• Journal of Pharmaceutical Investigation
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• 제32권1호
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• pp.1-6
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• 2002

The mucoadhesive characteristics of [P(AA-co-PEGMM)] films by estimating the glass transition temperature $(T_g)$, analyzing surface energy and studying FT-IR was previously reported. In this study, the possibility of buccal mucoadhesive dosage form of [P(AA-co-PEGMM)] films by mucoadhesive force measurements and dissolution tests were also investigated. Mucoadhesiveness of [P(AA-co-PEGMM)] films was compared with cr-PAA and cr-PEGMM films crosslinked with 3% ethyleneglycol dimethacrylate (EGDMA). The buccal mucoadhesive force of [P(AA-co-PEGMM)] films increased with increasing content of PEGMM. [P{AA-co-PEGMM (18 mole%)}] films showed a significantly greater mucoadhesiveness than cr-PAA and cr-PEGMM films. The mucoadhesive force measured in normal saline (pH 5.0) was higher than that measured in phosphate buffer (pH 6.8) because of the pH dependence of hydrogels with carboxyl ions within the PAA. Moreover, the mucoadhesive force of [P{AA-co-PEGMM (18 mole%)}] films was at maximum after 2 hr attachment of buccal mocosa and it was maintained over $1\;N/cm^2$ for up to 10 hr. In dissolution studies, the release of butorphanol tartrate from [P(AA-co-PEGMM)] films increased with increasing PEGMM content, and films prepared with 18 mole% PEGMM gave almost zero order release kinetics.

• Advances in Traditional Medicine
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• 제7권1호
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• pp.51-64
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• 2007

Mucus is an aqueous gel complex with a constitution of about 95% water, high molecular weight glycoprotein (mucin), lipid, salts etc. Mucus appears to represent a significant barrier to the absorption of some compounds. Natural mucoadhesive agent was isolated and purified from the aqueous extract of the seeds of prosopis pallida (PP). Formulated tablet with the isolated material by wet granulation method. Some natural edible substances are in consideration for candidates as mucoadhesive agents to claim more effective controlled drug delivery as an alternative to the currently used synthetic mucoadhesive polymers. Subjected the materials obtained from natural source i.e. PP and standard synthetic substance, sodium carboxymethyl cellulose for evaluation of mucoadhesive property by various in vitro and in vivo methods. Through standard dissolution test and a model developed with rabbit, evaluated in vitro controlled release and bioadhesive property of theophylline formulation. Mucoadhesive agent obtained from PP showed good mucoadhesive potential in the demonstrated in vitro and in viνo models. The results suggest that the mucoadhesive agent showed controlled release properties by their application, substantially. In order to assess the gastrointestinal transit time in vivo, a radio opaque X-ray study performed in healthy rabbit testing the same controlled release formulation with and without bioadhesive polymer. Plasma levels of theophylline determined by the HPLC method and those allowed correlations to the in vitro mucoadhesive study results. Better correlation found between the results in different models. PP may acts as a better natural mucoadhesive agent in the extended drug delivery system.

• 폴리머
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• 제37권5호
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• pp.625-631
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• 2013

점막접착 기능은 인체의 다양한 장기에 적용되는 의료용 접착제에 요구되는 중요한 특성이며, 점막접착 기능을 갖는 고분자를 개발하기 위하여 많은 연구가 이루어지고 있다. 최근 많은 연구자들이 생체모방 기술을 통한 점막접착형 고분자를 개발하고 있고, 그 중 해양 부착 생물인 홍합의 접착 기능 및 특성이 접착제 연구의 주요 대상이 되어왔다. 본 연구에서는 홍합 접착 물질 속에 과량 존재해 표면 접착 기능을 발현하는 카테콜 구조가 도입된 생체모방형 고분자를 합성하였고, 핵자기공명분광법 및 젤투과크로마토그래피를 사용하여 분석하였다. In vitro 상에서 돼지의 소장점막하조직 sheet를 준비하여 전단 시편을 제작하고 점막접착력을 측정하였다. 점막접착형 고분자는 현재 상업적으로 사용되고 있는 대조군인 피브린글루와 비교할 때 월등한 접착력을 보였다. 또한, 다양한 인자를 변화시키며 최적의 점막접착력을 나타내는 조건을 확립하였다. 이러한 결과들을 토대로 우수한 점막접착형 특성을 나타내는 고분자를 개발하였고 다양한 임상적용 및 의료용 기기에 도입가능한 소재의 기초연구를 수행하였다고 사료된다.

