New Insights of Turmeric Extract-Loaded PLGA Nanoparticles: Development, Characterization and In Vitro Evaluation of Antioxidant Activity.

Here, we presented new insights of the development of poly(lactic-co-glycolic acid) nanoparticles containing turmeric compounds (turmeric-PLGA-NPs) using emulsion-solvent evaporation method. The nanoparticulate system was characterized by size, zeta potential, morphology, release profile, partition parameter, stability and encapsulation efficiency (%EE). Antioxidant activity studies were also evaluated. The Korsmeyer-Peppas model (Mt/M∞ vs. t) was used to determine the release mechanisms of the studied system. Our results demonstrated the emulsion-solvent evaporation method was shown advantageous for producing turmeric-PLGA-NPs in the range of 145 nm with high homogeneity in size distribution, zeta potential of -21.8 mV and %EE about 72%. Nanoparticles were stable over a period of one month. In vitro study showed a release of curcumin governed by diffusion and relaxation of the polymeric matrix. The partition parameter of the extract in relation to blank-PLGA-NPs was 0.111 ± 0.008 M-1, indicating a low affinity of curcumin for the polymer matrix. Antioxidant ability of the turmeric-PLGA-NPs in scavenging the radical 2,2-azinobis (3-ethylbenzothiazoline- 6-sulfonic acid) (ABTS) was inferior to free turmeric extract and showed a concentration and time-dependent profile. The study concluded that PLGA nanoparticles are potential carriers for turmeric extract delivery.

Nanoemulsion as a Platform for Iontophoretic Delivery of Lipophilic Drugs in Skin Tumors.

Lipophilic drugs do not usually benefit from iontophoresis mainly because they do not solubilize in aqueous formulations suitable for the application of electric current. To explore the influence of iontophoresis on penetration of these drugs, a cationic nanoemulsion was developed to solubilize zinc phthalocyanine (ZnPc), a promising drug for the treatment of skin cancer. To verify the influence of particle size on iontophoresis, an emulsion of nanoemulsion-like composition was also developed. The formulations were characterized and cutaneous and tumor penetration studies were performed in vitro and in vivo, respectively. With particles of about 200 nm, the nanoemulsion solubilized 2.5-fold more ZnPc than the 13-µm emulsion. At the same concentration of ZnPc, in vitro passive penetration studies showed that the nanoemulsion increased, after 1 h of treatment, by almost 4 times the penetration of ZnPc into the viable layers of the skin when compared to the emulsion, whereas iontophoresis of nanoemulsion resulted in a 16-fold increase in ZnPc penetration in only 30 min. An in vivo study in a murine model of melanoma showed that ZnPc reached the tumor after iontophoresis of the nanoemulsion. Therefore, iontophoresis of nanoemulsions appears to be a promising strategy for the topical treatment of tumors with lipophilic drugs.

Resveratrol-loaded nanocapsules inhibit murine melanoma tumor growth.

In this study, resveratrol-loaded nanocapsules were developed and its antitumor activity tested on a melanoma mice model. These nanocapsules were spherically-shaped and presented suitable size, negative charge and high encapsulation efficiency for their use as a modified-release system of resveratrol. Nanoencapsulation leads to the drug amorphization. Resveratrol-loaded nanoparticles reduced cell viability of murine melanoma cells. There was a decrease in tumor volume, an increase in the necrotic area and inflammatory infiltrate of melanoma when resveratrol-loaded nanocapsules were compared to free resveratrol in treated mice. Nanoencapsulation of resveratrol also prevented metastasis and pulmonary hemorrhage. This modified-release technology containing resveratrol can be used as a feasible approach in order to inhibit murine melanoma tumor growth.