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Biomedical subjects

Kinam Park

Publications and source records attributed to Kinam Park.

At least 19 recordsLinked to original sources

Preparation and swelling behavior of chitosan-based superporous hydrogels for gastric retention application.

Chitosan and glycol chitosan hydrogels were prepared, and their swelling behaviors in acidic solution were studied to investigate their application for gastric retention device. The optimum preparation condition of superporous hydrogels was obtained from the gelation and blowing kinetics measured at varying acidic conditions. Both the swelling rate and swelling ratio of glycol chitosan hydrogels were higher than those of chitosan hydrogels. Swelling behaviors were significantly affected by not only foaming/drying methods but also crosslinking density, as the sizes and structures of pores generated were highly dependent on those preparation conditions. The prepared superporous hydrogels were highly sensitive to pH of swelling media, and showed reversible swelling and de-swelling behaviors maintaining their mechanical stability. The degradation kinetics in simulated gastric fluid was also studied.

Biocompatible Materials↗

Fast-melting tablets based on highly plastic granules.

Highly plastic granules that can be compressed into tablets at low pressure were developed to make fast-melting tablets (FMTs) by compression method. The highly plastic granules are composed of three components: a plastic material, a material enhancing water penetration, and a wet binder. One of the unique properties of the highly plastic granules is that they maintain a porous structure even after compression into tablets. The porous and plastic nature of the granules allows fast absorption of water into the compressed tablet for fast melting/dissolution of the tablet. The prepared tablets possess tablet strength and friability that are suitable for multi-tablet packages. The three-component highly plastic granules provide an effective way of making FMTs by compression.

Chemistry, Pharmaceutical↗

Hydrogen bonding interactions between adsorbed polymer molecules and crystal surface of acetaminophen.

The objective of this work was to investigate whether or not the hydrogen bonding interaction between polymer and crystal surface can be detected by the etching pattern changes in the presence of polymers. The (010) face of acetaminophen single crystal was used as a model solid surface. The etching patterns on the (010) face of acetaminophen crystal by water are in the directions of a- and c-axes, which are the same as the directions of the dominant attachment energies on the (010) face. In the presence of polymer, the hydrogen bonding interactions between adsorbed polymer and crystal surface can affect surface diffusion of acetaminophen molecules and change the etching patterns in the direction of a-axis, i.e., the direction of one hydrogen bond chain. Studies with 2-hydroxyethyl cellulose (HEC), hydroxypropyl cellulose (HPC), hydroxypropyl methylcellulose (HPMC) and poly(vinyl alcohol) (PVA) showed that polymers, which can form hydrogen bonds with acetaminophen crystal surface, can change etching patterns in the direction of a-axis. Study with Dextran suggested that if a polymer cannot form hydrogen bonds with crystal surface due to steric repulsion, it will not change the etching pattern in the direction of a-axis. Studies with poly(ethylene glycol) (PEG) and poly(propylene glycol) (PPG) further confirmed that only if a polymer can form hydrogen bonds with acetaminophen on crystal surface, the etching patterns in the direction of a-axis will be affected. The study results suggest that in the presence of polymers, the etching pattern change in the direction of hydrogen bond chain, the a-axis of acetaminophen crystals, can be used to indicate the existence of the hydrogen bonding interactions between adsorbed polymers and acetaminophen crystal surface.

Acetaminophen↗

Bioadhesive interaction and hypoglycemic effect of insulin-loaded lectin-microparticle conjugates in oral insulin delivery system.

