• Biomolecules & Therapeutics
• /
• 제21권2호
• /
• pp.173-179
• /
• 2013

Objective of present study was to prepare and characterize self-nanoemulsifying drug delivery system (SNEDDS) of lutein and to evaluate its effect on bioavailability of warfarin. The SNEDDS was prepared using an oil, a surfactant, and co-surfactants with optimal composition based on pseudo-ternary phase diagram. Effect of the SNEDDS on the bioavailability of warfarin was performed using Sprague Dawley rats. Lutein was successfully formulated as SNEDDS for immediate self-emulsification and dissolution by using combination of Peceol as oil, Labrasol as surfactant, and Transcutol-HP or Lutrol-E400 as co-surfactant. Almost complete dissolution was achieved after 15 min while lutein was not detectable from the lutein powder or intra-capsule content of a commercial formulation. SNEDDS formulation of lutein affected bioavailability of warfarin, showing about 10% increase in $C_{max}$ and AUC of the drug in rats while lutein as non-SNEDDS did not alter these parameters. Although exact mechanism is not yet elucidated, it appears that surfactant and co-surfactant used for SNEDDS formulation caused disturbance in the anatomy of small intestinal microvilli, leading to permeability change of the mucosal membrane. Based on this finding, it is suggested that drugs with narrow therapeutic range such as warfarin be administered with caution to avoid undesirable drug interaction due to large amount of surfactants contained in SNEDDS.

• 한국의학물리학회지:의학물리
• /
• 제18권3호
• /
• pp.161-166
• /
• 2007

공모양의 단단한 종양안에서 수동조준된 약물의 전달에 관한 모델이론이 적절한 경계조건과 초기조건하에서 픽의 확산법칙으로부터 유도된다. 종양안의 농도는 초기값이 일정하면 시간과 지름의 함수로 나타난다. 생각실험(사고실험)으로부터 예측되는 바와 같이, 농도는 시간이 경과함에 따라 평형값에 접근한다. 시간에 따른 농도의 변화는 조직안의 약물의 확산계수, 종양의 크기, 주입된 약물의 양, 경계면에서의 농도의 물매(gradient)에 의해 결정된다.

• Journal of Pharmaceutical Investigation
• /
• 제29권1호
• /
• pp.37-45
• /
• 1999

ABSTRACT-A self-microemulsifying drug delivery system (SMEDDS) was developed to enhance the solubility and dissolution rate of poorly water soluble drug, biphenyl dimethyl dicarboxylate, DDB. The system was optimized by evaluating the solubility of DDB and the microemulsion existence range after the preparation of microemulsions with varying compositions of triacetin and surfactant-cosurfactant mixtures (Labrasol as surfactant (S) and the combination of Transcutol, Cremophor RH 40 and Plurol oleique as cosurfactant (CoS)). SMEDDS in this study markedly improved the solubility of DDB in water up to 10 mg/ml and the size of the o/w microemulsion droplets measured by dynamic light scattering showed a narrow monodisperse size distribution with an average diameter less than 50 nm. The microemulsion existing range is increased proportional to the ratio of S/CoS, however, it decreased remarkably as the oil content was more than 20%. In vitro dissolution study of SMEDDS showed a significantly increased dissolution rate of DDB in water (> 12 fold over DDB powder), and SMEDDS also had significantly greater permeability of DDB in Caco-2 cell compared to powders.

• Journal of Pharmaceutical Investigation
• /
• 제31권3호
• /
• pp.181-184
• /
• 2001

The purpose of this study was to develop transdermal drug delivery system (TDDS) for the combination of physostigmine and procyclidine. The effects of various pressure sensitive adhesives (PSA) on the percutaneous absorption of procyclidine across hairless mouse skin were evaluated to select an appropriate PSA. In addition, the influences of various vehicles on the percutaneous absorption of procyclidine from PSA matrix across hairless mouse skin were evaluated using flow-through diffusion cell system at $37^{\circ}C$. Physostigmine did not have any influence on the permeation rate of procyclidine. The flux of procyclidine was the highest in silicone and PIB and was relatively lower in SIS, Acryl, and SBS adhesive matrices, however, their use was limited by the crystallization of the drug in the matrix. Among acrylic adhesives, the permeability of procyclidine was the highest from poly (ethylene oxide) grafted acrylic adhesive. Some enhancers show different enhancing effect depending on the drug, however, many of the tested enhancers showed enhancing effect for the permeation of both procyclidine and physostigmine to some extent. $Crovol^{\circledR}$ EP 40 showed the highest enhancing effect on the permeation of both compounds. The size of TDDS to provide required permeation rate was estimated to be $35\;cm^2$ based on available information.

