• 폴리머
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• 제26권4호
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• pp.535-542
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• 2002

투석법을 이ctide-co-glycolide) (PLGA) 나노입자를 제조하고 다양한 용매에 따른 입자 크기, 약물 함유량, 생분해도 등과 같은 물리ㆍ화학적 특성을 조사하였다. Dimethylacetamide (DMAc), dimethylformamide (DMF), dimethylsulfoxide (DMSO)로 제조된 PLGA 나노입자의 크기는 acetone으로 제조한 입자보다 적었다. 또한, 약물 함유량은 DMAc>DMF>DMSO=acetone 순서였다. PLGA 나노입자는 scanning electron microscopy (SEM)과 transmission electron microscopy (TEM)의 측정으로 구형임을 알 수 있었다. 계면활성제를 사용하지 않는 나노입자에 봉입된 norfloxacin (NFx)은 X-ray diffraction 분석을 통하여 입자 표면에 약물을 가지지 않는 좋은 약물 봉입 효율을 가짐을 알 수 있었다. 모델약물로 사용된 NFx의 방출속도는 약물 함유량뿐만 아니라 입사크기에 의해 좌우된다. 또한 PLGA 나노입자의 분해속도는 아세톤보다는 DMF를 사용하였을 때 더 빠르며 이는 PLGA 나노입자의 생분해성도 입자크기에 좌우된다는 것을 알 수 있었다.

• BMB Reports
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• 제57권2호
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• pp.71-78
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• 2024

Melanoma is one of the most aggressive skin tumors, and conventional treatment modalities are not effective in treating advanced melanoma. Although immunotherapy is an effective treatment for melanoma, it has disadvantages, such as a poor response rate and serious systemic immune-related toxic side effects. The main solution to this problem is the use of biological materials such as hydrogels to reduce these side effects and amplify the immune killing effect against tumor cells. Hydrogels have great advantages as local slow-release drug carriers, including the ability to deliver antitumor drugs directly to the tumor site, enhance the local drug concentration in tumor tissue, reduce systemic drug distribution and exhibit good degradability. Despite these advantages, there has been limited research on the application of hydrogels in melanoma treatment. Therefore, this article provides a comprehensive review of the potential application of hydrogels in melanoma immunotherapy. Hydrogels can serve as carriers for sustained drug delivery, enabling the targeted and localized delivery of drugs with minimal systemic side effects. This approach has the potential to improve the efficacy of immunotherapy for melanoma. Thus, the use of hydrogels as drug delivery vehicles for melanoma immunotherapy has great potential and warrants further exploration.

• 대한화학회지
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• 제56권4호
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• pp.473-477
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• 2012

The novel chitosan-based thermosensitive hydrogels were prepared as control-releasing drug carriers. N-carboxyethyl chitosan (ACS) was synthesized by microwave heating for 1 h through Michael addition of CS to acrylic acid in a grafting yield of 52.97%, which was proved to be a faster and more efficient way than ordinary methods. 5-Fu was modified with formaldehyde to synthesize N,N'-Bis(hydroxymethyl)-5-fluorouracil (5-Fu-OH). Then an esterification was performed using ACS and 5-Fu-OH to give 5-Fu-ACS. The new thermosensitive hydrogels were prepared by adding sodium glycerophosphate to the solution of compounds under a certain constant temperature. Simultaneously, the hydrogels' swelling rate, in vitro drug release rate and thermosensitive were studied, and found that the 5-Fu-ACS composite hydrogel had more excellent releasing effect, higher drug loading and better thermosensitive.

• Journal of Pharmaceutical Investigation
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• 제29권1호
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• pp.21-27
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• 1999

Semi-solid poly(ortho esters) (POE) were prepared to provide bioerodible carriers for sustained drug delivery systems of naloxone (NLX) in the treatment of narcotic addiction. As the POE have viscous behavior at room temperature, a significant advantage of this polymer is that it can be injected without any surgical intervention. The POE was synthesized by a transesterification reaction between 1,2,6-hexanetriol and trimethyl orthoacetate, and the structure of the polymer was confirmed by IR. The in vitro release of the drug from POE was studied. The release rate of NLX decreased with increasing intrinsic viscosities of the polymer. In vivo biocompatibility studies were carried out in rats with NLX loaded POE. Histopathological analysis showed that NLX implants are well-tolerated by rats when used subcutaneously. Pharmacokinetic studies of POE-NLX implants of two different viscosities were carried out in rabbits. In all cases, plasma concentrations of NLX were maintained over 1 ng/ml for at least 168 hours, but initial burst effect was observed. Mean residence time(MRT) was found to depend on the viscosity of the polymer.

• Journal of Pharmaceutical Investigation
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• 제29권4호
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• pp.309-313
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• 1999

This study was prepared to develop the sustained release dosage form of phenylpropanolamine hydrochloride (PPA) by complexation with cation exchange resin(CER). The PPA-CER complex was confirmed by differential scanning calorimetry(DSC) thennogram, indicating a relative shift of an endometric peak of PPA to higher temperature. The loading efficiency was increased as the amount of PPA was increased as well as the time of fractional exchange was advanced as the temperatures were increased. Loading efficiency, fractional exchange, reaction rate constant and activation energy were highly dependent on the temperature and drug : resin ratio. The optimal ratio of PPA and resin was estimated to be 10: 10 for the sustained release.

