• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 춘계총회 및 학술대회
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• pp.206.1-206.1
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• 2000

• 한국항공우주학회지
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• 제36권6호
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• pp.587-593
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• 2008

본 연구의 목적은 신체 조직의 손상을 최소화할 수 있는 경피(transdermal) 및 국부적인(topical) 약물전달을 가능하게 하는 마이크로 입자가속시스템 개발에 있다. Ballistic 역학을 기반으로 하는 본 방법을 통하여 체순환을 위한 경피 및 국부적 약물 전달이 가능하다. 얇은 금속 포일의 한 쪽 면에 마이크로 입자들을 얹어놓고 뒷면에 레이저를 조사하면 충격파가 발생하고, 이 충격파는 포일을 통과하며 포일의 끝에서 금속-공기간의 acoustic impedance 차이로 expansion wave로 반사되어 포일이 반대 방향으로 변형을 일으키게 한다. 이 순간적인 변형으로 인해 포일에 붙어있던 마이크로 입자들이 가속되어 튕겨 나가게 된다. 입자들이 가속되는 속도가 굉장히 크기 때문에 이들은 신체 조직을 침투할 만한 충분한 운동량을 갖고 있다. 입자들의 침투 여부를 확인하기 위해 우리는 5${\mu}m$ 크기의 코발트 입자들을 연조직을 묘사하는 젤라틴에 가속시켰으며, 주목할 만한 침투 깊이를 얻으며 실험에 성공하였다.

• 폴리머
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• 제37권3호
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• pp.347-355
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• 2013

본 연구에서는 항산화제인 quercetin과 그 배당체인 rutin의 피부 흡수를 증진시키기 위한 전달체로 다공성 셀룰로오스 하이드로젤을 제조하였고 그 특성을 연구하였다. Quercetin과 rutin을 위한 최적의 하이드로젤을 가교제인 12% epichlorohydrin(ECH)과 2% 셀룰로오스를 반응용액으로 하여 만들었다. 플라보노이드 함유 하이드로젤의 방출 실험에서, quercetin의 방출은 $10{\sim}500{\mu}M$ 농도에서 확산 속도에 영향을 받았으나, rutin의 경우는 비교적 낮은 농도($10{\sim}50{\mu}M$)에서 하이드로젤의 침식에 의한 방출이 지배적이었다. 플라보노이드에 대한 하이드로젤의 포집효율과 방출량은 quercetin보다도 rutin에서 모두 크게 나타났다. 하지만, Franz diffusion cell을 이용한 피부 투과 실험에서 quercetin이 rutin보다 1.2배나 더 큰 피부 투과능을 나타냈다. 플라보노이드 함유 하이드로젤은 대조군인 20% 1,3-butylene glycol phosphate buffer에서보다도 더 큰 경피 투과능을 나타내었다. 이 결과들은 난용성 항산화제인 플라보노이드의 피부 흡수 증진 전달체로서 셀룰로오스 다공성 하이드로젤이 이용 가능성이 있음을 시사한다.

• 대한정형외과학회지
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• 제55권6호
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• pp.527-533
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• 2020

목적: 슬관절 인공관절 전치환술(total knee arthroplasty, TKA) 후 통증 조절을 위한 부프레노르핀 경피 패치(buprenorphine transdermal patch, BTDP)의 흉부 적용 및 무릎 적용 효과를 비교하고자 하였다. 대상 및 방법: 2018년 8월부터 2019년 8월까지 TKA를 시행한 231명 중에서 나이, 성별, 체질량 지수(body mass index) 등을 고려한 환자-대조군 연구를 통해 선별된 200예를 대상으로 후향적으로 분석하였다. BTDP를 적용하기 전후에 Numeric Rating Scale (NRS), 부작용 및 순응도를 측정하였으며 흉부 적용군(A군=100명)과 무릎 적용군(B군=100명) 사이의 모든 측정치를 비교하였다. 결과: 술 후 BTDP 적용군 간의 휴식 시 NRS는 전반적으로 비슷하였으나 B군의 술 후 2, 3일째 오후, 5일, 6일, 7일째 휴식 시 NRS는 A군의 NRS보다 통계적으로 유의하게 낮았다. BTDP 적용 후 중추신경계, 위장관계 부작용은 B군에서 유의하게 낮았다. 심혈 관계, 피부의 부작용은 두 군 간에 유의한 차이가 없는 것으로 나타났다. 통증 조절을 위한 지속적인 BTDP 유지에서도 B군이 A군에 비하여 유의하게 높게 나타났다. 결론: TKA 후 BTDP를 통증이 있는 무릎 관절에 직접 적용하는 것은 술 후 초기 통증 조절에 있어 우수한 결과를 보였으며 기존의 흉부 적용 방법보다 부작용 빈도를 줄여 환자의 순응도를 높일 수 있는 유용한 방법으로 판단된다.

