• Asian Pacific Journal of Cancer Prevention
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• 제15권24호
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• pp.10705-10711
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• 2015

Oral cancer is one of the most common and lethal cancers in the world. Combination chemotherapy coupled with nanoparticle drug delivery holds substantial promise in cancer therapy. This study aimed to evaluate the efficacy and safety of two dosages of our novel pH and temperature sensitive doxorubicin-methotrexate-loaded nanoparticles (DOX-MTX NPs) with attention to the MMP-2 mRNA profile in a 4-nitroquinoline-1-oxide induced oral squamous cell carcinoma (OSCC) model in the rat. Our results showed that both IV and oral dosages of DOX-MTX NP caused significant decrease in mRNA levels of MMP-2 compared to the untreated group (p<0.003). Surprisingly, MMP-2 mRNA was not affected in DOX treated compared to cancer group (p>0.05). Our results indicated that IV dosage of MTX-DOX is more effective than free DOX (12 fold) in inhibiting the activity of MMP-2 in OSCCs (P<0.001). Furthermore, MMP-2 mRNA expression in the DOX-MTX treated group showed a significant relation with histopathological changes (P=0.011). Compared to the untreated cancer group, we observed no pathological changes and neither a significant alteration in MMP-2 amount in either of healthy controls that were treated with oral and IV dosages of DOX-MTX NPs whilst cancer group showed a high level of MMP-2 expression compared to healthy controls (p<0.001).Taking together our results indicate that DOX-MTX NPs is a safe chemotherapeutic nanodrug that its oral and IV forms possess potent anti-cancer properties on aggressive tumors like OSCC, possibly by affecting the expression of genes that drive tumor invasion and metastasis.

• 대한약학회:학술대회논문집
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• 대한약학회 2005년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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• pp.182-183
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• 2005

• Biotechnology and Bioprocess Engineering:BBE
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• 제11권6호
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• pp.526-529
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• 2006

The aim of this study was to prepare cyclosporin A-loaded liposome (CyA-Lip) as an oral delivery carrier, with their encapsulation into microspheres based on alginate or extracellular polysaccharide (EPS) p-m10356. The main advantage of liposomes in the microspheres (LIMs) is to improve the restricted drug release property from liposomes and their stability in the stomach environment. Alginate microspheres containing CyA-Lip were prepared with a spray nozzle; CyA-Liploaded EPS microspheres were also prepared using a w/o emulsion method. The shape of the LIMs was spherical and uniform, and the particle size of the alginate-LIMs ranged from 5 to $10\;{\mu}m$, and that of the EPS-LIMs was about $100\;{\mu}m$. In a release test, release rate of CyA in simulated intestinal fluid (SIF) from the LIMs was significantly enhanced compared to that in simulated gastric fluid (SGF). In addition, the CyA release rates were slower from formulations containing the liposomes compared to the microspheres without the liposome. Therefore, alginate-and EPS-LIMs have the potential for the controlled release of CyA and as an oral delivery system.

• 대한소아치과학회지
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• 제25권2호
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• pp.259-267
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• 1998

For more than two decades, many investigators have tried a variety of methods for delivering antimicrobial agents to the oral cavity with the objective of eliminating mutans streptococci. In the belief that the effectiveness of chemotherapy might be improved by a more effective delivery system, the intention of the present study was to exploit a new drug delivery system delivering chlorhexidine to the oral cavity. The vehicle delivering chlorhexidine tested in this study was self-curing acrylic resin(polymethyl methacrylate). The powder of the acrylic resin was polymerized with the 5 different liquid preparations, in which $Chlorzoin^{(R)}$ was mixed with five different monomer/Chlorzoin ratios immediately prior to the polymerization, in a stainless steel mold ($40mm{\times}40mm{\times}2mm$). A total of 50 cured resin specimens were divided into 5 groups according to the different monomer preparations. Every specimen was soaked in an airtight container filled with distilled water (100 ml) and then kept in an incubator at $37^{\circ}C$. The solutions (0.8 ml) were collected from the container at every 24 hours, and the amount of released chlorhexidine in the solutions was measured in an ultraviolet spectrophotometer at 250nm. The container was refilled with distilled water every after measurement. This procedure was repeated for 14 days. It was found that chlorhexidine was continuously released from all of the 50 specimens during the experimental period. And it was noted that the pattern of chlorhexidine release was a type of sustained-release preparation, that is, the amount of the released chlorhexidine at the first day in all 5 groups was high (p<0.0001), and then the release was decreased during the rest of the experimental period (p<0.001).

• Journal of the Korean Association of Oral and Maxillofacial Surgeons
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• 제38권5호
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• pp.264-270
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• 2012

Many oral and maxillofacial bone defects are not self-healing. Guided bone regeneration (GBR), which uses a barrier membrane to prevent the soft tissues from invading the defect to enable slower-growing bone cells to penetrate the area, was developed as a therapy in the 1980s. Although there has been some success with GBR in some clinical situations, better treatments are needed. This review discusses the concept of GBR focusing on bioactive membranes that incorporate osteoconductive materials, growth factors and cells for improved oral and maxillofacial bone regeneration.