• Archives of Pharmacal Research
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• 제28권5호
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• pp.612-618
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• 2005

A mucoadhesive microsphere was prepared by an interpolymer complexation and solvent evaporation method, using chitosan and poly(acrylic acid) (PAA), to prolong the gastric resid ence time of the delivery system. The Fourier transform infrared results showed that microspheres were formed by an electrostatic interaction between the carboxyl groups of the PAA and the amine groups of the chitosan. X-ray diffraction and differential scanning calorimetry analysis showed that the enrofloxacin in the chitosan-PAA microsphere was molecularly dispersed in an amorphous state. Scanning electron microscopy of the surface and the quantity of mucin attached to the microspheres indicated that chitosan-PAA microspheres had a higher affinity for mucin than those of chitosan alone. The swelling and dissolution of the chitosan-PAA microspheres were found to be dependent on the pH of the medium. The rate of enrofloxacin released from the chitosan-PAA microspheres was slower at higher pH; therefore, based on their mucoadhesive properties and morphology, the chitosan-PAA microspheres can be used as a mucoadhesive oral drug delivery system.

• Journal of Pharmaceutical Investigation
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• 제29권2호
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• pp.127-136
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• 1999

In order to eliminate demerits of conventional dosage forms, dipotassium glycyrrhizate was formulated as a slim mucoadhesive film type dosage form. The mucoadhesive drug layer gel containing dipotassium glycyrrhizate was prepared using $Noveon^{\circledR}$ AA-1, hydroxypropylcellulose-M, ethylcellulose N 100 and citric acid, and the protective layer gel by using ethylcellulose N 100, $Eudragit^{\circledR}$ RS and castor oil. The viscosity of drug layer gel of mucoadhesive film was enhanced as the increased amount of $Noveon^{\circledR}$ AA-1 or hydroxypropyl cellulose-M. The drug content was unifonnly $1160{\pm}14.6\;{\mu}g$, and was varied within 3.5%. The optimum film dosage form showed a good fluidity and malleability of drug layer, with 179 g of thickness, pH 5.7, 411 min of in vitro adhesion time and 172 g in gravity adhesive strength. The release time of drug from the mucoadhesive film was significantly shorter but was delayed when polymers such as ethylcellulose was added. From these results, the new mucoadhesive film may be effective for the treatment of aphthous stomatitis.

• 생체재료학회지
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• 제22권4호
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• pp.249-258
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• 2018

Background: Mucoadhesive polymers, which may increase the contact time between the polymer and the tissue, have been widely investigated for pharmaceutical formulations. In this study, we developed a new polysaccharide-based mucoadhesive polymer with thermogelling properties. Methods: Hexanoyl glycol chitosan (HGC), a new thermogelling polymer, was synthesized by the chemical modification of glycol chitosan using hexanoic anhydride. The HGC was further modified to include thiol groups to improve the mucoadhesive property of thermogelling HGC. The degree of thiolation of the thiolated HGCs (SH-HGCs) was controlled in the range of 5-10% by adjusting the feed molar ratio. The structure of the chemically modified polymers was characterized by $^1H$ NMR and ATR-FTIR. The sol-gel transition, mucoadhesiveness, and biocompatibility of the polymers were determined by a tube inverting method, rheological measurements, and in vitro cytotoxicity tests, respectively. Results: The aqueous solution (4 wt%) of HGC with approximately 33% substitution showed a sol-gel transition temperature of approximately $41^{\circ}C$. SH-HGCs demonstrated lower sol-gel transition temperatures ($34{\pm}1$ and $31{\pm}1^{\circ}C$) compared to that of HGC due to the introduction of thiol groups. Rheological studies of aqueous mixture solutions of SH-HGCs and mucin showed that SH-HGCs had stronger mucoadhesiveness than HGC due to the interaction between the thiol groups of SH-HGCs and mucin. Additionally, we confirmed that the thermogelling properties might improve the mucoadhesive force of polymers. Several in vitro cytotoxicity tests showed that SH-HGCs showed little toxicity at concentrations of 0.1-1.0 wt%, indicating good biocompatibility of the polymers. Conclusions: The resultant thiolated hexanoyl glycol chitosans may play a crucial role in mucoadhesive applications in biomedical areas.

