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.
Highlights
Many methods have been developed for improving the oral BA of curcumin, including adjuvant therapy with piperine, which interferes with glucuronidation metabolism, and the use of other delivery vehicles[9] such as liposomes[10], phospholipid complexes[11], and nanoparticles[12,13,14]
When a low tocopheryl polyethylene glycol succinate (TPGS) concentration was used, the micelles precipitated within 12 h even in the presence of lecithin
When the CREMOPHOR concentration was low, the micelles precipitated within 12 h even in the presence of lecithin
Summary
Many methods have been developed for improving the oral BA of curcumin, including adjuvant therapy with piperine, which interferes with glucuronidation metabolism, and the use of other delivery vehicles[9] such as liposomes[10], phospholipid complexes[11], and nanoparticles[12,13,14]. Phospholipids play a major role in nanoparticle drug delivery In addition to their solubilization property, they have numerous advantages for incorporation into a carrier system for enhancing therapeutic efficacy. The BA of curcumin-loaded phospholipid nanoparticles was 2.5 times greater than that of free curcumin These results are in concordance with those of an in vivo report revealing that curcumin-formulated PC has higher peak plasma levels and AUC values than does free curcumin[26]. Lecithin-based formulations improve the therapeutic efficacy of poor oral absorption drugs[29]. Curcumin-loaded lecithin liposomes exhibited 4-fold increased absorption (based on the AUC) compared with free curcumin in 9 healthy volunteers[30]
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