Linear-dendrimer type methoxy-poly (ethylene glycol)-b-poly (ɛ-caprolactone) copolymer micelles for the delivery of curcumin

Abstract

(2015) Linear-dendrimer type methoxy-poly (ethylene glycol)-b-poly (ɛ-caprolactone) copolymer micelles for the delivery of curcumin, Drug Delivery, 22:1, 58-68, DOI: 10.3109/10717544.2014 Methods: A novel linear-dendrimer methoxy-poly (ethylene glycol)-b-poly ("-caprolactone) copolymer was synthesized through O-alkylation, basic hydrolysis and ring-opening polymerization reaction with methoxy-poly (ethylene glycol), epichlorohydrin and "-caprolactone as raw materials. Its structure was characterized by 1 H-NMR and GPC. The copolymer's hemolysis and micellar encapsulation for curcumin by thin-film hydration were studied. Curcumin-loaded micelles were evaluated by use of in vitro release, FT-IR and X-ray diffraction. Curcumin-loaded micelles' in vitro cytotoxic activities against Hela and HT-29 cells were done, and its pharmacokinetic parameters were also carried out. Results: Curcumin was encapsulated into the micelles with 92.54% of entrapment efficiency and 12.84% of drug loading in amorphous forms. The dissolubility of nanoparticulate curcumin was 1.70 Â 10 5 times higher than that of curcumin in water. The obtained copolymer showed no hemolysis. In vitro drug release study indicated that, in all cases, the kinetics was adjusted well to the Makoid-Banakar model (R 2 abj ¼ 0.9984). In addition, data were analyzed by the Korsmeyer-Peppas model, n values were 0.43, indicating that the drug release was accomplished by the combination diffusion and polymer chain relaxation. The cytotoxicity experiment indicated that the nanoparticulate curcumin kept up its potent anti-cancer activities. The pharmacokinetic results showed that the MRT 0-1 , t 1/2z and AUC 0-1 of Curcuminloaded micelles were 1.64, 6.54 and 4.67 times higher than that of CUR control solution. Conclusions: The copolymeric micelles loading curcumin might act as a delivery vehicle for CUR.

A novel curcumin-loaded nanoparticle restricts atherosclerosis development and promotes plaques stability in apolipoprotein E deficient mice

“…The curcumin-loaded NPs (Cur-NPs) of small size were obtained from the copolymer’s self-assembling aided by thin-film hydration with effective encapsulation. 10 Our results demonstrated that Cur-NPs can significantly raise dissolution ratio of curcumins in water, providing a proper sustained-release characteristic for curcumin in vitro, suggesting that the Cur-NP is an appropriate candidate for the continuous delivery of curcumin. In the current study, we further evaluated the anti-atherosclerotic function of this Cur-NPs in apolipoprotein E −/− mice (apoE −/− mice).…”

“…Moreover, the release behavior of curcumin from the nanoparticle has been investigated in our previous studies. 10 The release results demonstrated that the release of curcumin from control solution was much faster, about 87% of curcumin was released in 20 h. In contrast, the Cur-NPs showed a sustained-release property and the accumulative release percentage at 60 h was about 81%. These results suggested that Cur-NPs would have a prospective clinical application as a new injectable dosage form.…”

<p>Pharmacokinetic studies of nanoparticles as a delivery system for conventional drugs and herb-derived compounds for cancer therapy: a systematic review</p>

“…These results suggested that LNC could be used for the delivery of traditional medicines to cancer cells. The methoxy poly(ethylene glycol)-b-poly(ε-caprolactone) (mPEG-PCL) micelles could extend the plasma concentration and delay the clearance of curcumin 38. The bioavailability and t 1/2 of curcumin were greatly improved when loaded with Poly (D, L-lactic acid)-glycerol (PDLLA-G) when compared with free curcumin 39…”

Targeted delivery of etoposide to cancer cells by folate-modified nanostructured lipid drug delivery system

“…In vitro ETP release from FA-ETP-NLCs and ETP-NLCs was assessed by the dialysis method (Song et al, 2015). FA-ETPNLCs and ETP-NLCs were positioned in the dialysis bag separately.…”