• Bulletin of the Korean Chemical Society
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• 제32권5호
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• pp.1587-1592
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• 2011

The aim of the present study was to improve the solubility and bioavailability of a poorly water-soluble drug in human body, using a solid dispersion technique (hot melt extrusion). The solid dispersion was prepared by cooling the hot melt of the drug in the carrier (Vitamin E TPGS and PVP). The dissolution rate of formulation 1 from a novel formulation prepared by solid dispersion technique was equal to release of formulation 6 (40% of eprosartan mesylate is in contrast to teveten$^{(R)}$) within 60 min (Table 1). The oral bioavailability of new eprosartan mesylate tablet having vitamin E TPGS and PVP K29 was tested on rats and dogs. Of the absorption enhancer and polymer tested, vitamin E TPGS and PVP K29, resulted in the greatest increases of AUC in animals (about 2.5-fold increase in rat and dog). When eprosartan mesylate was mixed with the absorption enhancer and polymer in a ratio of 2.94:2:1, vitamin E TPGS and PVP K29 improved eprosartan mesylate bioavailability significantly compared with the conventional immediate release (IR) tablet Teveten$^{(R)}$ (formulation 7). These results show that solid dispersion using vitamin E TPGS and PVP K29 is a promising approach for developing eprosartan mesylate drug products.

• Journal of Pharmaceutical Investigation
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• 제40권1호
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• pp.9-14
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• 2010

Lacidipine used for the treatment of hypertension has low water solubility and is classified as BCS Class II category. Gelucire-based solid dispersions (SD) containing lacidipine were prepared by solvent evaporation method to enhance drug dissolution. The powdered forms of SD showed irregularly spherical shape. Thermal behaviors of SD from differential scanning calorimetry indicated that distinct endothermic peak of lacidipine ($184^{\circ}C$) was shifted to lower region ($150.1^{\circ}C$). Drug was present in a crystalline form. NMR spectra also showed some molecular interaction between drug and Gelucire. There was no significant difference in DSC and NMR behaviors between Gelucire 44/14 and Gelucire 50/13. The initial dissolution rate of SD-loaded tablet linearly increased both in water and in water containing 1% tween 20, and much higher than the commercial tablet, $Vaxar^{(R)}$. When the amount of SD was increased, the release rate was greater. The Gelucire 50/13 showed higher dissolution than the Gelucire 44/14. The produced solid dispersion with various kinds of excipients and making tablets, it was found that solid dispersions can increase the solubility in artificial gastric juice and finally increases dissolution rate.

• 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%.

• 폴리머
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• 제34권3호
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• pp.269-273
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• 2010

본 연구는 염산 알푸조신의 서방화를 위한 과립제의 최적 구성을 찾기 위해 수행되었으며, 이에 따라 고분자의 점도에 따른 염산 알푸조신 과립정제를 제조하였다. 사용된 고분자는 경구를 통한 약물전달 시스템 설계에 가장 널리 사용되는 하이드록시프로필메틸셀룰로오스(HPMC)이며, HPMC의 팽윤성은 가장 중요한 특성으로 약물의 방출에 큰 영향을 미친다. 염산 알푸조신 과립정제의 구조변화를 확인하기 위하여 적외선분광법(FTIR)을 분석하였으며, 결정학적 특성을 알아보기 위해 X선 회절분석법(XRD)을 이용하여 분석하였다. 과립정제를 제조하여 인공장액에서의 방출거동을 알아보았으며, 본 연구를 통해 첨가제로 사용된 HPMC의 점도에 따라 모델약물인 염산 알푸조신의 방출거동을 조절할 수 있었다.

• Bulletin of the Korean Chemical Society
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• 제23권11호
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• pp.1579-1584
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• 2002

Since surfactant or emulsifiers remained on the nanoparticle surface significantly affect the physicochemical properties, the biodegradation rate, the biodistribution, and the biocompatibility of nanoparticles, surfactant-free nanoparticles should be good candidate. surfactant-free PLGA nanoparticles were successfully prepared by both the dialysis method and the solvent diffusion method. The PLGA nanoparticles prepared using the solvent diffusion method has a smaller particle size than the dialysis method. The solvent diffusion method was better for a higher loading efficiency than the dialysis method but the nanoparticle yield was lower. Testosterone (TST) release from the PLGA nanoparticles was dependent on the particle size rather than the drug contents. Testosterone release from the PLGA nanoparticles prepared by the solvent diffusion method using acetone was faster than those prepared by the dialysis method. TST release from the PLGA nanoparticles prepared by the solvent diffusion method using acetone and the dialysis method using dimethylformamide (DMF) was completed for 4 days while the PLGA nanoparticles prepared by the dialysis method using acetone showed approximately 80% TST release after 4 days. Since the PLGA nanoparticle degradation ratio was below 20% within 5 days at all samples while TST release completed within 4 days, TST release was dependent on the diffusion mechanism rather than degradation.