• Journal of Pharmaceutical Investigation
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• v.31 no.4
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• pp.233-239
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• 2001

Local drug delivery by using biocompatible polymers has been developed in the treatment of periodontitis for many years. In the field of dental therapy, doxycycline is usually a first choice because of its broad-spectrum antibiotic activity. The strip releases antibiotics for a week, and the polymer should be degradable after a week. In this study, we prepared and evaluated the chitosan strips and nanoparticle strips containing doxycycline hydrochloride, and studied their antiacterial activity, dissoultion, and degrability in vitro. The weight of cast strip containing a 5 mg of doxycycline hydrochloride and a 45 mg of chitosan polymer was $57.67{\pm}0.17\;mg$. The release rate of doxycycline hydrochloride from the strip was measured by HPLC. The drug released from chitosan strip and nanoparticle strip was shown to be $50\;{\mu}g/mL$ in first 24 hours. In antibacterial test showed growth inhibitory activity after 24 hrs anaerobic incubation. In vitro degradability showed demolished weight of $93.74{\pm}0.08%$ chitosan strip, $82.48{\pm}1.29%$ chitosan nanoparticle strip, $2.47{\pm}1.99%$ polycarprolactione strip (control). These results showed that, with this doxycycline hydrochloride strip, it is feasible to obtain a sustained release of the drug within the periodontal pocket for seven days which may be improve for local drug delivery system for treatment of periodontal disease.

• Journal of Dental Anesthesia and Pain Medicine
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• v.18 no.5
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• pp.287-294
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• 2018

Mandibular third molar extraction is commonly performed in dental clinics. However, the optimal method of anesthesia has not been established for this procedure. The conventional inferior alveolar nerve block is the most widely used method. However, its success rate is not high and it may lead to complications, such as aspiration and nerve injury. Therefore, various anesthesia methods are being investigated. Articaine has been proven to be efficacious in a number of studies and is being used with increasing frequency in clinical practice. In this review article, we will briefly review various local anesthesia techniques, anesthetics, and a computer-controlled local anesthetic delivery (CCLAD) system, which reduces pain by controlling the speed of drug injection, for mandibular third molar extraction.

• Biomolecules & Therapeutics
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• v.16 no.3
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• pp.226-230
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• 2008

Monoolein-based cubic liquid crystalline systems were formulated for the local delivery of oregonin and hirsutanonol for the treatment of atopic dermatitis. The liquid crystalline phase and its nanodispersion containing drugs were prepared. The skin permeation and deposition properties of the drugs were examined in normal and delipidized rat skin. The proportion of oregonin (%) deposited in normal skin after topical administration of the drugs in the form of aqueous solution, cubic phase or cubic nanodispersions were $1.53\;{\pm}\;0.46$, $3.62\;{\pm}\;0.17$ and $5.13\;{\pm}\;0.73$, and those of hirsutanonol were $2.46\;{\pm}\;0.02$, $5.44\;{\pm}\;0.27$ and $17.28\;{\pm}\;2.19$, respectively. The greater lipophilicity and thus greater skin affinity of hirsutanonol than oregonin contributed the greater amount of skin deposition. The monoolein-based liquid crystalline phases significantly increased the amount of both drugs permeated and deposited. Approximately 3.2, 2.1 and 3.0 times greater amount of oregonin, and 3.4, 2.1 and 2.2 times greater amount of hirsutanonol were deposited in delipidized skin after administration of each drug in the form of aqueous solution, cubic phase and cubic nanodispersions system, respectively, because of lowered barrier function of the delipidized skin. In this study, the effects of drug property, vehicles type and skin condition on skin deposition and permeation properties of drug were examined and concluded that monoolein-based liquid crystalline systems would be a promising formulation for the local delivery of drugs.

