Study On Intestinal Targeted Oral Delivery System For Curcumin

Inflammatory bowel disease(IBD),including ulcerative colitis and Crohn’s disease,is a chronic,relapsing and medically incurable inflammatory disorders of the intestine,and has gradually developed into a worldwide problem in recent years.Current available drugs for IBD therapy include aminosalicylates,corticosteroids,antibiotics and immunosuppressive agents,however,administration of high dose these drugs can lead to severe side effects.Therefore,anti-inflammatory active ingredient from natural source can effectively resolve this problem.Curcumin,extracted form rhizomes of turmeric(Curcuma longa),is a natural polyphenol compound.Studies suggests that curcumin possesses a series of pharmacological activities such as antioxidant,anti-inflammatory and anti-tumor et al.Despite its potential advantages,the application of curcumin is strictly limited due to poor water-solubility.Nanoparticle drugs delivery systems have been widely applied into IBD because of their preferential accumulation in the area of inflamed intestine.Design of nanocarrier utilizing the difference between gastrointestinal tract and between healthy tissue and inflamed tissue of intestine can greatly improve bioavailability of active ingredient,which provide a broad promising therapeutic perspective for IBD.In this paper,in order to improve the bioavailability of anti-inflammatory active ingredient curcumin,different curcumin loaded nanocomplexes were prepared and made some basic characterizations.This study is aimed at improving the solubility of curcumin and providing an idea for IBD therapy.The research content includes the following two parts:In the first part,curcumin loaded casein/pectin nanocomplexes were prepared and a series of physical and chemical properties were characterized.The results showed that curcumin loaded nanocomplexes had the smallest particle size and the highest encapsulation efficiency at p H 4.Under this condition,the particle size of nanocomplexes was 266.4 nm,the encapsulation efficiency was as high as 93.04%,and the morphology was regularly spherical-like.Fourier transform infrared(FT-IR)spectroscopy revealed that curcumin was successfully encapsulated into casein/pectin nanocomplexes.Differential scanning calorimetry(DSC)results showed that curcumin is in an amorphous form,rather than the form of crystals.In vitro drug release experiments showed that the nanocomplexes exhibited sustained release in the gastrointestinal tract.In the second part,we use anthocyanin/chondroitin sulfate as the carrier material to load curcumin by a simple mixing method.The characterization of physical and chemical properties showed that when the concentration ratio of anthocyanin: curcumin:chondroitin sulfate was 4: 1: 4,curcumin loaded anthocyanin/chondroitin sulfate nanocomplexes showed smaller particle size(253.7 nm),minimum potential(-48.5 m V),and had narrow size distribution.Meanwhile,the morphology of curcumin loaded nanocomplexes was spherical.Fluorescence spectroscopy results indicated that there was an interaction between curcumin and anthocyanin.In vitro drug release results demonstrated that curcumin loaded nanocomplexes exhibits a significant release of curcumin dependent on the concentration of hydrogen peroxide.Combining the above two parts of the research,preparation of nanoparticles with stimulating materials to encapsulate the hydrophobic active ingredient curcumin can greatly improve the solubility of curcumin and providing an effective method for the therapy of IBD.