Self-microemulsifying drug delivery system of curcumin with enhanced solubility and bioavailability using a new semi-synthetic bicephalous heterolipid: in vitro and in vivo evaluationElectronic supplementary information (ESI) available. See DOI: 10.1039/c5ra18112g

• Main Authors: Dhumal, Dinesh M, Kothari, Priya R, Kalhapure, Rahul S, Akamanchi, Krishnacharya G
• Format: Article
• Language: English
• ISSN: 2046-2069
• DOI: 10.1039/c5ra18112g

Despite the various therapeutic actions displayed by curcumin, its poor aqueous solubility and bioavailability restricts its biological applications. This problem can be addressed by its efficient loading into a nano formulation. The present paper reports the utilization of a new semi-synthetic oleic acid derived bicephalous heterolipid, E1E, as an oil phase in the formulation development of a self-microemulsifying drug delivery system (SMEDDS) of curcumin to enhance its solubility and bioavailability. The solubility of curcumin in E1E was found to be 14 and 2.6-fold greater than oleic acid and ethyl oleate respectively. The SMEDDS developed from E1E (Curcumin-E1E_SMEDDS5e) had high curcumin loading efficiency of 70.52 ± 2.46 mg g −1 , and was able to form spontaneous microemulsion on addition to aqueous phase with mean globule diameter of 22.39 ± 0.2 nm and polydispersity index of 0.243 ± 0.010. In vivo oral bioavailability studies in male Wistar rats revealed that the maximum serum concentration ( C max ) and time taken to reach maximum serum concentration ( T max ) were 4.921 ± 0.42 μg mL −1 and 60 min respectively. The absorption of curcumin increased 26-folds via its delivery through Curcumin-E1E_SMEDDS5e. The cytostatic and total growth inhibition concentrations of Curcumin-E1E_SMEDDS5e against HeLa cell line were almost comparable to doxorubicin (GI 50 and TGI < 10 μg mL −1 ) whereas lethal concentration (LC 50 ) was 71.8 μg mL −1 . Further, the minimum inhibitory concentrations against E. coli and S. aureus were 48.62 and 97.65 μg mL −1 respectively. These results suggested potent anticancer, antibacterial activity and non-cytotoxicity of developed Curcumin-E1E_SMEDDS5e. The heterolipid, E1E, proved to be an efficient solubility and bioavailability enhancer for curcumin for formulation development of its SMEDDS. Curcumin SMEDDS from heterolipid E1E.