The present study was designed to prepare and compare bio-adhesive pellets of panax notoginseng saponins (PNS) with hydroxy propyl methyl cellulose (HPMC), chitosan, and chitosan : carbomer, explore the influence of different bio-adhesive materials on pharmacokinetics behaviors of PNSbio-adhesive pellets, and evaluate the correlation between in vivo absorption and in vitro release (IVIVC). In order to predict the in vivo concentration-time profile by the in vitro release data of bio-adhesive pellets, the release experiment was performed using the rotating basket method in pH 6.8 phosphate buffer. The PNS concentrations in rat plasma were analyzed by HPLC-MS-MS method and the relative bioavailability and other pharmacokinetic parameters were estimated using Kinetica4.4 pharmacokinetic software. Numerical deconvolution method was used to evaluate IVIVC. Our results indicated that, compared with ordinary pellets, PNS bio-adhesive pellets showed increased oral bioavailability by 1.45 to 3.20 times, increased C, and extended MRT. What's more, the release behavior of drug in HPMC pellets was shown to follow a Fickian diffusion mechanism, a synergetic function of diffusion and skeleton corrosion. The in vitro release and the in vivo biological activity had a good correlation, demonstrating that the PNS bio-adhesive pellets had a better sustained release. Numerical deconvolution technique showed the advantage in evaluation of IVIVC for self-designed bio-adhesive pellets with HPMC. In conclusion, the in vitro release data of bio-adhesive pellets with HPMC can predict its concentration-time profile in vivo.
Acrylic Resins ; Adhesives ; Animals ; Chitosan ; Drug Carriers ; Drug Liberation ; In Vitro Techniques ; Intestinal Absorption ; Male ; Methylcellulose ; Panax notoginseng ; chemistry ; Plant Extracts ; administration & dosage ; metabolism ; pharmacokinetics ; Rats, Sprague-Dawley ; Saponins ; administration & dosage ; metabolism ; pharmacokinetics

Acrylic Resins ; chemistry ; Composite Resins ; chemistry ; Dental Research ; Dental Stress Analysis ; Polymerization ; Polyurethanes ; chemistry

OBJECTIVETo prepare the cross-linked chitosan/poly(acrylic acid)/poly (ethylene oxide) nanofibrous membrance loaded with pseudo-ginseng and to determine its characteristics.

METHODSPseudo-ginseng entrapped in chitosan, poly (acrylic acid), poly (ethylene oxide) nanofibrous membrane loaded with pseudo-ginseng was prepared by electrospinning and thermal treatment method. The surface morphology of fiber membrane was observed by scanning electron microscopy and the chemical structures were characterized by infrared spectroscopy; the thermal decomposition temperature was analyzed by the thermogravimetric analysis. UV-Vis spectra were used to evaluate the in vitro release properties.

RESULTSThe average diameter of the prepared nanofibrous particles was (181 ± 71) nm. The tensile strength of fiber membrane increased by 35.3% and the decomposition temperature increased from 197℃ to 208℃ after crosslinking. Compared with casting film, the structure of fiber membrane increased the release rate and the overall amount of active components from pseudo-ginseng.

CONCLUSIONThe preparation of chitosan fiber loaded with pseudo-ginseng is simple and the dispersion of pseudo-ginseng is homogeneous. This fibrous pseudo-ginseng exhibited good release performance, providing a new Chinese medicine formulation.

Acrylic Resins ; chemistry ; Chitosan ; chemistry ; Drugs, Chinese Herbal ; chemistry ; Microscopy, Electron, Scanning ; Panax ; chemistry ; Polyethylene Glycols ; chemistry ; Temperature

