The use of fucosphere in the treatment of dermal burns in rabbits.

The aim of this study was to prepare a new microsphere (fucosphere) system based on polyion complexation of fucoidan with chitosan, and to evaluate its treatment efficiency on dermal burns. The physicochemical properties such as mean particle size and distribution, zeta potential and bioadhesive properties of the microspheres were investigated. The formulation which had the high surface charge, narrow size distribution and the highest bioadhesive property was selected and applied on seven male New Zealand white rabbits with dermal burns. Biopsy samples were taken on day 7, 14 and 21. Each burn site was evaluated macroscopically and histopathologically and the findings were compared with controls of fucoidan solution and chitosan microspheres. The microspheres between the size ranges of 367 and 1017 nm were obtained. The work of bioadhesion of microspheres, with the surface charges +6.1 to +26.3 mV, changed between 0.081 and 0.191 mJ cm(-2). Macroscopically and histopathological observations indicated that the fastest healing of the burns was obtained in group treated with fucosphere after 21 days of treatment (P<0.05). Rete peg formation values and nuclear organize regions (NORs) were higher with treated fucospheres than the other groups on day 14. In conclusion, in vitro and in vivo evaluation of fucospheres indicated that the new microsphere system shortened the treatment period of burns and provided fast and effective healing by improving regeneration and re-epithelization. Hence fucosphere may find application in the treatment of dermal burns.

Fucosphere--new microsphere carriers for peptide and protein delivery: preparation and in vitro characterization.

PURPOSE: Fucoidan is a complex polysaccharide containing sugars and high amounts of sulphate derived from marine brown algaes. In this study, a new microsphere-delivery system based on cross-linking of fucoidan with chitosan, named Fucosphere, was evaluated as a drug carrier. Bovine serum albumin (BSA) was used as a model protein. The effect of fucoidan (1.5, 1.75, 2.0 and 2.5%), chitosan (0.25, 0.50 and 0.75%) and protein (0.25, 0.50 and 0.75%) concentrations, the origin of chitosan and the preparation methods of the particles on the microsphere characteristics were evaluated. METHODS: The microspheres were prepared by a simple method based on the cross-linking of the opposite charged biopolymers. The shape and surface morphologies of the particles were evaluated by scanning electron microscopy (SEM) and the size, charge and encapsulation capacity of the microspheres were determined. The released amount of BSA from the microspheres into phosphate buffered saline (PBS pH 7.4) was determined spectrophotometrically by the Bradford method. SDS-PAGE was performed to check the structural integrity of BSA after the preparation. RESULTS: Smooth and spherical microspheres between the size ranges of 0.61-1.28 microm were obtained. BSA was efficiently encapsulated into the microspheres (51.8-89.5%). All formulation parameters affected the encapsulation capacity of Fucosphere (p < 0.05). The highest encapsulation was obtained with microspheres containing 2.5% of fucoidan (89.5%). CONCLUSIONS: The extent of drug release from the microspheres was dependent on the concentrations of polymers and BSA, chitosan origin and type of preparation method. When the addition methods of protein compared, BSA encapsulated into Fucosphere released slower than the adsorbed protein (E) (p < 0.05). The electrophoretic mobility values of Fucospheres changed between +6.9 and +32.3 mV. In general, BSA release from Fucosphere showed a three-phasic release curve. In conclusion, this new fucoidan microsphere system may be a potential delivery of macromolecular drug such as peptide and protein.

Release characteristics of chitosan treated alginate beads: II. Sustained release of a low molecular drug from chitosan treated alginate beads.

The aim of this paper was to investigate the possible applicability of chitosan treated alginate beads as a controlled release system of small molecular drugs with high solubility. Timolol maleate (mw 432.49) was used as a model drug. The beads were prepared by the ionotropic gelation method and the effect of various factors (alginate, chitosan, drug and calcium chloride concentrations, the volume of external and internal phases and drying methods) on bead properties were also investigated. Spherical beads with 0.78-1.16 mm diameter range and 10.8-66.5% encapsulation efficiencies were produced. Higher encapsulation efficiencies and retarded drug release were obtained with chitosan treated alginate beads. Among the different factors investigated such as alginate, drug, chitosan and CaCl2 concentrations, the volumes of the external and internal phases affected bead properties. The drying technique has an importance on the bead properties also. The release data was kinetically evaluated. It appeared that chitosan treated alginate beads may be used for a potential controlled release system of small molecular drugs with high solubility, instead of alginate beads.

Release characteristics of chitosan treated alginate beads: I. Sustained release of a macromolecular drug from chitosan treated alginate beads.

Alginate and chitosan treated alginate beads were prepared and compared as an oral controlled release system for macromolecular drugs. Dextran (M.W. 70,000) was used as a model substance. The beads were prepared by the ionotropic gelation method and the effect of various factors (alginate, chitosan, drug and calcium chloride concentrations, the volume of external and internal phases and drying methods) on bead properties were investigated. The addition of chitosan increased the drug loading capacity of the beads, and larger beads were obtained in the presence of chitosan. On the other hand, addition of chitosan in the gel structure reduced the drug release from beads. The erosion of the beads was suppressed by chitosan treatment. The drying method was important to the properties of the chitosan-alginate beads. It is proposed that chitosan treated alginate beads may be used as a potential controlled release system of such macromolecules.