Design and Development of Microparticulate Delivery System for Curcumin

Background: Curcumin has been associated with remarkable beneficial effects; despite having a broad spectrum of activities, curcumin is characterized by poor water solubility and low bioavailability. Objective: The objective of this study is to enhance the solubility of curcumin using polyethylene glycol 400 (PEG400) and establish a microparticulate drug delivery system in a sodium alginate polymer matrix (microspheres containing curcumin triturated with PEG400 [Cur‑PEGMS]) to improve the bioavailability of curcumin. Materials and Methods: The microspheres were formulated using the ionic gelation technique. Nine batches (F1 to F9) were prepared using 32 factorial design. The amount of sodium alginate and calcium chloride was selected as a formulation variable. The prepared Cur‑PEGMS were characterized by Fourier‑transform infrared spectroscopy, scanning electron microscope, differential scanning calorimeter, ultraviolet spectrophotometer, and high‑performance thin‑layer chromatography (HPTLC). The pharmacokinetics of curcumin was characterized in rats using high‑performance liquid chromatography, and calculations were performed using WinNonlin standard edition version 1.1 software. Results: We found that solubility was affected by the use of cosolvent. All F1–F9 batches were investigated for entrapment efficiency, and batch F5 was found to be optimum batch which was further evaluated. HPTLC chromatogram of Cur‑PEGMS shows peak retention for curcumin. The particle size of microspheres was found to be in the range of 384–468 μm. Remarkable improvement in maximum plasma concentration and bioavailability was observed. Maximum the time after administration of a drug when maximum plasma concentration is reached (Tmax) was found to be 0.5 h, and AUC0–24 was found to be 374.75 ng/ml and 622 ng/ml for curcumin suspension and curcumin microspheres, respectively. Conclusion: The developed formulation enhances the bioavailability of the drug. This enhanced oral absorption of Cur‑PEGMS may provide a practical formulation to conduct a correlative pharmacodynamic study.