Therapeutic effects of curcumin nanoemulsions on prostate cancer.

The therapeutic potential of curcumin (Cur) is hampered by its poor aqueous solubility and low bioavailability. The aim of this study was to determine whether Cur nanoemulsions enhance the efficacy of Cur against prostate cancer cells and increase the oral absorption of Cur. Cur nanoemulsions were developed using the self-microemulsifying method and characterized by their morphology, droplet size and zeta potential. The results showed that the cytotoxicity and cell uptake were considerably increased with Cur nanoemulsions compared to free Cur. Cur nanoemulsions exhibited a significantly prolonged biological activity and demonstrated better therapeutic efficacy than free Cur, as assessed by apoptosis and cell cycle studies. In situ single-pass perfusion studies demonstrated higher effective permeability coefficient and absorption rate constant for Cur nanoemulsions than for free Cur. Our study suggested that Cur nanoemulsions can be used as an effective drug delivery system to enhance the anticancer effect and oral bioavailability of Cur.

Therapeutic Effects of Curcumin Nanoemulsions on Prostate Cancer / 华中科技大学学报（医学）（英德文版）

The therapeutic potential of curcumin (Cur) is hampered by its poor aqueous solubility and low bioavailability.The aim of this study was to determine whether Cur nanoemulsions enhance the efficacy of Cur against prostate cancer cells and increase the oral absorption of Cur.Cur nanoemulsions were developed using the self-microemulsifying method and characterized by their morphology,droplet size and zeta potential.The results showed that the cytotoxicity and cell uptake were considerably increased with Cur nanoemulsions compared to free Cur.Cur nanoemulsions exhibited a significantly prolonged biological activity and demonstrated better therapeutic efficacy than free Cur,as assessed by apoptosis and cell cycle studies.In siru single-pass perfusion studies demonstrated higher effective permeability coefficient and absorption rate constant for Cur nanoemulsions than for free Cur.Our study suggested that Cur nanoemulsions can be used as an effective drug delivery system to enhance the anticancer effect and oral bioavailability of Cur.

[Study on preparation and optimization of saikoside liposomes].

OBJECTIVE: To optimize the prescription and technique for preparing saikoside (SS) liposomes and evaluate its quality. METHODS: The preparation methods of liposomes included film dispersion, ether injection, reverse phase evaporation and pH gradients were explored. The encapsulation ratio was determined by macroreticular resin method. The main factors affecting encapsulation ratio were studied by single factor analysis and central composite design. RESULTS: The appearance of SS liposomes prepared by optimized method was satisfactory. The encapsulation ratio was more than 60% and the verage particle size of SS liposomes was 110 nm. CONCLUSION: The formulation and preparation process is practical and simple for the preparation of SS liposomes. It is valuable to be further studied.

Bis{1-[(1H-benzimidazol-1-yl)meth-yl]-1H-imidazole-κN (3)}bis-(3,5-dicarb-oxy-benzoato-κ(2) O (1),O (1'))nickel(II) octa-hydrate.

In the title complex, [Ni(C9H5O6)2(C11H10N4)2]·8H2O, the Ni(II) ion exhibits site symmetry 2. It has a distorted octa-hedral coordination defined by two N atoms from two symmetry-related 1-[(1H-benzimidazol-1-yl)meth-yl]-1H-imidazole ligands and four O atoms from two symmetry-related 3,5-dicarb-oxy-benzoate anions. In the crystal, the complex mol-ecules and solvent water mol-ecules are linked via O-H⋯O, O-H⋯N and N-H⋯O hydrogen bonds, forming a three-dimensional structure. There are also a number of C-H⋯O inter-actions present.

Poly[[diaqua-(µ(8)-benzene-1,2,4,5-tetra-carboxyl-ato)calciumzinc] monohydrate].

In the title complex, {[CaZn(C(10)H(2)O(8))(H(2)O)(2)]·H(2)O}(n), the Zn(II) ion is coordinated by four O atoms from four benzene-1,2,4,5-tetra-carboxyl-ate anions in a distorted tetra-hedral geometry. The Ca(II) ion is eight-coordinated by six O atoms from four benzene-1,2,4,5-tetra-carboxyl-ate anions and by two water mol-ecules in a distorted square-anti-prismatic geometry. The Ca(II) and Zn(II) ions and the lattice water mol-ecule are located on twofold rotation axes; the centroid of the benzene-1,2,4,5-tetra-carboxyl-ate anion is located on a centre of inversion. The µ(8)-bridging mode of the anion results in the formation of a three-dimensional structure with channels extending along [100] in which lattice water mol-ecules are situated. Inter-molecular O-H⋯O hydrogen bonds involving the coordinating and lattice water mol-ecules as donors and the carboxyl-ate O atoms and lattice water mol-ecules as acceptors are present in the structure.

Poly[[tetra-aqua-bis-(µ(3)-5-carboxybenzene-1,2,4-tri-carboxyl-ato)tricadmium] tetra-hydrate].

There are three independent Cd(II) ions in the title complex, {[Cd(3)(C(10)H(3)O(8))(2)(H(2)O)(4)]·4H(2)O}(n), one of which is coordinated by four O atoms from three 5-carboxybenzene-1,2,4-tri-carboxyl-ate ligands and by two water mol-ecules in a distorted octa-hedral geometry. The second Cd(II) ion is coordinated by five O atoms from four 5-carboxybenzene-1,2,4-tri-carboxyl-ate ligands and by one water mol-ecule also in a distorted octa-hedral geometry while the third Cd(II) ion is coordinated by five O atoms from three 5-carboxybenzene-1,2,4-tri-carboxyl-ate ligands and by one water mol-ecule in a highly distorted octa-hedral geometry. The 5-carboxybenzene-1,2,4-tri-carboxyl-ate ligands bridge the Cd(II) ions, resulting in the formation of a three-dimensional structure. Intra- and inter-molecular O-H⋯O hydrogen bonds are present throughout the three-dimensional structure.