Curcumin-loaded mixed micelles: preparation, optimization, physicochemical properties and cytotoxicityin vitro

Abstract

Although curcumin (CUR) can inhibit proliferation and induce apoptosis of tumors, the poor water solubility restricted its clinical application. The aim of this study was to improve the aqueous solubility of CUR and make more favorable changes to bioactivity by preparing curcumin-loaded phospholipid-sodium deoxycholate-mixed micelles (CUR-PC-SDC-MMs). CUR-PC-SDC-MMs were prepared by the thin-film dispersion method. Based on the results of single factor exploration, the preparation technology was optimized using the central composite design-response surface methodology with drug loading and entrapment efficiency (EE%) as indicators. The images of transmission electron microscopy showed that the optimized CUR-PC-SDC-MMs were spherical and well dispersed. The average size of the mixed micelles was 66.5 nm, the zeta potential was about À26.96 mV and critical micelle concentration was 0.0087 g/l. CUR was encapsulated in PC-SDC-MMs with loading capacity of 13.12%, EE% of 87.58%, and the solubility of CUR in water was 3.14 mg/ml. The release results in vitro showed that the mixed micelles presented sustained release behavior compared to the propylene glycol solution of CUR. The IC 50 values of CUR-loaded micelles and free drug in human breast carcinoma cell lines were 4.10 mg/ml and 6.93 mg/ml, respectively. It could be concluded from the above results that the CUR-PC-SDC-MMs system might serve as a promising nanocarrier to improve the solubility and bioactivity of CUR.

Optimization and anticancer activity in vitro and in vivo of baohuoside I incorporated into mixed micelles based on lecithin and Solutol HS 15

“…In previous studies, various drug delivery systems, including lecithin complexes and nanoparticles, have been developed to overcome the aforementioned limitations of baohuoside I (Jin et al, 2012a,b). Among the several micellar formulations evaluated as carriers of anticancer drugs, mixed micelles are the appropriate choice for the carriers of baohuoside I. Micellar systems have many advantages such as increasing the drug solubility, circumventing the uptake by the reticuloendothelial system (RES), improving circulation time, and passive tumor targeting by the enhanced permeability and retention (EPR) effect (Fang et al, 2011;Duan et al, 2015). In addition, mixed micelles have synergistic properties such as increased drug stability and drug loading efficiency compared with that of the individual components (Potluri & Betageri, 2006;Chen et al, 2013).…”

Zonisamide-loaded triblock copolymer nanomicelles as a novel drug delivery system for the treatment of acute spinal cord injury

“…16,17 The common advantage of these drug delivery systems is that micelles are resistant to glomerular filtration, which could extend their retention time in the blood. 18 Furthermore, micelles can facilitate the passage of drugs through the blood-brain barrier and blood-spinal cord barrier (BSCB), increasing therapeutic efficacy and safety compared to conventional pharmaceutical dosage forms. 19 There have been several reports of biodegradable polymeric micelles for SCI treatment.…”

Targeted delivery of doxorubicin and vincristine to lymph cancer: evaluation of novel nanostructured lipid carriers in vitro and in vivo

“…These data illustrated that the loading of drugs did not increase the size significantly. It has been reported that the nanoparticles with the size less than 200 nm can significantly accumulate in tumor by ''filtration'' mechanism (Xu et al, 2009;Duan et al, 2015). Small particles are also minimal endocytosis by macrophages, so destruction and clearance could be minimized, and the nanocarriers were desirable for in vitro and in vivo drug delivery (Accardo et al, 2012;Wang et al, 2013).…”