Abstract
There is a pressing clinical need for advanced colon-specific local drug delivery systems that can provide major advantages in treating diseases associated with the colon, such as inflammatory bowel disease (IBD) and colon cancer. A precise colon targeted drug delivery platform is expected to reduce drug side effects and increase the therapeutic response at the intended disease site locally. In this study, we report the fabrication of hyaluronan (HA) functionalized polymeric hybrid nanoparticulate system (Cur-HA NPs) by using curcumin as a model fluorescent drug. The Cur-HA NPs were about 200–300 nm in size, −51.3 mV overall surface charge after HA functionalization, with 56.0% drug released after 72 h in simulated gastrointestinal fluids. The Cur-HA NPs did not exhibit any cytotoxicity by AlamarBlue, PicoGreen and Live/Dead assays. Following the Cur-HA NPs use on HT-29 monolayer cell cultures demonstrating, the efficacy of HA functionalization increases cellular interaction, uptake when compared to uncoated nanoparticulate system. These findings indicate that HA functionalized nano-hybrid particles are effective in delivering drugs orally to the lower gastrointestinal tract (GIT) in order to treat local colonic diseases.
Highlights
The site-specific delivery of drugs to the colon provides significant advantages in treating diseases associated with the lower gastrointestinal tract (GIT)
The curcumin-loaded hyaluronan functionalized nanoparticle (Cur-HA NPs) system was successfully synthesized by the layer-by-layer approach with the emulsification-solvent evaporation method (Figure 1A,B)
Nanoparticles allow for a certain amount of protection for the entrapped compound during GI passage, polymeric particles alone, such as poly (lactide-co-glycolide) acid (PLGA), are unable to resist release within the small intestines, and an uncontrollable drug release frequently occurs before particles arrive at their intended destination
Summary
The site-specific delivery of drugs to the colon provides significant advantages in treating diseases associated with the lower gastrointestinal tract (GIT). Colon-targeted dosage form with local onsite delivery and an appropriate release pattern could be very useful for designing advanced drug delivery technologies for IBD therapy [1,2]. Disadvantages in terms of the inability to target the drugs directly at the diseased tissue, with limited therapeutic efficacy and a high risk of adverse drug reactions make the conventional strategies replaceable [4]. Henceforward, strategies or mechanisms are in the developmental stages during which a payload is delivered by the use of pathophysiological parameters that are directly related to the site of colon inflammation and cancer, which has to be investigated in order to make advanced effective pharmaceutical dosage forms
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