Biodegradable microparticles were prepared with alginate by the piezoelectric ejection process, and lectin (wheat germ agglutinin, WGA) was conjugated to alginate microparticles to take advantage of the protective effects of alginate microparticles and the mucoadhesive properties of WGA for improved oral delivery of insulin. Their specific interaction with model mucin was determined by pig mucin (PM) immobilized surface plasmon resonance (SPR) biosensor and in vitro adsorption studies. The hypoglycemic effects of alginate and WGA-conjugated alginate microparticles were examined after oral administration in streptozotocin-induced diabetic rats. The alginate microparticles were fabricated by ejecting alginate/insulin solution into 0.1 M CaCl2 solution through a nozzle actuated by the piezoelectric transducer. The WGA was conjugated to alginate microparticles by activating hydroxyl groups with carbonyldiimidazole (CDI). The affinity constant (K(A)) of alginate-WGA microparticles from the SPR data (K(A)=5.455 g(-1) L) was about nine times greater than alginate microparticles (K(A)=0.628 g(-1) L). In vitro experiments in the mucin solution showed that the conjugated WGA enhanced the interaction about three times. In vivo studies with diabetic rats showed that the blood glucose level of SPF rats was lowest when alginate-WGA microparticles were orally administered. Larger K(A) of alginate-WGA microparticles resulted in larger glucose change (%) from base level. Still, it is not clear whether the transport of insulin through the intestinal mucous membrane was influenced by the increase of residence time at intestinal membrane through the specific adsorption of WGA-conjugated microparticles. However, it is concluded that alginate-WGA microparticles enhance the intestinal absorption of insulin sufficient to drop the glucose level of blood.

Adhesives↗

Advances in superporous hydrogels.

Superporous hydrogels (SPHs) are different from superabsorbent polymers (SAPs) in that SPHs swell fast, within minutes, to the equilibrium swollen state regardless of their size. The fast swelling property is based on water absorption through open porous structure by capillary force. The poor mechanical strength of SPHs was overcome by developing the second-generation SPH composites (SPHCs) and the third-generation SPH hybrids (SPHHs). This review examines the differences between SAPs and SPHs and describes three different generations of SPHs.

Chemistry, Pharmaceutical↗

Hydrotropic polymer micelle system for delivery of paclitaxel.

Hydrotropic polymer micelle system has been developed for delivery of poorly water-soluble drugs such as paclitaxel. Hydrotropic polymers based on N,N-diethylnicotinamide were synthesized and used as a hydrophobic block for constructing amphiphilic block copolymers. The hydrotropic block copolymers self-assembled to form micelles in aqueous media. The size of the prepared polymer micelles was in the range of 30-50 nm, and increased to 100-120 nm after paclitaxel loading. The critical micelle concentrations (CMCs) of the block copolymers were higher by an order of magnitude than those of other typical polymer micelles, due to less hydrophobicity of the hydrotropic blocks. The drug loading capacity and physical stability of the polymer micelles were characterized and compared with those of other polymer micelles. The hydrotropic polymer micelles containing hydrotrope-rich cores showed not only higher loading capacity but also enhanced physical stability in aqueous media. They could be redissolved in aqueous media by simple vortexing and/or a mild heating. The hydrotropic polymer micelles provide an alternative approach for formulation of poorly soluble drugs.

Drug Delivery Systems↗

Study on the interactions between polyvinylpyrrolidone (PVP) and acetaminophen crystals: partial dissolution pattern change.

The objective of the study was to investigate the interactions between polyvinylpyrrolidone (PVP) and acetaminophen crystal especially on crystal surface. The effects of PVP on the etching pattern change of the acetaminophen (010) face, solubility enhancement as well as the intrinsic dissolution rate (IDR) of acetaminophen crystals have been studied. The etching patterns of the acetaminophen (010) face in the presence of PVP have stable ledges in the direction of a-axis, but deviate from c-axis, which shows that the dissolution on the (010) face has been affected by the adsorbed PVP especially in the direction of c-axis through van der Waals interactions rather than hydrogen bonding interactions. Even though PVP(K30) can enhance the solubility of acetaminophen in concentration higher than 1 mg/mL, the IDR of acetaminophen in diluted PVP solutions was lower than in water. Because the viscosity of those diluted PVP(K30) solutions were the same as water viscosity, the lowered IDR of acetaminophen cannot be explained simply by the viscosity effects of PVP solutions. Overall, the study suggests that the PVP molecules adsorbed on the surface of acetaminophen crystals play an important role in etching pattern change as well as the intrinsic dissolution rate change.

