• Journal of Pharmaceutical Investigation
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• v.35 no.2
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• pp.95-99
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• 2005

Mucoadhesive microspheres were prepared by interpolymer complexation of chitosan with poly(acrylic acid) (PAA) and solvent evaporation method to increase gastric residence time. The chitosan-PAA complex formation was confirmed by differential scanning calorimetry and swelling study. The DSC thermogram of chitosan-PAA microspheres showed two exothermic peaks for the decomposition of chitosan and PAA. The swelling ratio of the chitosan-PAA microspheres was dependent on the pH of the medium. The swelling ratio was higher at pH 2.0 than at neutral pH. The results indicated that the microspheres were formed by electrostatic interaction between the carboxyl groups of PAA and the amine groups of chitosan. The effect of various process parameters on the formation and morphology of microspheres was investigated. The best microspheres were obtained when 1.5% of the high molecular weight chitosan and 0.3% of PAA were used as an internal phase. The optimum internal phase volume was 7%. The com oil was used as the external phase of emulsion, and span 80 was used as the surfactant. The prepared microspheres had spherical shape.

• Journal of Pharmaceutical Investigation
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• v.31 no.3
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• pp.173-180
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• 2001

The physicochemical characteristics such as glass transition temperature (Tg), surface energy, swelling and FT-IR of [P(AA-co-PEGMM)], a copolymer of acrylic acid (AA) and polyethyleneglycol monoethylether mono methacrylate (PEGMM), were evaluated. The Tg of [P(AA-co-PEGMM)] decreased with increasing PEGMM content. [P(AA-co-PEGMM)] with 18 mole% PEGMM had the Tg of about $40^{\circ}C$, the similar physiological temperature of human. Moreover, [P(AA-co-PEGMM)] with lower PEGMM content had higher hydration and expected lower mucoadhesive strengths. To predict the mucoadhesiveness of [P(AA-co-PEGMM)] films, the contact angle of films were measured. With the increasing content of PEGMM of films, the contact angle was increased and the higher mucoadhesive forces was expected. ATR-FTIR studies revealed that the addition of the PEG moiety in AA increased the potential of hydrogen bonding for [P(AA-co-PEGMM)] as compared to cross linking polyacrylic acid (cr-PAA) because the oxygen in the repeat unit of PEG contributed in the formation of hydrogen bonding in the presence of mucin solution.

• Biotechnology and Bioprocess Engineering:BBE
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• v.10 no.6
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• pp.516-521
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• 2005

Drug delivery to the lymphatic system may be important in terms of the treatment with lymphatic involvement, such as tumor metastases and immunization. Especially, drug transport via the intestinal lymphatics after oral administration has been attracted lots of interests. The purpose of this study was to prepare cyclosporin A (CSA)-loaded liposomes, with different characteristics, and evaluate their mucoadhesivity. Three liposome preparations were formulated: cationic stearylamine liposomes (SA-Lip), anionic phosphatidylserine liposomes (PS-Lip), Polymer (chitosan)-coated liposomes (CS-Lip), and characterized. The liposome preparations were found to be spherical in shape, with PS-Lip being the smallest. The liposome preparations exhibited entrapment efficiencies in the order: PS-Lip $(52.5{\pm}2.9%)$ > SA-Lip $(48.8{\pm}3.3%)$ > CS-Lip $(41.7{\pm}4.2%)$. Finally, mucoadhesive tests were carried out using rat intestine, with SA-Lip (67%) showing the best adhesive rate of the three preparations (PS-Lip: 56%, CS-Lip: 61%). These results suggest that a positive charge on the surface of drug carriers may be an important factor for the intestinal drug delivery.

• Journal of Pharmaceutical Investigation
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• v.25 no.4
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• pp.339-345
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• 1995

For the effective treatment of aphthous stomatitis, the matrix type mucoadhesive patches containing triamcinolone acetonide have been formulated. The drug layer was obtained by drying the polymer gel which was prepared with carbomer 934P, ammoniomethacrylate copolymer, titanium dioxide and polyethylene glycol 400. The effects of the content of additives on physical characteristics of the polymer gel and the drug layer were evaluated. The addition of carbomer increased the yield point and the zero-shear viscosity of polymer gel as well as the thickness, the water absorption ratio, the adhesive time and $T_{50%}$ of drug layer. The adhesive time and the water absorption ratio of drug layer were also improved by the addition of ammoniomethacrylate copolymer, but the addition of titanium dioxide had decreased the zero-shear viscosity of polymer gel and the adhesive time of drug layer.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.408.1-408.1
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• 2002

A interpolymer complexes composed of poly(acrylic acid)(PAA) and po!y(vinyl alcohol)(PVA) were prepared by template polymerization of acrylic acid in the presence of PVA for mucoadhesive drug delivery. FT -IR results showed that the PAA/PVA interpolymer complex was formed by hydrogen bonding between the carboxyl groups of PAA and the hydroxyl group of PVA. The dissolution rate or the swelling ratio of the PAA/PVA interpolymer complexes was dependent on the pH and molecular weight of PVA that was used as a template. (omitted)