• Archives of Pharmacal Research
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• 제26권8호
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• pp.644-648
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• 2003

To investigate the feasibility of developing a new ondansetron transdermal system, the effects of vehicles and penetration enhancers on the in vitro permeation of ondansetron hydrochloride (OS) from a pressure-sensitive adhesive (PSA) matrices across dorsal hairless mouse skin were studied. Vehicles employed in this study consisted of various ratios of propylene glycol monocaprylate (PGMC)-diethylene glycol monoethyl ether (DGME) co-solvents and PGMC-propylene glycol (PG) co-solvents with 3% oleic acid. $Duro-Tak^\circledR$ 87-2100 and $Duro-Tak^\circledR$ 87-2196 were used as PSAs. The concentration of DGME in PGMC-DGME co-solvent system affected the release rate; as the concentration of DGME increased, the release rate decreased. The cumulative release amount of OS increased as the ratio of PSA to drug solution decreased. The permeation flux was also primarily affected by the amount of PSAs; as the amount decreased, the permeation flux increased. The overall fluxes from matrix formulations were significantly lower when compared to those obtained from solution formulations. The ratio of PG to PGMC did not affect permeation flux, while the lag time decreased significantly from $5.14\pm3.31 to 0.31\pm0.12$ h as the PG increased from 40% to 60%.

• Journal of Pharmaceutical Investigation
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• 제27권4호
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• pp.303-311
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• 1997

Proliposomal patch of clenbuterol, ${\beta}_2-agonist$ bronchodilator, was prepared and its feasibility as a novel transdermal drug delivery system was examined. Proliposomal granules containing clenbuterol was prepared by a standard method using sorbitol and lecithin with (Rx 2) or without cholesterol (Rx 1). The porous structure of sorbitol in the proliposomes was maintained allowing tree flowability of the granules. Following contact with water, the granules were converted probably to liposomes almost completely within several minutes. It indicates that proliposomes may be hydrated, when they are applied on the skin under occlusive condition in vivo, by the sweat to form liposomes. Clenbuterol release from Rx 1 and Rx 2 proliposomes to pH 7.4 isotonic phospate buffer (PBS) across cellulose membrane (mol. wt. cut-off of 12000-14000) was retarded significantly compared with that from the mixture of clenbuterol powder and blank proliposomes. Interestingly, proliposomes prepared with lecithin and cholesterol (i.e., Rx 2 proliposomes) showed much more retarded release of clenbuterol than proliposomes prepared only with lecithin (i.e.. Rx 1 proliposomes), indicating that clenbuterol release from proliposomes can be controlled by the addition of cholesterol to the proliposomes. Proliposomal patches were prepared using PVC film as an occlusive backing sheet, two sides adhesive tape (urethane, 1.45 mm thickness) as a reservoir for proliposome granules and Millipore MF-membrane (0.45 mm pore size) as a drug release-controlling membrane. Rx 1 or Rx 2 proliposomes containing 4.6 mg of clenbuterol were loaded into the reservoir of the patch. Clenbuterol release from the patches to pH 7.4 PBS was determined using USP paddle (50 rpm)-over-disc release method. Clenbuterol release from the proliposomal patches was much more retarded even than from a matrix type clenbuterol patch (Boehringer Ingelheim ltd). Being consistent with clenbuterol release from the proliposomal granules, the release from the patches was highly dependent on the presence of cholesterol in the proliposomes : Patches containing Rx 2 proliposomes showed several fold slower drug release than patches containing Rx 1 proliposomes. When the patch containing Rx 1 proliposomes was applied on to the back of a hair-removed rat, clenbuterol concentration in the rat blood was maintained during 6-72 hrs. Transdermal absorption of clenbuterol from the patch was accelerated when the patch was prehydrated with 50 ml of pH 7.4 PBS before topical application. Above results indicate that sustained transdermal delivery of clenbuterol is feasible using proliposomal patches if the cholesterol content and pore size of the release rate-controlling membrane of patches, for example, are appropriately controlled.

