Alginate nanoparticles protect ferrous from oxidation: Potential iron delivery system

A novel, efficient delivery system for iron (Fe²⁺) was developed using the alginate biopolymer. Iron loaded alginate nanoparticles were synthesized by a controlled ionic gelation method and was characterized with respect to particle size, zeta potential, morphology and encapsulation efficiency. Successful loading was confirmed with Fourier Transform Infrared spectroscopy and Thermogravimetric Analysis. Electron energy loss spectroscopy study corroborated the loading of ferrous into the alginate nanoparticles. Iron encapsulation (70%) was optimized at 0.06% Fe (w/v) leading to the formation of iron loaded alginate nanoparticles with a size range of 15-30nm and with a negative zeta potential (-38mV). The in vitro release studies showed a prolonged release profile for 96h. Release of iron was around 65-70% at pH of 6 and 7.4 whereas it was less than 20% at pH 2.The initial burst release upto 8h followed zero order kinetics at all three pH values. All the release profiles beyond 8h best fitted the Korsmeyer-Peppas model of diffusion. Non Fickian diffusion was observed at pH 6 and 7.4 while at pH 2 Fickian diffusion was observed.This research was financially supported by the HETC QIG Win 3 grant, University of Peradeniya, Peradeniya, Sri Lanka

Improved delivery of caffeic acid through liposomal encapsulation

Photoageing resulting from long term exposure of the skin to UV light can be minimized by scavenging the reactive photochemical intermediates with antioxidants. For effective photoprotection, the antioxidant must overcome the barrier properties of the skin and reach the target site in significant amounts. The present study aims to improve the skin penetration of caffeic acid, a very effective free radical scavenger, by encapsulating in liposomes. Caffeic acid loaded liposomes prepared using the reverse phase evaporation technique showed 70% encapsulation efficiency and size around 100 nm with zeta potential of −55 mV.In vitrodiffusion through a dialysis membrane enabled 70% release of encapsulated caffeic acid within 7 h, whereas 95% of free caffeic acid diffused within 4 h in PBS solution (pH 7.4). Liposomal caffeic acid permeation through pig skin epidermis in a Franz cell apparatus was 45 % during 7 h. In contrast, free caffeic acid was almost nonpermeable (<5%) to pig skin during this time. The DPPH assay indicated that skin penetration did not destroy the antioxidant activity of liposomal caffeic acid or free caffeic acid. In conclusion, we confirm that liposomal caffeic acid may be successfully employed as an effective photoprotective agent against UV mediated skin damage.Peer Reviewe

Chitosan-Alginate Nanoparticle System Efficiently Delivers Doxorubicin to MCF-7 Cells

A chitosan-alginate nanoparticle system encapsulating doxorubicin (DOX) was prepared by a novel ionic gelation method using alginate as the crosslinker. These nanoparticles were around 100 nm in size and more stable with higher positive zeta potential and had higher % encapsulation efficiency (95%) than DOX loaded chitosan nanoparticles (DOX Csn NP) crosslinked with sodium tripolyphosphate (STPP). FTIR spectroscopy and thermogravimetric analysis revealed successful loading of DOX. In vitro drug release showed an initial release phase followed by slow release phase with higher cumulative release obtained with DOX loaded chitosan-alginate nanoparticles (DOX Csn-Alg NP). The in vitro cytotoxicity of DOX released from the two nanoparticle systems showed a notable difference on comparison with that of free DOX on the MCF-7 cell line. The SRB assay, AO/EB staining, and fluorescence uptake study indicated that free DOX only showed dose dependent cytotoxicity, whereas both dose and time dependency were exhibited by the two sets of NPs. While both systems show sustained release of DOX, from the cell viability plots, DOX Csn-Alg NPs showed their superiority over DOX Csn NPs. The results obtained are useful for developing DOX Csn-Alg NPs as a sustained release carrier system for DOX.This research was financially supported by the HETC QIG Window 3 Grant, University of Peradeniya, Peradeniya, Sri Lanka.Peer Reviewe

Graphene Oxide–Based Nanocomposite for Sustained Release of Cephalexin

A sustained-release carrier system for the drug cephalexin (CEF) using functionalized graphene oxide is reported. PEGylation of GO (GO-PEG) and successful loading of CEF into PEGylated graphene oxide (GO-PEG-CEF) nanoconjugate are confirmed by Fourier transform infrared spectroscopy, Raman spectroscopy, and thermogravimetric analysis. Encapsulation efficiency of 69% and a loading capacity of 19% are obtained with the optimized formulation of GO-PEG-CEF. In vitro CEF release profiles show an initial burst release followed by a more sustained release over a 96 h period with cumulative release of 80%. The half maximal inhibitory concentration (IC50) values have both dose- and time-dependent antibacterial activity for GO-PEG-CEF against both gram-positive and gram-negative bacteria while pure CEF showed only dose-dependent antibacterial activity. The minimum inhibitory concentration values of GO-PEG-CEF are 7.8 and 3.9 μg/mL against S. aureus and B. cereus, respectively, while it is 10 μg/mL with pure CEF against both gram-positive bacteria. This confirms the enhanced antibacterial activity of GO-PEG-CEF over pure CEF against gram-positive bacteria. These findings therefore show GO-PEG-CEF is promising as a sustained-release nanoantibiotic system for effective treatment against S. aureus and B. cereus infections