Dendritic polymer polyamide - the amine - puerarin Composites and its impact on the cornea
|Keywords||Tree polymer Puerarin Composite Characterization In vitro release In vitro corneal penetration Eye retention time|
Dendritic polymers polyamidoamine (Polyamidoamine PAMAM) is developed in recent years a class of three-dimensional highly branched dendrimers, having a monodispersed, non-immunogenic, low cell toxicity, biodegradability, etc. characteristic, to increase the solubility of the drug as a pharmaceutical carrier, can delay the release of the drug after administration of the different ways to increase drug skin permeation coefficient, to extend the residence time of the cornea, thereby increasing the bioavailability of the drug, is a considerable potential for development of novel drugs carrier. This thesis puerarin (Puerarin PUE) as a model drug were prepared the different algebraic PAMAM PUE complex, determine both maximum binding molar ratio and drug mechanisms, release behavior of composite objects at the same time to inspect and study algebra PAMAM on PUE in vitro corneal permeability and the residence time in the anterior corneal PAMAM provide the basis for ocular drug delivery carrier. Prepare different algebraic the PAMAM PUE composite material, per molecule G3.5, G4, G4.5, G5 PAMAM up composite 36,56,125,170 PUE molecules, with the increase of the pH of the solution, the half-generation PAMAM PUE amount of complex no significant increase in generation PAMAM PUE complex increased with the increase of pH. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry spectrometry analysis (DSC) characterization of complex PAMAM PUE mainly through hydrogen bonding interactions to form complexes. PAMAM PUE complex release media exhibit different release characteristics with PAMAM increased Algebra, sustained-release effect is more obvious. Whole generation of over half PAMAM PUE complex sustained-release effect. Water media PUE slowest released from the complex, with increasing solution pH, ion concentration decreases, PUE is released from the complex slows down. Second, using a the Valia Chien diffusion cell apparatus, PAMAM pretreatment drugs (physical mixtures and composites) and corneal after in vitro permeation experiments, G3, G4, G5 PAMAM PUE physical mixture of PUE corneal permeability coefficient 2.48,1.99,1.36 times. With G3 PAMAM the PUE mixed weight ratio increased, PUE corneal permeability coefficient gradually increased to a maximum value remained stable or declined slightly. PAMAM pretreatment of the cornea, the increase in PUE vitro cornea through amount and corneal permeability coefficient, enhanced permeability ratio increased with the increase of PAMAM Generation. PAMAM form complexes with PUE PUE from the body through the amount of corneal and corneal permeability coefficient is not significantly increased. Free drug in the corneal penetration process dominates. The corneal hydration value measurement is less than 79% PAMAM without damage to corneal epithelial cells or endothelial cells. G3.5, G4 PAMAM PUE complex, for example, G3.5, the residence time before the the G4 PAMAM PUE composite corneal than PUE aqueous solution have been prolonged and G4 the PAMAM PUE composite material a longer residence time. Instructions under physiological conditions, the PAMAM can interact with the cornea, and open the cornea between \PAMAM is PUE ocular pharmaceutical carrier as an ideal for increasing the bioavailability of the drug.