The aimed of this study was to prepare stabilized thiomers to overcome the poor stability character of traditional thiomers. Poly(acrylic acid)-cysteine (PAA-Cys) was synthesized by conjugating cysteine with poly(acrylic acid) and poly(acrylic acid)-cysteine-6-mercaptonicotinic acid (PAA-Cys-6MNA, stabilized thiomers) was synthesized by grafting a protecting group 6-mercaptonicotinic acid (6MNA) with PAA-Cys. The free thiol of PAA-Cys was determined by Ellmann's reagent method and the ratio of 6MNA coupled was determined by glutathione reduction method. The study of permeation enhancement and stabilized function was conducted by using Franz diffusion cell method, with fluorescein isothiocyanate dextran (FD4) used as model drug. The influence of polymers on tight junctions of Caco-2 cell monolayer was detected with laser scanning confocal fluorescence microscope. The results indicated that both PAA-Cys and PAA-Cys-6MNA could promote the permeation of FD4 across excised rat intestine, and the permeation function of PAA-Cys-6MNA was not influence by the pH of the storage environment and the oxidation of air after the protecting group 6MNA was grafted. The distribution of tight junction protein of Caco-2 cell monolayer F-actin was influenced after incubation with PAA-Cys and PAA-Cys-6MNA. In conclusion, stabilized thiomers (PAA-Cys-6MNA) maintained the permeation function compared with the traditional thiomers (PAA-Cys) and its stability was improved. The mechanism of the permeation enhancement function of the polymers might be related to their influence on tight junction relating proteins of cells.
Acrylic Resins ; chemistry ; Actins ; metabolism ; Animals ; Caco-2 Cells ; Cysteine ; chemistry ; Dextrans ; Fluorescein-5-isothiocyanate ; analogs & derivatives ; Glutathione ; Humans ; Intestinal Absorption ; Intestinal Mucosa ; drug effects ; Nicotinic Acids ; chemistry ; Rats ; Sulfhydryl Compounds ; chemistry

OBJECTIVETo prepare matrine double-sensitive colon-specific pellets and study the factors affecting its quality and evaluateing the colon-specific effects of preparation.

METHODMatrine enzyme-sensitive pellets core were prepared by carboxymethyl konjac glucomannan as the main carrier material, and coated the core by acrylic resin II and III to prepare matrine double-sensitive colon-specific pellets. The prescription and technology of the matrine colon-specific pellets were studied by the single factor investigation, through the in vitro release test and coating rate determination.

RESULTThe optimized process conditions: FeCl3 concentration is 4.0 g x L(-1), chitosan concentration is 3.0 g x L(-1), carboxymethyl konjac glucomannan concentration is 20 g x L(-1), mixed gel solution pH value is 3. The release of matrine is less than 30% in the simulation of the upper gastrointestinal medium. The release of matrine is close to 100% in simulated full gastrointestinal medium, the coating weight is 7%.

CONCLUSIONThe prepared pellets have good colon positioning effect in vitro.

Acrylic Resins ; chemistry ; Administration, Oral ; Alkaloids ; administration & dosage ; chemistry ; pharmacokinetics ; Chitosan ; chemistry ; Chlorides ; chemistry ; Colon ; metabolism ; Delayed-Action Preparations ; administration & dosage ; chemistry ; pharmacokinetics ; Drug Compounding ; methods ; Drug Delivery Systems ; methods ; Ferric Compounds ; chemistry ; Humans ; Hydrogen-Ion Concentration ; Mannans ; chemistry ; Quinolizines ; administration & dosage ; chemistry ; pharmacokinetics ; Reproducibility of Results ; Tablets, Enteric-Coated ; Time Factors

