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Cancer is among the most dreadful fatal diseases globally, and the efficacy of recent chemotherapeutic approaches is limited due to many related drawbacks. The major limitation associated with cancer chemotherapy is the poor aqueous solubility of most of the anticancer drugs, development of multidrug resistance, low bioavailability, small plasma half-life, and serious side effects to healthy tissues due to unspecific distribution of chemotherapeutic drugs. Advancement in nanoscience provides the means of specific and selective targeting of cancer cells. Chitosan, one of the naturally occurring biocompatible and mucoadhesive biopolymers that have been widely used in recent years for the effective delivery of anti-cancer drugs at the target site. Chitosan nanoparticles can encapsulate both hydrophilic and lipophilic chemotherapeutic drugs, proteins/peptides as well as different genetic materials like DNA, miRNA, siRNA, etc. in their polymeric matrix. Due to the unique polymeric matrix, these nanoparticles improve the solubility as well as the stability of encapsulated molecules in the biological system. Chitosan nanoparticles can improve the pharmacokinetic profile as well as the therapeutic efficacy of encapsulated drugs by controlling the release rates and targeted delivery process. These nanoparticles selectively deliver the encapsulated drugs to desired sites through passive or active targeting mechanisms thereby decrease the undesirable side-effects. The surface of chitosan nanoparticles can be modified with different ligands like antibodies, proteins, peptides, polysaccharides, and nucleic acids to achieve selective targeting. This review will provide a state-of-the-art perspective on recent development in chitosan-nanoparticles for smart anti-cancer therapeutic delivery. [ABSTRACT FROM AUTHOR]

The major limitation with the oral administration of most of the phytochemicals is their low aqueous solubility and bioavailability. Thymoquinone (THQ) is one of the most widely used phytochemicals used to treat a variety of diseases. However, strong lipophilic characteristics limit its clinical application. Therefore, this study was aimed to design novel chitosan (C) modified polycaprolactone (PL) nanoparticles (NPs) for improved oral bioavailability of THQ. THQ-CPLNPs was optimized 33-Box-Behnken design. After that, the optimized THQ-CPLNPs was characterized by different parameters. THQ-CPLNPs showed the size, PDI, and ZP of 182.32 ± 6.46nm, 0.179 ± 0.012, and þ21.36 ± 1.22 mV, respectively. The entrapment and loading capacity were found to be 79.86 ± 4.36%, and 13.45 ± 1.38%, respectively. THQ-CPLNPs exhibited burst release in initial 2 h followed by prolonged release up to 24 h in simulated intestinal fluids. THQ-CPLNPs showed excellent mucoadhesion properties which were further confirmed with the intestinal permeation study as well as confocal microscopy. The study revealed higher permeation of THQ-CPLNPs compared to neat THQ suspension (THQ-S). Moreover, in vivo gastric irritation study revealed good compatibility of THQ-CPLNPs with the gastric mucosa. Furthermore, pharmacokinetic results depicted -3.53-fold improved oral bioavailability of THQ from THQ-CPLNPs than THQ-S. Therefore, from the findings, it was concluded that the prepared polymeric NPs could be an effective delivery system for improved oral bioavailability of THQ. [ABSTRACT FROM AUTHOR]