• 약학회지
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• 제42권2호
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• pp.187-195
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• 1998

In order to ameliorate disadvantages of buccal ointments and mucoadhesive tablets used for the treatment of aphthosis, a thin mucoadhesive patch containing triamcinolone acetoni de was designed and evaluated for the pharmaceutical properties. The adhesive gel layer consisting of Noveon AA-1, hydroxypropylcellulose-M and ethylcellulose N 100, and the protective gel layer of ethylcellulose N 100, Eudragit RSPO and castor oil have been formulated and various properties such as viscosity of drug gel layer, thickness, in vitro adhesion time, adhesive strength, surface pH, content uniformity and drug release are tested. The mean viscosity of drug-containing gel layer was found to increase with increasing amount of Noveon OAA-1 or hydroxypropylcellulose-M. The optimum formulation showed the thickness of 171 ${\mu}$m, surface pH of 4.6, in vitro adhesion time of 8 hours and adhesive strength of 272.7g/sheet. The drug content of each patch was relatively homogeneous with the value of 273${\pm}$6.77g. Drug release study showed that compared to mucoadhesive tablet, the patch showed a faster drug release. Drug release was delayed by hydroxypropylcellulose-M, but not by ethylcellulose N 100. The patches prepared were nonirritant and the muco adhesion was better than the commercial product (AftachR) on the market. Based on these results, this mucoadhesive patch is expected to be an effective dosage form for the treatment of aphthosis.

• 폴리머
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• 제36권2호
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• pp.182-189
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• 2012

본 연구에서는 전자빔을 이용하여 폴록사머 하이드로젤을 제조하여 구강 점막부착성 약물전달체로서의 특성을 평가하고자 하였다. 온도감응성을 나타내는 폴록사머 고분자의 말단에 가교반응을 위한 비닐기를 도입한 후, 방사선 가교반응을 이용하여 하이드로젤을 제조하였다. 점착성 향상을 위한 첨가제로 점착성 고분자인 카보폴을 첨가하여 하이드로젤을 제조하였고, 카보폴이 점막부착성과 서방성 방출에 미치는 영향을 알아보았다. 결과적으로, 폴록사머 고분자의 말단 개질과 카보폴의 첨가에 의해 하이드로젤의 기계적 물성과 점막부착성이 향상되었고, 약물방출실험 결과 약물이 방출되는 속도가 지연되는 결과를 확인하였다.

• 대한약학회:학술대회논문집
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• 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.236.1-236.1
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• 2002

Mucosal administration of drug or therapeutic gene is emerging as a new route of delivery for systemic and local therapeutics. Previously. in situ gelling system has been applied to chemical drug such as acetaminophen. insulin. prostaglandin E1. and clotrimazole. Plasmid DNA has not been delivered in form of in situ gelling vehicles. To improve the intranasal absorption of plasmid DNA. we designed delivery systems composed of provide of in 냐셔 gelling and mucoadhesive polymers. (omitted)

• Journal of Pharmaceutical Investigation
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• 제35권5호
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• pp.369-373
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• 2005

The objectives of the current work is to understand the factors impacting the formulation and performance of a Carbopol mucoadhesive buccal delvery system for a model peptide drug, $[D-Ala{^2},\;D-Leu{^5}]$enkephalin (DADLE, Mw=569.7) with comparable chemical and enzymatic stability. Specifically, in vitro buccal DADLE delivery from the cross-linked poly(acrylic acid) (PAA) hydrogel system was characterized. In addition, the influences of several penetration enhancers on the ex vivo buccal absorption of DADLE were also studied. In this study, the PAA hydrogels generally swell to 100% of their original weight in the phosphate pH 7.4 buffer. The water penetration into the PAA hydrogel occurred based on a zero-order kinetics for the first 60 min and steadily decreased afterwards. From the release study, it can be seen that the initial DADLE release was so rapid and the rate of release of DADLE decreased as the time elapsed. The porcine buccal tissue was found to be permeable to DADLE with a flux value of $0.07%/cm{^2}/hr({\pm}0.01\;SD)$. From the ex vivo diffusion study, it was found that sodium taurodihydrofusidate showed a greater degree of enhancement compared to the phospholipids with an Enhancement Ratio (ER) of 8.7 compared to 2.7 and 1.9 for didecanoylphosphatidylcholine and lysophosphatidylcholine, respectively. The work encompassed within this paper has demonstrated the feasibility of using the PAA hydrogel delivery system with its good mucoadhesive properties for the buccal delivery of peptides.