In the present work, a simple method was used to develop composite curcumin-amine functionalized mesoporous silica nanoparticles (MSN). The nanoparticles were used to improve the bioavailability of curcumin in mice through oral administration. We investigated the effect of particle size on the release profile, solubility and oral bioavailability of curcumin in mice, including amine functionalized mesoporous silica micron-sized-particles (MSM) and MSN (100-200 nm). Curcumin loaded within amine functionalized MSN (MSN-A-Cur) had a better release profile and a higher solubility compared to amine MSM (MSM-A-Cur). The bioavailability of MSN-A-Cur and MSM-A-Cur was considerably higher than that of 'free curcumin'. These results indicate promising features of amine functionalized MSN as a carrier to deliver low solubility drugs with improved bioavailability via the oral route.

Curcumin, well-known polyphenol drug shows great promise as a therapeutic agent. However, a major concern for this molecule is its low bioavailability. We have recently reported the use of mesoporous silica nanoparticles (MSN) to enhance curcumin bioavailability significantly. In the present work, we investigated anti-inflammatory effects of the curcumin-MSN and related side effects caused to the gastrointestinal tract and kidney, compared with curcumin and diclofenac sodium. The anti-inflammatory effect tests were performed by induction of carrageenan in Wistar rat feet. Ulcerogenic observations were performed macroscopically and microscopically. Kidney histopathology were performed on the average number of necrotic cells of the proximal tubule and distal tubules. There was anti-inflammatory activity in the administration of peroral curcumin and curcumin-MSN, in the absence of significant macroscopic and microscopic changes in the stomach organ. Curcumin-MSN showed a high anti-inflammatory activity comparable to diclofenac sodium but with a significantly enhanced biocompatibility.

Mesoporous silica nanoparticles (MSN) with large surface areas and pore volumes show great potential as drug and gene carriers. However, there are still some challenging issues hinders their clinical application. Many types of research in the use of mesoporous silica material for drug and gene delivery involving complex and rigorous procedures. A facile and reproducible procedure to prepare combined drug carrier is required.We investigated the effect of physiochemical parameters of mesoporous silica, including structural symmetry (cubic and hexagonal), particles size (micro size: 1-2 µm and nano size: 100 -300 nm), on the solubility and release profile of curcumin. Transmission Electron Microscopy, X-Ray Powder Diffraction, and Nitrogen sorption were used to confirm the synthesis of the mesoporous silica materials. Mesoporous silica materials with different mesostructures and size have been synthesized successfully. Curcumin has anti-oxidant, anti-inflammation and antivirus properties which are beneficial to fight various diseases such as diabetic, cancer, allergic, arthritis and Alzheimer. Curcumin has low solubility which minimizes its therapeutic effect. The use of nanoporous material to carry and release the loaded molecules is expected to enhance curcumin solubility. Mesoporous silica materials with a cubic mesostructure had a higher release profile and curcumin solubility, while mesoporous silica materials with a particle size in the range of nano meter (100-300) nm also show better release profile and solubility.

It has been reported that curcumin has a hepatoprotective effect, but its low solubility limited its utilization. Recently there was so many emerging research of advanced curcumin formulation, such as nanoparticles curcumin. In our previous study, curcumin has been loaded into mesoporous silica nanoparticles (C-MSN). This study was performed to evaluate of C-MSN hepatoprotective effect in CCl4-induced rats. Sixteen rats were divided into four groups, namely normal and CCl4 control, curcumin, C-MSN group. Treatment was given according to its group for fourteen days consecutively. At day 14, three hours after the last administration, CCl4 (1.25mL/kgBB) were administered orally. Twelve hours later the rats were sacrificed, and blood samples were drawn from their hearts. Blood serum examination result revealed that C-MSN caused a significantly lower ALT and AST than CCl4 control group (851±271U/L vs 1734±275U/L; 295±155U/L vs 1348±235U/L; p<0.05). Its effect on hepatic serum level resembled curcumin group. However, the result was not supported by histology examination which showed a higher number of necrotic hepatic cells in C-MSN group than in the curcumin group (147±9 vs 80±16; p<0.05). From this study, it can be concluded that C-MSN revealed an excellent hepatoprotective property, but it was suspected that MSN itself has the toxic effect on the liver. A further study of MSN toxicity was needed to support its safety use.

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