Development and Characterization of Lecithin-based Self-assembling Mixed Polymeric Micellar (saMPMs) Drug Delivery Systems for Curcumin

Abstract

Self-assembling mixed polymeric micelles (saMPMs) were developed for overcoming major obstacles of poor bioavailability (BA) associated with curcumin delivery. Lecithin added was functioned to enlarge the hydrophobic core of MPMs providing greater solubilization capacity. Amphiphilic polymers (sodium deoxycholate [NaDOC], TPGS, CREMOPHOR, or a PLURONIC series) were examined for potentially self-assembling to form MPMs (saMPMs) with the addition of lecithin. Particle size, size distribution, encapsulation efficacy (E.E.), and drug loading (D.L.) of the mixed micelles were optimally studied for their influences on the physical stability and release of encapsulated drugs. Overall, curcumin:lecithin:NaDOC and curcumin:lecithin:PLURONIC P123 in ratios of 2:1:5 and 5:2:20, respectively, were optimally obtained with a particle size of < 200 nm, an E.E. of >80%, and a D.L. of >10%. The formulated system efficiently stabilized curcumin in phosphate-buffered saline (PBS) at room temperature or 4 °C and in fetal bovine serum or PBS at 37 °C and delayed the in vitro curcumin release. In vivo results further demonstrated that the slow release of curcumin from micelles and prolonged duration increased the curcumin BA followed oral and intravenous administrations in rats. Thus, lecithin-based saMPMs represent an effective curcumin delivery system, and enhancing BA of curcumin can enable its wide applications for treating human disorders.

Curcumin-Loaded Mixed Micelles: Preparation, Characterization, and In Vitro Antitumor Activity

“…It could be concluded from abovementioned results that most of curcumin was embedded in the hydrophobic core by hydrophobic interaction or hydrogen bonds, and the curcumin in the surface of the particles was little [19]. e released mechanism of curcumin from micelles might be related to the drug di usion and the disintegration of the polymer material [27]. Curcumin was physically entrapped in the hydrophobic core of the mixed micelles that restricts its release from the micelles.…”

An integrated vitamin E-coated polymer hybrid nanoplatform: A lucrative option for an enhanced in vitro macrophage retention for an anti-hepatitis B therapeutic prospect

“…PLGA, a synthetic polyester, approved by US FDA and European Medicine Agency for human use has been extensively investigated in the fabrication of LPH [28]. Lecithin (LEC) is a type of phospholipids which are vital components of the cell membrane to conserve membrane fluidity [29]. Generally, phospholipids play a crucial role in solubilization, sustainment of drug release, improvement of therapeutic efficacy and biocompatibility [30,31].…”

Orthogonal self-assembly of an organoplatinum(II) metallacycle and cucurbit[8]uril that delivers curcumin to cancer cells

“…Despite the recent advances in cancer research, how to improve the water solubility of hydrophobic drugs such as paclitaxel, curcumin (Cur), camptothecin, tamoxifen, and others is still a formidable challenge (23)(24)(25)(26)(27). Various nanocarriers including nanostructures (28)(29)(30)(31), conjugates (32)(33)(34), hydrogels (35), carbon nanomaterials (36), and so on have been developed to overcome this problem. Likewise, the solubility, stability, and bioavailability of anticancer drugs have been significantly improved in physiological environments via host-guest complexations (37)(38)(39)(40).…”