Acetaminophen↗

Accelerated chondrocyte functions on NaOH-treated PLGA scaffolds.

Compared to conventional poly(lactic-co-glycolic acid) (PLGA), previous studies have shown that NaOH-treated PLGA two-dimensional substrates enhanced functions of osteoblasts (bone-forming cells), vascular and bladder smooth muscle cells, and chondrocytes (cartilage-synthesizing cells). In this same spirit, the purpose of this in vitro study was to fabricate three-dimensional NaOH-treated PLGA scaffolds and determine their efficacy toward articular cartilage applications. To improve functions of chondrocytes including their adhesion, growth, differentiation, and extracellular matrix synthesis, PLGA scaffolds were modified via chemical etching techniques using 1N NaOH for 10 min. Results demonstrated that NaOH-treated PLGA three-dimensional scaffolds enhanced chondrocyte functions compared to non-treated scaffolds. Specifically, chondrocyte numbers, total intracellular protein content, and the amount of extracellular matrix components (such as glycosaminoglycans and collagens) were significantly greater on NaOH-treated than on non-treated PLGA scaffolds. Underlying material properties that may have enhanced chondrocyte functions include a more hydrophilic surface (due to hydrolytic degradation of PLGA by NaOH), increased surface area, altered porosity (both percent and diameter of individual pores), and a greater degree of nanometer roughness. For these reasons, this study adds a novel tissue-engineering scaffold to the cartilage biomaterial community: NaOH-treated PLGA. Clearly, such modifications to PLGA may ultimately enhance the efficacy of tissue-engineering scaffolds for articular cartilage repair.

Biocompatible Materials↗

Frosta: a new technology for making fast-melting tablets.

The fast-melting tablet (FMT) technology, which is known to be one of the most innovated methods in oral drug delivery systems, is a rapidly growing area of drug delivery. The initial success of the FMT formulation led to the development of various technologies. These technologies, however, still have some limitations. Recently, a new technology called Frosta (Akina) was developed for making FMTs. The Frosta technology utilises the conventional wet granulation process and tablet press for cost-effective production of tablets. The Frosta tablets are mechanically strong with friability of < 1% and are stable in accelerated stability conditions when packaged into a bottle container. They are robust enough to be packaged in multi-tablet vials. Conventional rotary tablet presses can be used for the production of the tablets and no other special instruments are required. Thus, the cost of making FMTs is lower than that of other existing technologies. Depending on the size, Frosta tablets can melt in < 10 s after placing them in the oral cavity for easy swallowing. The Frosta technology is ideal for wide application of FMTs technology to various drug and nutritional formulations.

Administration, Oral↗

A new microencapsulation method using an ultrasonic atomizer based on interfacial solvent exchange.

Reservoir-type microcapsules were produced in a mild and highly efficient manner using a coaxial ultrasonic atomizer. To understand the microencapsulation mechanism, the atomizer was operated in different modes. The results suggested the reservoir-type microcapsules were formed by midair collision of the microdrops of the two component liquids consisting of a polymer solution and an aqueous solution. The encapsulation efficiency and the distribution of the microdrops captured in midair were dependent on the ratio of the flow rates of the two liquids, which suggested that the collision involved multiple microdrops. This method allowed lysozyme to be encapsulated without loss of functional integrity and to be released with near zero-order kinetics for over 50 days. The ultrasonic atomizer provided a new method of preparing reservoir-type microcapsules.

Anti-Infective Agents↗

Characterization of reservoir-type microcapsules made by the solvent exchange method.

The purpose of this research was to characterize and optimize the properties of microcapsules produced by the solvent exchange method, a new microencapsulation technique. Reservoir-type microcapsules containing lysozyme as a model protein were produced using a coaxial ultrasonic atomizer under various formulation and instrument settings, and characterized with respect to in vitro release kinetics and stability of the encapsulated protein. The solvent exchange method could encapsulate protein drugs with high efficiency under an optimized condition and was mild enough to preserve the integrity of the encapsulated lysozyme during the process. In vitro release studies showed that the microcapsules could release proteins in a controllable manner. The solvent exchange method is a mild and simple microencapsulation method that could encapsulate lysozyme, maintaining its functional integrity.

