sulphate).The understanding of the relationship between chemical structure and toxicological profile is fundamental for the disclosure of the full potential of these amphiphiles. With this aim, two series of N-acyl surfactants, with different length of the hydrophobic tails and serine or alanine as polar head, were synthesized and fully characterized.The correlation between the surface and toxicological parameters allowed highlighting the role exerted by the length of the hydrocarbon chain and the polar head on cytotoxicity. The length of the hydrocarbon chain mainly influences surface properties and toxicological parameters, while the amino acid polar head plays a key role only on cellular toxicity. Overall, our data suggest that minor differences in the polar head, not affecting significantly CMC values, may have a strong impact on cytotoxicity.</p

Correlation among chemical structure, surface properties and cytotoxicity of N-acyl alanine and serine surfactants

Toxicity is one of the main concern limiting the use of surfactants. Many efforts have been devoted to the development of new amphiphilic molecules characterized by a lower toxicological profile and environmental impact. N-acyl amino acids are a class of anionic surfactants that can find applications in different technological fields as an alternative to sulphate-based surfactants (e.g., sodium dodecyl sulphate).The understanding of the relationship between chemical structure and toxicological profile is fundamental for the disclosure of the full potential of these amphiphiles. With this aim, two series of N-acyl surfactants, with different length of the hydrophobic tails and serine or alanine as polar head, were synthesized and fully characterized.The correlation between the surface and toxicological parameters allowed highlighting the role exerted by the length of the hydrocarbon chain and the polar head on cytotoxicity. The length of the hydrocarbon chain mainly influences surface properties and toxicological parameters, while the amino acid polar head plays a key role only on cellular toxicity. Overall, our data suggest that minor differences in the polar head, not affecting significantly CMC values, may have a strong impact on cytotoxicity.</p