• Journal of Pharmaceutical Investigation
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• 제37권4호
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• pp.243-247
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• 2007

Retinoids have many important and diverse functions and particularly, have been widely used as anti-aging agent and for the treatment of acne and psoriasis in cosmetics. However, retinoids have low stability against the air, light, water, oxygen and heat, thus, to stabilize the retinoids in formulations is very critical procedure. In this study, cubic liquid crystalline phase of monoolein was applied to stabilize the retinylpalmitate (RP) and to enhance the transdermal permeation. Cubic liquid crystalline phase significantly enhanced the stability of RP. After 15 days, the content of RP in the cubic formulation was 94.7% while the content of RP in ethanol solution was below 0.5% at room temperature. Although BHT containing crystalline phase showed the slightly increased stability of RP, there were no significant differences in RP stability between with or without antioxidants (ascorbic acid, ${\alpha}$-tocopherol, BHT, BHA) at $40^{\circ}C$. The skin retention of RP in crystalline formulations was approximately $5.3{\sim}6.4$ times greater than that of o/w cream formulation. Incorporation of RP into cubic liquid crystalline phase of monoolein effectively stabilized the RP and worked as excellent topical vehicle for RP. Liquid crystalline phase is considered to be suitable formulation for RP for topical delivery system as a stabilizer and permeation enhancing agent.

• Archives of Pharmacal Research
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• 제28권9호
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• pp.1097-1102
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• 2005

An O/W microemulsion system was developed to enhance the skin permeability of ace-clofenac. Of the oils studied, Labrafil? M 1944 CS was chosen as the oil phase: of the microemulson, as it showed a good solubilizing capacity. Pseudo-ternary phase diagrams were constructed to obtain the concentration range of oil, surfactant, Cremophor ELP, and co-surfactant, ethanol, for micoemulsion formation. Eight different formulations with various values of oil of $6-30\%$, water of $0-80\%$, and the mixture of surfactant and co-surfactant (at the ratio of 2) of $14-70\%$. The in vitro transdermal permeability of aceclofenac from the microemulsions was evaluated using Franz diffusion cells mounted with rat skin. The level of aceclofenac permeated was analyzed by HPLC and the droplet size' of the microemulsions was characterized using a Zetasizer Nano-ZS. Terpenes were added to the microemulsions at a level of $5\%$, and their effects on the skin permeation of aceclofenac were investigated. The mean diameters of the microemulsions ranged between approximately $10\~100nm$, and the skin permeability of the aceclofenac incorporated into the microemulsion systems was 5-fold higher than that of the ethanol vehicle. Of the various terpenes added, limonene had the best enhancing ability. These results indicate that the microemulsion pystem studied is a promising tool for the percutaneous delivery of aceclofenac.

• 한국응용과학기술학회지
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• 제32권1호
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• pp.157-164
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• 2015

올레아놀릭산은 항암, 신행혈관 생성방지, 항염증, 항산화 및 주름 개선효과가 알려져 있다. 본 연구자들은 천연에서 분리한 올레아놀릭산의 항산화효과에 주목하여 연구하였고 미백효과가 있음을 확인하였다. 본 연구에서는 천연유래의 폴리글리세릴계 계면활성제를 사용하여 간단한 교반만으로 올레아놀릭산을 안정화하였고 고가의 장비인 마이크로풀루다이저를이용하여 제조한 레시틴리포좀과 경피흡수투과율을 비교하였다. 0.4% 올레아놀릭산을 안정화한 폴리글리세릴 나노에멀젼의 12시간 후 경피흡수투과율은 95%였다. 레시틴 리포좀은 92%로 유사하였으나 폴리글리세릴 나노에멀젼은 3시간 경피 흡수투과율이 65%로 레시틴리포좀의 45%에 비해 속방성의 특징을 보였다. 인체대상 임상시험결과 올레아놀릭산을 무배합한 대조군에 비해 올레아놀릭산을 배합한 폴리글리세릴 나노에멀젼은 MEXAMETER의한 멜라닌 색소감소효과가 2주차 25%, 4주차 58%, 8주차 58%이상 높았다.

• Journal of Pharmaceutical Investigation
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• 제38권1호
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• pp.45-50
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• 2008

5-Fluorouracil (5-FU) is an antimetabolic of the pyrimidine derivatives that is used in chemotherapy for the treatment of several types of cancer. 5-FU have poor oral absorption and short biological half-time and strong side effects. Microneedle introduced to find a solution of problems. Microneedle device with roll was manufactured for transdermal delivery of various drugs. 5-FU was mixed in non-ionic surfactant such as tween 20 and tween 80. Camscope was used to analysis the permeation magnitude of treated skin by microneedle and trypan blue staining. The 5-FU solution with surfactant measured by ZETA-potential analysis system for stability of solution. The skin permeation rate of 5-FU determined by HPLC. We confirmed that cross treated skin was dyed more deeply than parallel treated skin through trypan blue staining. The results indicate that skin permeation rate of 5-FU was increased with the treatment types and treatment times.