• Journal of Pharmaceutical Investigation
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• v.32 no.3
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• pp.165-172
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• 2002

Injectable gel composed of egg phosphatidylcholine (egg PC), hyaluronate (HA) and water was formulated for local drug delivery. The lamellar liquid crystalline structure of the egg PC/water system did not change by adding HA in the formulation. However, egg PC/HA/water gel was more resistant to erosion than the egg PC/water gel. The egg PC/HA/water and egg PC/water gels containing model drugs, tetracycline and sudan IV were prepared to perform in vitro and in vivo drug release experiments. In vitro release of tetracycline was sustained in the gel type formulations. The release rate of hydrophobic sudan IV was extremely slow. More than 99% of sudan IV remained inside the gel after 5 days. In vivo release of drugs from the air pouch model in Balb/c mice shows that lipophilic sudan IV remained for more than 10 days whereas tetracycline remained for 1 day in the pouch. The compatibility of the gels was also examined by histopathology. The gels did not cause any adverse inflammatory effect in the air pouch.

• Journal of Pharmaceutical Investigation
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• v.30 no.4
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• pp.273-278
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• 2000

Several topical preparations containing lidocaine, a widely used local anesthetic agent, have been developed and marketed recently for the treatment of premature ejaculation. In this study, microemulsion(ME)-based hydrogels containing lidocaine were prepared by dispersing ME to hydrogel bases such as Carbopol, sod. alginate, and sod. carboxymethylcellulose. Lidocaine-containing ME was thermodynamically stable over 6 months and had a diameter ranging from 10 to 100 nm. In vitro skin penetration of lidocaine from ME-based hydrogels followed apparent zero-order kinetics. ME-based hydrogel showed higher drug penetration during fifteen minutes after application than alcoholic hydrogel, reference preparation. Tail flick test in rat was introduced to compare in vivo local anesthetic effects of different hydrogels, and the results showed that ME-based hydrogels are superior to other hydrogels. In optical microscopy, recrystallization of lidocaine was observed within 5 min after application of reference hydrogel, but there was no change in ME-based hydrogels even after 30 minnute. These results indicated that ME-based hydrogels had some advantages in skin penetration, anesthetic effect and physical stability compared with alcoholic hydrogels. Finally it is possible to conclude that ME-based hydrogels containing lidocaine is a good topical drug delivery system for the treatment of premature ejaculation.

• Journal of Haehwa Medicine
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• v.19 no.1
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• pp.49-54
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• 2010

Inhalational drug is an attractive modality for local therapy of pulmonary diseases as well as systemic drug delivery. Flower of Lonicera japonica (FLJ) and flower of Tussilag farfara (FTF) are medicinal herbs for respiratory disease in traditional Korean medicine. As a preliminary study for effective inhalable formulation of FLJ and FTF, this study was to provide the toxicity and anti-inflammatory effect on murine macrophages. The dried FLJ and FTF were extracted with distilled water, filtered and freeze-dried. After treatment with FLJ and FTF extract on RAW 264.7 cells, the cell viabilities were measured by MTT assay. FLJ and FTF did not show cytotoxicity on RAW 264.7 cells. LPS stimulated RAW 264.7 cells were treated with 3 and $30\;{\mu}g/ml$ of FLJ or FTF. FLJ and FTF did not inhibit TNF-a and IL-6 secretion in both concentration of treatment. We suggest that FLJ and FTF may be useful drugs for respiratory disease. Future work will focus on the physical characteristics for inhalable formulation.

• Macromolecular Research
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• v.10 no.5
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• pp.246-252
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• 2002

In order to the development of the delivery device of long-acting local anesthetics for postoperative analgesia and control of chronic pain of cancer patient, fentnyl-loaded poly (L-lactide-co-glycolido) (PLGA, molecular weight, 5,000 g/mole; 50 : 50 mole ratio by lactide to glycolide) microspheres (FMS) were studied. FMS were prepared by an emulsion solvent-evaporation method. The influence of several preparation parameters such as initial drug loading, PLGA concentration, emulsifier concentration, oil phase volume, and fabrication temperature has been investigated on the fentanyl release profiles. Generally, the drug showed the biphasic release patterns, with an initial diffusion followed by a lag period before the onset of the degradation phase, but there was no lag time in our system. Fentanyl was slowly released from FMS over 10 days in vitro with a quasi-zero order property. The release rate increased with increasing drug loading as well as decreasing polymer concentration with relatively small initial burst effect. From the results, FMS may be a good formulation to deliver the anesthetic for the treatment of chronic pain.