• The Journal of Korean Physical Therapy
• /
• 제13권3호
• /
• pp.719-726
• /
• 2001

Transdermal drug delivery offers various advantages over conventional drug delivery systems, such as avoidance gastrointestinal degradation and hepatic first-pass effect. encourages patient compliance. and possible sustained release of drugs. However, transdermal transport of drugs is low permeability of the stratum corneum, the superficial layer of the skin. Many physicochemical and biological factors influencing transdermal transport is described together with the corresponding experimental and clinical results. Phonophoresis is medical treatment with drugs introduced into the skin by ultrasound energy. Enhanced drug penetration is through to result from the biophysical alterations of skin structure by ultrasound waves. The frequency used for phonophoresis is usually from 20 kHz to 15MHz. Phonophoresis can be categorized in to three ranges: low-frequency range(below 1 MHz). therapeutic frequency range(1 to 3MHz), and high-frequency range(above 3 MHz). The depth of penetration of ultrasound into skin is inversely proportional to the frequency. Cavitation may cause mechanical stress. temperature elevation, or enhanced chemical reactivity causing drug transport. One theory is that ultrasound affects the permeation of the stratum corneum lipid structure as the limiting step in permeating through the skin. The range of indications for phonophoresis is wide. Aspecific classification of the range of indications is obtained by classification of pathological conditions. The continuous research is needed for many interesting issucs of phonophoretic transdermal delivory in new future.

• 생명과학회지
• /
• 제31권9호
• /
• pp.849-855
• /
• 2021

최근에는 나노기술이 다양한 분야에 도입되고 활용되면서 신약개발이 가속화되고 있다. 나노입자는 약물의 단일 투여로 장기간 동안 혈중 약물 농도를 유지하고, 병리학적 부위에만 선택적으로 방출되는 장점이 있어 비병리 주위에 대한 부작용을 줄일 수 있다. Poly (D,L-lactic-co-glycolic acid) (PLGA)는 가장 광범위하게 개발된 생분해성 고분자 중 하나이다. PLGA는 다양한 응용분야의 약물전달에 널리 사용된다. 또한 FAD에 의해 약물전달 시스템으로 승인되었으며, 유전자 치료제와 같은 제어방출제형에 널리 적용된다. PLGA 나노입자는 수동 및 능동 표적화 방법을 사용하여 특정 세포 유형에 고효율의 전달 시스템으로 개발되었다. 이러한 PLGA 나노입자를 이용한 약물전달체 개발 후 표적 부위에 선택적으로 약물을 전달하고 질병에 따라 장기간 유효 혈중 농도를 최적화한다. 이 리뷰논문에서 우리는 유전자 치료를 위한 PLGA 나노 물질을 기반으로 하는 성상 세포 선택적 나노입자의 개발을 조사하여 세포 특이적으로 치료결과를 향상시키는 방법에 중점을 두고자 한다.

• Bulletin of the Korean Chemical Society
• /
• 제33권8호
• /
• pp.2635-2641
• /
• 2012

Novel silver/salep-g-poly(acrylic acid) nanocomposite hydrogel were prepared in aqueous solution using poly(acrylic acid) grafted onto salep as a biopolymer based material. FT-IR spectra confirmed that poly(acrylic acid) (PAA) had been grafted onto salep in graft copolymerization reaction. TEM observations showed that silver nanoparticles have been uniformly dispersed in polymeric matrix. Effects of pH, acrylic acid (AA) amount and silver ion concentration on swelling capabilities were investigated. Results indicate that modifying AA and silver ion can improve swelling properties of the resultant nanocomposite hydrogel. pH response of this nanocomposite hydrogel in acidic and neutral pH made it suitable for drug delivery applications.

• Journal of Pharmaceutical Investigation
• /
• 제22권2호
• /
• pp.149-153
• /
• 1992

The applicability of sodium alginate as a carrier of 5-fluorouracil as an oral delivery system was investigated. Hydrophobicity of sodium alginate was controlled by introducing cetyl group to this polymer. The effects of degree of esterification for n-cetyl partial ester on the rate of release of 5-fluorouracil in artificial gastric juice and artificial intestinal juice were examined. The release rete of the drug in the gastric juice was mainly affected by the diffusion of the drug. The release rate of the drug in the intestinal juice could be controlled by the degree of esterification. The alginate matrices may be a valuable addition as the carrier of 5-fluorouracil for an oral delivery system.

• 한국가시화정보학회:학술대회논문집
• /
• 한국가시화정보학회 2005년도 추계학술대회 논문집
• /
• pp.89-92
• /
• 2005

A microcapsule for drug delivery was successfully produced by utilizing the flow-through droplet-based supramolecular self-assembly in a crossed microchannel network. The PS-b-PMMA block copolymer synthesized atom transfer radical polymerization (ATRP) was initially formed as microdroplets and after the evaporation process it turned to spherical capsule by polymer self-assembly of the micro domains. The characteristics were studied using various analysis methods.

• 한국응용약물학회:학술대회논문집
• /
• 한국응용약물학회 1996년도 춘계학술대회
• /
• pp.287-287
• /
• 1996

Long-circulating liposomes have prompted interests in using them as a drug delivery system. This improvements in delivery has been thought to be the results from sustained action of liposomes in plasma without RES uptake. Although methotrexate(MTX) has been one of the most widely used antineoplastc drug, its use was limited by prompt RES uptake. The purpose of this study was to prepare long-circulating liposomes for MTX using highly water-soluble polymer (PEG-PE). In vitro, release of MTX from liposomes in phosphate buffer (pH 7.4), rat liver homogenate, and rat plasma was investigated. The pharmacokinetics and organ distribution of fee drug, conventional and long-circulating liposomes were also compared with one another after intravenous administration to rats.