Capsules↗

Hydrotropic agents for study of in vitro paclitaxel release from polymeric micelles.

A new experimental method for in vitro release studies of poorly soluble drugs from polymeric micelle systems was developed using a hydrotropic agent, sodium salicylate. It is difficult to maintain a good sink condition for poorly water-soluble drugs, such as paclitaxel (PTX), because of their low aqueous solubility. In this study, a good sink condition for PTX was achieved by using aqueous sodium salicylate solution which solubilized more than 10 times the total amount of PTX incorporated in polymeric micelles. Sodium salicylate at 1 M concentration increased the aqueous PTX solubility by 100 times without destroying the micellar structure of poly(ethylene glycol)-block-poly(phenylalanine) (PEG-b-PPhe) copolymer. PTX was continuously released from PEG-b-PPhe micelles in the hydrotropic release medium. The hydrotropic solution presents a simple method for studying in vitro release behavior of poorly soluble drugs from polymeric micelles in aqueous media.

Antineoplastic Agents, Phytogenic↗

Control of encapsulation efficiency and initial burst in polymeric microparticle systems.

Initial burst is one of the major challenges in protein-encapsulated microparticle systems. Since protein release during the initial stage depends mostly on the diffusional escape of the protein, major approaches to prevent the initial burst have focused on efficient encapsulation of the protein within the microparticles. For this reason, control of encapsulation efficiency and the extent of initial burst are based on common formulation parameters. The present article provides a literature review of the formulation parameters that are known to influence the two properties in the emulsion-solvent evaporation/extraction method. Physical and chemical properties of encapsulating polymers, solvent systems, polymer-drug interactions, and properties of the continuous phase are some of the influential variables. Most parameters affect encapsulation efficiency and initial burst by modifying solidification rate of the dispersed phase. In order to prevent many unfavorable events such as pore formation, drug loss, and drug migration that occur while the dispersed phase is in the semi-solid state, it is important to understand and optimize these variables.

Capsules↗

Solvent exchange method: a novel microencapsulation technique using dual microdispensers.

PURPOSE: A new microencapsulation method called the "solvent exchange method" was developed using a dual microdispenser system. The objective of this research is to demonstrate the new method and understand how the microcapsule size is controlled by different instrumental parameters. METHOD: The solvent exchange method was carried out using a dual microdispenser system consisting of two ink-jet nozzles. Reservoir-type microcapsules were generated by collision of microdrops of an aqueous and a polymer solution and subsequent formation of polymer films at the interface between the two solutions. The prepared microcapsules were characterized by microscopic methods. RESULTS: The ink-jet nozzles produced drops of different sizes with high accuracy according to orifice size of a nozzle, flow rate of the jetted solutions, and forcing frequency of the piezoelectric transducers. In an individual microcapsule, an aqueous core was surrounded by a thin polymer membrane; thus, the size of the collected microcapsules was equivalent to that of single drops. CONCLUSIONS: The solvent exchange method based on a dual microdispenser system produces reservoir-type microcapsules in a homogeneous and predictable manner. Given the unique geometry of the microcapsules and mildness of the encapsulation process, this method is expected to provide a useful alternative to existing techniques in protein microencapsulation.

Capsules↗

Polymer composition and acidification effects on the swelling and mechanical properties of poly(acrylamide-co-acrylic acid) superporous hydrogels.

Poly(acrylamide-co-acrylic acid) (poly(AM-co-AA)) superporous hydrogels (SPHs) were synthesized and the acidification effects on the swelling and mechanical properties were studied. Gelation exotherms were measured to determine the optimum introduction time for adding a blowing agent. The gelation kinetics decreased with increasing the AA concentration. The maximum equilibrium swelling was observed around an AA weight fraction of 0.4, but the compressive strength decreased monotonically with increasing the AA concentration. Poly(AM-co-AA) SPHs were much less swollen in acidic solution than in distilled water of pH 6.7. The swelling ratio decreased with increasing acidity (decreasing pH). Reduction of water absorption content by acidification led to considerable increase in the mechanical strength.