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.231.1-231.1
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• 2003

Mucoadhesive microsphere was prepared by interpo]ymer complexation of po]y(acrylic acid) (PAA) with po]y(vinyl pyrrolidone) (PVP) using solvent diffusion method. The loading efficiency of acetaminophen into the microsphere was 91.3 ${\pm}$ 6.5%. The release rate of acetaminophen from the PAA/PVP complex microspheres was slower than that from PVP microspheres at pH 2.0 and 6.8. The dissolution of microspheres made of the complex was significantly slower than those made of PVP due to H-bond between PVP and PAA. As a result, the release rate of acetaminophen from the complex microspheres was slower than that from PVP microspheres.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.235.2-235
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• 2003

To develop the buccal delivery system of rhEGF for the treatment of buccal mucosal ulcer, polymer films and hydrogels were investigated. Methods: Hydrogels for thermosenstive sol/gel systems were prepared by the cold method (Schmolka, 1972). And mucoadhesive films were prepared by mixing sod. alginate/polycarbophil 974p. To find an optimum buccal mucosal adhesive gel or film, the gel strength of the poloxamer and sod. alginate/polycarbophil 974p hydrogels were determined by the Simple Rheology Method and their mucoadhesiveness were measured by the Instron (M 4400, Instron Co., U.S.A.) method. (omitted)

• 한국생물공학회:학술대회논문집
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• 2005.04a
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• pp.579-579
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• 2005

• Journal of Pharmaceutical Investigation
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• v.24 no.3
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• pp.155-165
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• 1994

Some mucoadhesive polymers such as hydroxypropylcelluose (HPC) and carbopol-934 (CP) have been employed for the preparation of mucoadhesive polymeric systems, and their physical properties including mucoadhesion, swelling, and drug release were evaluated. A new simple experimental technique that can quantitatively measure the bioadhesive properties of various polymeric systems has been developed by the methods of detachment force test. As the polymeric systems, the discs of freeze-dried HPC/CP solid dispersions were prepared. The mucosa used in these tests were upper, middle, and lower parts of small intestine of male rats weighing $300{\sim}350\;g$. Detachment forces were increased as the mole fraction of CP increased in discs of HPC/CP solid dispersions. In the points of intestinal site dependence of mucoadhesion, the solid dispersions revealed non-specific mucoadhesion to the intestine. Swelling and drug release characteristics of mucoadhesive polymeric systems were studied extensively to find out the feasibility for the oral controlled delivery systems. Swelling ratio, expressed as the final height/initial height, has been determined in various pH buffer solutions. Hydrochlorothiazide (HCT) was employed as a model drug for release study. Apparent swelling and drug release rate constants, $K_s$ and $K_r$ respectively, were obtained from the square-root time plot of either swelling ratio or released amount of drug, particularly for the time periods before reaching the equilibrium. As a result, the swelling ratio of HPC/CP solid dispersions was increased as the weight percentage of CP increased. Similarly, the release of HCT from the solid dispersions was dependent on pH changes and CP contents, resulted in the slower release of HCT with the increases of pH and CP contents.

• Journal of Microbiology and Biotechnology
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• v.29 no.5
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• pp.721-730
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• 2019

The probiotic Lactobacillus acidophilus KBL409 was encapsulated with alginate (Al) and alginate-chitosan (Al/Chi) through extrusion method. The sizes and zeta potentials of microspheres were measured to confirm encapsulation. To evaluate the protective effect of microspheres against gastrointestinal fluids, all the samples were exposed to simulated gastric fluids (SGFs, pH 1.5) at $37^{\circ}C$ for 1 or 2 h, followed by incubation with simulated intestinal fluids (SIFs, pH 6.5) for 2 h. The mucoadhesive ability of microspheres was evaluated using the intestinal epithelial cell line HT29-MTX. To extend the shelf-life of probiotics, lyoprotectants such as disaccharide and polysaccharide were mixed with free or encapsulated cells during the freeze-drying process. The size of the microspheres demonstrated a narrow distribution, while the zeta potentials of Al and Al/Chi-microspheres were $-17.9{\pm}2.3$ and $20.4{\pm}2.6mV$, respectively. Among all the samples, Al/Chi-encapsulated cells showed the highest survival rate even after exposure to SGF and SIF. The mucoadhesive abilities of Al and Al/Chi-microspheres were higher than 94%, whereas the free L. acidophilus showed 88.1% mucoadhesion. Ten percent of sucrose showed over 80% survival rate in free or encapsulated cells. Therefore, L. acidophilus encapsulated with Al and Al/Chi-microspheres showed higher survival rates after exposure to the gastrointestinal tract and better mucoadhesive abilities than the free cells. Also, sucrose showed the highest protective effect of L. acidophilus during the freeze-drying process.