Novel uniform-sized magnetic molecularly imprinted polymers (MMIPs) were synthesized for selective recognition of active antitumor ingredients of kaempferol (KMF) and protoapigenone (PA) in Macrothelypteris torresiana (M. torresiana) by surface molecular imprinting technique in this study. Super paramagnetic core-shell nanoparticles (γ-MPS-SiO2@Fe3O4) were used as seeds, KMF as template molecule, acrylamide (AM) as functional monomer, and N, N'-methylene bisacrylamide (BisAM) as cross-linker. The prepared MMIPs were characterized by X-ray diffraction (XRD), Fourier transform infrared spectrum (FTIR), transmission electron microscopy (TEM) and thermo-gravimetric analysis (TGA), respectively. The recognition capacity of MMIPs was 2.436 times of non-imprinted polymers. The adsorption results based on kinetics and isotherm analysis were in accordance with the pseudo-second-order model (R (2)=0.9980) and the Langmuir adsorption model (R (2)=0.9944). The value of E (6.742 kJ/mol) calculated from the Dubinin-Radushkevich isotherm model suggested that the physical adsorption via hydrogen-bonding might be predominant. The Scatchard plot showed a single line (R (2)=0.9172) and demonstrated the homogeneous recognition sites on MMIPs for KMF. The magnetic solid phase extraction (MSPE) based on MMIPs as sorbent was established for fast and selective enrichment of KMF and its structural analogue PA from the crude extract of M. torresiana and then KMF and PA were detected by HPLC-UV. The established method showed good performance and satisfactory results for real sample analysis. It also showed the feasibility of MMIPs for selective recognition of active structural analogues from complex herbal extracts.
Acrylic Resins ; chemical synthesis ; chemistry ; Antineoplastic Agents, Phytogenic ; chemistry ; isolation & purification ; Cyclohexanones ; chemistry ; isolation & purification ; Ferns ; chemistry ; Flavones ; chemistry ; isolation & purification ; Kaempferols ; chemistry ; isolation & purification ; Nanoparticles ; chemistry

The objective of this research is to evaluate the effects of different silane coupling agents on the bond strength between Ceramco3 opaque porcelain and indirect composite resin. Five groups of Co-Cr metal alloy substrates were fabricated according to manufacturer's instruction. The surface of metal alloy with a layer of dental opaque porcelain was heated by fire. After the surface of opaque porcelain was etched, five different surface treatments, i.e. RelyX Ceramic Primer (RCP), Porcelain Bond Activator and SE Bond Primer (mixed with a proportion of 1:1) (PBA), Shofu Porcelain Primer (SPP), SE bond primer (SEP), and no primer treatment (as a control group), were used to combine P60 and opaque porcelain along with resin cement. Shear bond strength of specimens was tested in a universal testing machine. The failure modes of specimens in all groups were observed and classified into four types. Selected specimens were subjected to scanning electron microscope and energy disperse spectroscopy to reveal the relief of the fracture surface and to confirm the failure mode of different types. The experimental results showed that the values of the tested items in all the tested groups were higher than that in the control group. Group PBA exhibited the highest value [(37.52 +/- 2.14) MPa] and this suggested a fact that all of the specimens in group PBA revealed combined failures (failure occurred in metal-porcelain combined surface and within opaque porcelain). Group SPP and RCP showed higher values than SEP (P < 0.05) and most specimens of SPP and RCP performed combined failures (failure occurred in bond surface and within opaque porcelain or composite resin) while all the specimens in group SEP and control group revealed adhesive failures. Conclusions could be drawn that silane coupling agents could reinforce the bond strength of dental composite resin to metal-opaque porcelain substrate. The bond strength between dental composite resin and dental opaque porcelain could meet the clinical requirements.
Acrylic Resins ; chemistry ; Ceramics ; chemistry ; Composite Resins ; chemistry ; Dental Bonding ; Dental Porcelain ; chemistry ; Humans ; Polyurethanes ; chemistry ; Resin Cements ; chemistry ; Silanes ; chemistry

We studied the interaction between proteins and polystyrene-polyacrylic acid (PS-PAA) spherical polyelectrolyte brushes with different polyacrylic acid (PAA) chain lengths, including the physical adsorption and chemical adsorption in PBS buffer. Results showed that the amount of bovine serum albumin (BSA) physically adsorbed on PS-PAA spherical polyelectrolyte brushes decreased to a minimum of 33 microg/mg whereas the amount of streptavidin (SA) chemically adsorbed increased with the increase of chain length and carboxyl quantity. The biotin binding capacity of streptavidin chemically adsorbed on PS-PAA spherical polyelectrolyte brushes was roughly evaluated via enzyme competitive inhibition.
Acrylic Resins ; chemistry ; Adsorption ; Biosensing Techniques ; Electrochemical Techniques ; methods ; Electrolytes ; chemistry ; Polyamines ; Polymers ; chemistry ; Polystyrenes ; chemistry ; Proteins ; chemistry ; Serum Albumin, Bovine ; chemistry ; Surface Properties