• Journal of Pharmaceutical Investigation
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• 제37권4호
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• pp.237-242
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• 2007

The chemical formula of indapamide is 3-(aminosulfonyl)-4-chloro-N-(2,3-dihydro-2-methyl-1H-indol-l-yl)-benzamide, Indapamide is an oral antipertensive diuretic agent indicated for the treatment of hypertensive and edema. Indapamide inhibits carbonic anhydrase enzyme. Transdermal drug delivery systems, as compared to their corresponding classical oral or injectable dosage form counterparts, offer many advantages. The most important advantages are improved systemic bioavailability of the pharmaceutical active ingredients (PAI), because the first-pass metabolism by the liver and digestive system are avoided; and the controlled, constant drug delivery profile (that is, controlled zero-order absorption). Also of importance is the reduced dose frequency compared to the conventional oral dosage forms (that is, once-a-day, twice-a-week or once-a-week). Other benefits include longer duration of therapeutic action from a single application, and reversible action. For example, patches can be removed to reverse any adverse effects that may be caused by overdosing. In order to evaluate the effects of vehicles and penetration enhancers on skin permeation of Indapamide, the skin permeation rates of Indapamide from vehicles of different composition were determined using Franz cells fitted with excised hairless skins. Solubility of Indapamide in various solvents was investigated to select a vehicle suitable for the percutaneous absorption of Indapamide, The solvents used were Tween80, Tween20, Labrasol, Lauroglycol90 (LG90) and Peceol. Lauroglycol90 increase the permeability of indapamide approximately 3.75-fold compared with the control. Tween80, Tween20, Labrasol, Lauroglycol90 (LG90) and Peceol showed flux of $0.06ug/cm^2/hr,\;0.4ug/cm^2/hr,\;0.21ug/cm^2/hr,\;0.72ug/cm^2/hr,\;0.29ug/cm^2/hr$, respectively.

• 공업화학
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• 제10권2호
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• pp.201-205
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• 1999

Hydroxypropylmethylcelluloses (HPMC)는 친수성 cellulose 계통의 중합체로서 독성이 적고 가격이 저렴하여 경구용 서방출성 제제에 널리 이용되고 있다. 본 연구에서는 매트릭스로서 HPMC를 이용하여 새로운 서방출성제제인 HPMC/염산슈도에페드린계를 설계하고, 직타법에 의하여 정제를 제조하였으며, 이 팽윤될 수 있는 친수성 약물전달계를 이용하여 약물의 방출에 영향을 주는 여러 인자들이 약물의 방출속도에 미치는 영향에 대하여 조사하였다. 결과로서, HPMC/염산슈도에페드린계에서 매트릭스인 HPMC의 분자량이 클수록, HPMC의 함량이 많을수록 약물의 방출속도가 더 느려짐을 알 수 있었으며, 정제의 경도나 용출시 pH 변화에는 무관한 것으로 나타났다. 특히, 음이온 계면활성제인 sodium laurylsulfate는 HPMC로부터 염산슈도에페드린의 방출속도를 지연시키는데 큰 영향을 미치는 것으로 나타났으며, 이러한 현상은 음이온 계면활성제인 sodium laurylsulfate가 반대의 이온성을 갖는 약물인 염산슈도에페드린과 착물을 형성함으로써 약물의 용해성이 떨어져서 약물방출이 지연되는 것으로 생각된다.

• Journal of Pharmaceutical Investigation
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• 제40권5호
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• pp.297-304
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• 2010

The present work focuses on preparation of olanzapine, orally dispersing tablets by direct compression method. Effect of super disintegrant crospovidone, disintegration time, drug content on in vitro release has been studied. A factorial design was employed in formulating a prompt dispersible tablet. The selected independent variables crospovidone and fmelt showed significant effect on dependent variables i.e. disintegration time and percent drug dissolved. Disintegration time and percent drug dissolved decreased with increase in the level of crospovidone. The similarity factor $f_2$ was found to be 97.48 for the developed formulation indicating the release was similar to that of the marketed formulation. Pharmacokinetics of olanzapine after single-dose oral administration of orally disintegrating tablet in normal volunteers were evaluated and the results showed that PK parameters (Cmax, Tmax, AUC) of the designed ODT matrix were similar to those of commercial product, Zyprexa Zydis$^{(R)}$ as a reference.

• Toxicological Research
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• 제20권2호
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• pp.123-129
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• 2004

The present study was conducted to investigate the single and 2-week repeated dose toxicity of DHP2, a hydrophobic drug delivery vehicle, in ICR mice. The test article was administered orally to mice at the dose levels of 2.5, 12.5 and 37.5 g/kg for single dose toxicity study and at the dose levels of 0, 2.5, 5, and 10 g/kg for repeated dose toxicity study. In both studies, there were no treatment-related effects on mortality, clinical signs, food and water consumption, ophthalmoscopy, urinalysis, hematology, serum biochemistry, necropsy findings and organ weights of all animals treated DHP2. Based on these results, it was concluded that the 2-week repeated oral dose of DHP2 may have no toxic effect in mice at a dose level of 10 g/kg. In the condition of this study, the no-observed-adverse-effect level (NOAEL) was considered to be 10 g/kg/day for both sexes.

• Journal of Oral Medicine and Pain
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• 제25권2호
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• pp.247-251
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• 2000

Snoring, the sign of obstructive sleep apnea may cause medical problems and also a serious problem in human relationship. Some of the treatment methods for snoring patients are drug therapy, intraoral appliance, surgical operation, etc. This is a case report of a 48 years old female patient who continuously complained about snoring after uvulopalatopharyngoplasty and a remarkable improvement of the symptom after the delivery of an oral appliance.