Acrylamide↗

Aqueous N,N-diethylnicotinamide (DENA) solution as a medium for accelerated release study of paclitaxel.

N,N-Diethylnicotinamide (DENA) was identified as an excellent hydrotropic agent for paclitaxel (PTX) in our previous studies. The aqueous solubility of PTX was increased by several orders of magnitude in the presence of DENA. Because of such a high hydrotropic property, DENA was used as a release medium providing a sink condition for the release of PTX from poly(lactic-co-glycolic acid) (PLGA) matrices. The release profiles of PTX from PLGA matrices into DENA, serum and phosphate-buffered saline (PBS) were compared. The stability of PTX in DENA and the degradation of PLGA molecules in DENA were examined. The degradation rate constant of PTX in 2 M DENA was similar to those in other aqueous solutions. The use of 2 M DENA as a release medium allowed differentiation of the release profiles of PTX from PLGA matrices made of different PLGA compositions. The PTX release from PLGA matrices was much faster in DENA solution than in serum or PBS, and the concentration of DENA affected the PTX release rate. The presence of DENA in the release medium increased the hydrolysis rate of PLGA polymers. The faster release of PTX from PLGA matrices in DENA solution may be due to the high PTX solubility and faster degradation of PLGA polymers in the presence of DENA. Our study suggests that the aqueous DENA solution can be used for the accelerated release study of PTX from PLGA matrices.

Animals↗

Application of poly(acrylic acid) superporous hydrogel microparticles as a super-disintegrant in fast-disintegrating tablets.

Poly(acrylic acid) superporous hydrogel (SPH) microparticles possessing a unique porous structure were used as a wicking agent to decrease disintegration time of fast-disintegrating tablets (FDTs). The compression behaviour of poly(acrylic acid) SPH microparticles was evaluated using the Kawakita equation. Effects of various SPH microparticle sizes and a 19-run fractional factorial design were evaluated. The factorial design was based on four factors consisting of ketoprofen, SPH microparticle, filler, and tableting pressure, and each factor contained three levels on the disintegration time and tensile strength of the prepared FDTs. The poly(acrylic acid) SPH microparticles existed in an amorphous state and swelled approximately 80-times in distilled water and 50-times in pH 6.8 0.2 M phosphate buffer. The compressibility of SPH microparticles increased significantly as the microparticle size increased. The FDTs made of SPH microparticles in the range of 75-106 microm showed the fastest disintegration time and higher tensile strength. SPH microparticle, tableting pressure and ketoprofen had significant effects on disintegration time and tensile strength of ketoprofen FDTs. The FDTs that were prepared with 2.5% w/w SPH microparticles of 75-106 microm at 63 MPa pressure possessed a tensile strength of 84.4 +/- 4.1 N cm(-2) and disintegrated in 15.0 +/- 2.0 s. It was concluded that the poly(acrylic acid) SPH microparticles could serve as a good super-disintegrant decreasing the disintegration time of FDTs.

Acrylic Resins↗

Orally fast disintegrating tablets: developments, technologies, taste-masking and clinical studies.

Fast disintegrating tablets (FDTs) have received ever-increasing demand during the last decade, and the field has become a rapidly growing area in the pharmaceutical industry. Upon introduction into the mouth, these tablets dissolve or disintegrate in the mouth in the absence of additional water for easy administration of active pharmaceutical ingredients. The popularity and usefulness of the formulation resulted in development of several FDT technologies. This review describes various formulations and technologies developed to achieve fast dissolution/dispersion of tablets in the oral cavity. In particular, this review describes in detail FDT technologies based on lyophilization, molding, sublimation, and compaction, as well as approaches to enhancing the FDT properties, such as spray-drying, moisture treatment, sintering, and use of sugar-based disintegrants. In addition, taste-masking technologies, experimental measurements of disintegration times, and clinical studies are also discussed.

Chemistry, Pharmaceutical↗