The aim of the study was to evaluate the effect of adding acrylamide monomer (AAm) on the characterization, flexural strength, flexural modulus and thermal degradation temperature of poly(methyl methacrylate) (PMMA) denture-base resins. Specimens (n=10) were fabricated from a conventional heat-activated QC-20 (Qc-) and a microwave heat-activated Acron MC (Ac-) PMMA resins. Powder/liquid ratio followed the manufacturer's instructions for the control groups (Qc-c and Ac-c) and for the copolymer groups, the resins were prepared with 5% (-5), 10% (-10), 15% (-15) and 20% (-20) acrylamide contents, according to the molecular weight ratio, respectively. The flexural strength and flexural modulus were measured by a three-point bending test. The data obtained were statistically analyzed by Kruskal-Wallis test (α=0.05) to determine significant differences between the groups. The chemical structures of the resins were characterized by the nuclear magnetic resonance spectroscopy. Thermal stabilities were determined by thermogravimetric analysis (TGA) with a heating rate of 10 °C⋅min(-1) from 35 °C to 600 °C. Control groups from both acrylic resins showed the lowest flexural strength values. Qc-15 showed significant increase in the flexural strength when compared to Qc-c (P<0.01). Ac-10 and Ac-15 showed significance when compared to Ac-c (P<0.01). Acrylamide incorporation increased the elastic modulus in Qc-10, Qc-15 and Qc-20 when compared to Qc-c (P<0.01). Also significant increase was observed in Ac-10, Ac-15 and Ac-20 copolymer groups when compared to Ac-c (P<0.01). According to the (1)H-nuclear magnetic resonance (NMR) results, acrylamide copolymerization was confirmed in the experimental groups. TGA results showed that the thermal stability of PMMA is increased by the insertion of AAm.
Acrylamide ; chemistry ; Acrylic Resins ; chemistry ; Dental Materials ; chemistry ; Denture Bases ; Elastic Modulus ; Hot Temperature ; Humans ; Magnetic Resonance Spectroscopy ; Materials Testing ; Microwaves ; Pliability ; Polymerization ; Polymethyl Methacrylate ; chemistry ; Powders ; Solutions ; Stress, Mechanical ; Thermodynamics ; Thermogravimetry ; Time Factors

In this paper, chloramphenicol was selected as a model drug to prepare in situ gels. The intrinsic dissolution rate of chloramphenicol from in situ gel was evaluated using the surface dissolution imaging system. The results indicated that intrinsic dissolution rate of chloramphenicol thermosensitive in situ gel decreased significantly when the poloxamer concentration increased. The addition of the thickener reduced the intrinsic dissolution rate of chloramphenicol thermosensitive gel, wherein carbomer had the most impact. Different dilution ratios of simulated tear fluid greatly affected gel temperature, and had little influence on the intrinsic dissolution rate of chloramphenicol from the thermosensitive in situ gel. The pH of simulated tear fluid had little influence on the intrinsic dissolution rate of chloramphenicol thermosensitive in situ gel. For the pH sensitive in situ gel, the dissolution rates of chloramphenicol in weak acidic and neutral simulated tear fluids were slower than that in weak alkaline simulated tear fluid. In conclusion, the intrinsic dissolution of chloramphenicol from in situ gel was dependent on formulation and physiological factors. With advantages of small volume sample required and rapid detection, the UV imaging method can be an efficient tool for the evaluation of drug release characteristics of ophthalmic in situ gel.
Acrylic Resins ; chemistry ; Anti-Bacterial Agents ; administration & dosage ; chemistry ; Chloramphenicol ; administration & dosage ; chemistry ; Drug Delivery Systems ; Gels ; chemistry ; Hydrogen-Ion Concentration ; Ophthalmic Solutions ; chemistry ; Poloxamer ; chemistry ; Solubility ; Spectrophotometry, Ultraviolet ; Temperature ; Viscosity