• YAKHAK HOEJI
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• v.55 no.1
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• pp.1-10
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• 2011

Mastic is a bleed resin formed in pistacia lentiscus tree extract form the anacatdiaceae family. Mastic is used as a food ingredient in the Mediteraanean resin, and has been used by local inhabitants as a traditional medicine for relief of upper abdominal discomfort, dyspepsiaand peptic ulcer. Clinically, mastic has been effective in the treatment of benign gastric and duodenal, ulcers, giving symptomatic relief and endoscopically proven healing. In this study, to enhance activiteies of poorly water soluble Mastic with oils, surfactants and cosurfactants and then the mixure was microemulsified in aqueous media under condition of gentle agitation and digestive motility that would be encountered in the gastrointestinal tract. Formulation development and screening were based on phase diagrams and characteristics of resultant microemulsion. For optimum mastic formulation, microemulsions with various ratio (w/w%) of mastics, oils, surfactants and cosurfactants were prepared and their solubility was evaluated by monitoring particles size in their buffer through visual asessment and electrophoretic light scattering spectrophotomerter (ELS). In vitro activity of self microemulsified mastic (SME mastic) was determined by minimum ingibition concentration (MIC) test against a panel of Helicobacter pylori (H. pylori) clinical strains. Additionally, in vivo activity of SME masitc was investigated us mouse infected by CH275 of H. pylori. The mean diameter of SME mastic was less then 100 nm in water and SME mastic was showed similar antiboisis effect compared to tometronidazole, clarithromycin and omeproazole. Consequently, SME mastic would be effective system to exterminate H. pylori. If mastic were dose with combined treatment, mastic might augur well for effect of H. pylori eradication as good remedy.

• Journal of Periodontal and Implant Science
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• v.26 no.1
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• pp.317-333
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• 1996

The main goal of periodontal regeneration is to be achieved by epithelial exclusion, periodontal ligament cell activation or alveolar bone regeneration. The purpose of this study was to investigate on the physico- chemical and biological characteristics of biodegradable chitosan beads. Chitosan beads were fabricated by ionic gelation with sodium tripolyphosphate and they had the size in 300um diameter. As therapeutic agent, flurbiprofen was incorporated into the beads by 10, 20% loading contents. The release of drugs from the chitosan beads was measured in vitro. Also, biological activity tests of flurbiprofen loaded chitosan beads including cytotoxicity test, ihhibition of $IL-1{\beta}$ production, suppression to $PGE_2$ production, collagenase inhibition test, the ability of total protein synthesis, and tissue response were evaluated. The amount of flurbiprofen released from chitosan was 33-50% during 7 days. Minimal cytotoxicity was observed in chitosan beads. Flurbiprofen released from chitosan beads significantly suppressed the $IL-1{\beta}$ production of monocyte, $PGE_2$ production and markedly inhibited collagenase activity. Meanwhile, flurbiprofen released from this system showed increased ability for protein synthesis. Throughout 4 -week implantation period, no significant inflammatory cell infiltrated around chitosan bead and also fibroblast like cell types at the beads - tissue interface were revealed with gradual degradation of implanted chitosan beads. From these results, it was suggested that flurbiprofen loaded chitosan beads can be effectively useful for biocompatible local delivery system in periodontal regeneration.

• Maxillofacial Plastic and Reconstructive Surgery
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• v.35 no.6
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• pp.396-401
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• 2013

Chronic osteomyelitis is an infection and inflammation of the bone or bone marrow, causing ischemia in bone marrow due to lack of blood, nutrients, and oxygen supply to the bone marrow, eventually leading to necrosis of bone marrow. A current method for treatment of chronic osteomyelitis is administration of systemic antibiotics followed by removal of the infected bone and tissues. Because infected tissue of chronic osteomyelitis is surrounded by avascular necrotic bone, supply of blood and antibiotics to the infected area is diminished. For effective treatment, high plasma concentrations of antibiotics should be provided for a prolonged period. However, long term high serum level of antibiotics may result in undesirable adverse effects. For delivery of a sufficient concentration of antibiotic to the infected area while avoiding the adverse effect, implantation of a local antibiotic delivery system is suggested. One of the implantation systems that has been utilized is antibiotic impregnated polymethyl methacrylate.