• Title/Summary/Keyword: Sustained drug delivery

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Drug Delivery Effect Using Biopolymer Chitosan Nanoparticles (생명고분자 키토산의 나노입자를 이용한 약물전달 효과)

  • Lee, Do Hun;Lee, Sang-wha;Yoo, In Sang;Park, Kwon-pil;Kang, Ik Joong
    • Applied Chemistry for Engineering
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    • v.16 no.6
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    • pp.790-793
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    • 2005
  • Recently, the interest in the extension of human life and personal health has been increased. Accordingly, many researchers in a pharmacy and a medical world have been making efforts to improve the sustained drug release property and the stability of drug release property in a body. Many biological researches have demonstrated that chitosan derivatives are effective, safe absorption enhancers that can improve the delivery efficiency of drug and vaccine, and they are suitable for controlled drug release because they have good stability, bio-compatibility, and biodegradability. In this study the experiment was performed in vivo by utilizing chitosan nanoparticles as a biopolymer to control drug delivery rate at an optimal temperature, pH, and concentration. It was observed that nanoparticles containing insulin could effectively control the blood glucose at a low level.

Research progress on hydrogel-based drug therapy in melanoma immunotherapy

  • Wei He;Yanqin Zhang;Yi Qu;Mengmeng Liu;Guodong Li;Luxiang Pan;Xinyao Xu;Gege Shi;Qiang Hao;Fen Liu;Yuan Gao
    • BMB Reports
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    • v.57 no.2
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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.

Injectable Sustained Release Gel as a Local Drug Delivery for Periodontal Diseases (치주질환치료를 위한 국소적용 서방출성 리오겔)

  • Kim, Ki-jun;Shin, Young-hee
    • YAKHAK HOEJI
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    • v.60 no.1
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    • pp.46-50
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    • 2016
  • The purpose of this study was the development of sustained-release lyogel of chlorhexidine in the treatment of periodontal diseases. A sustained-release chlorhexidine lyogel (CHX-G) was formulated, based on Eudragit$^{(R)}$ (1~3%), polyvinyl pyrrolidone (PVP) (0~10%), triacetin (20~40%), hydroxy ethyl cellulose (HEC) (1%) and glycerin. In vitro studies were performed to determine the release rate of chlorhexidine from CHX-Gs using dialysis tube. Our results suggest that the release rate of chlorhexidine from lyogel could be controlled by changing the lyogel compositions.

Pharmacokinetic Evaluation of Ketorolac Tromethamine Sustained-Release Pellets after Oral Administration in Rabbits (케토롤락트로메타민 서방성 펠렛의 약물속도론적 평가)

  • Kwak, Son-Hyok;Hwang, Sung-Joo;Jiang, Ge;Nam, Kyung-Wan;Moon, Young-Girl;Lee, Hai-Bang;Cho, Sun-Hang;Yuk, Soon-Hong;Lee, Han-Koo;Jeong, Sang-Young;Lee, Young-Won
    • Journal of Pharmaceutical Investigation
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    • v.30 no.4
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    • pp.241-246
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    • 2000
  • To develop a sustained-release preparation containing ketorolac tromethamine, two sustained-release pellet formulations were evaluated with a pharmacokinetic study as compared with a conventional commercial tablets (10 mg $Tarasyn^{TM}$, Roche Korea Ltd.). Two sustained-release formulations were as follows; formulation A was composed of an inner layer containing 75% of drug coated with $Eudragit^{TM}$ RS 100 membrane and an outer layer containing 25% of drug mixed with $Eudragit^{TM}$ NE30D, and formulation B was composed of only an inner layer containing 100% of drug coated with $Eudragit^{TM}$ RS 100 membrane. The dissolution test was performed for two formulations. In case of conventional tablets, 2.5 mg of drug per a dose was administered orally into male Albino rabbit (2.0-2.3 kg of body weight) 3 times at intervals of 4 hours. In case of two sustained formulations, 7.5 mg of drug was administered once orally. Blood samples were withdrawn periodically after the administration, and the blood concentration was determined by HPLC. The conventional tablets showed very high peak-trough fluctuation between administered doses, but two sustained formulations showed less fluctuation. Formulation A with the loading dose showed the time to reach minimum effective concentration (MEC) i.e. the onset time was less than 20 min, while Formulation B had more than 1 hr of the onset time. Formulation A had the more constant plasma level than formulation B. However, formulation B had a time lag, so the plasma level was less than MEC for an initial period of 1 hr. In formulation A, the plasma level was maintained within the therapeutic window $(0.3-5\;{\mu}g/ml)$ for a long period. Formulation A was thought to be an ideal sustained-release formulation for ketorolac tromethamine oral delivery system.

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Formulation and Preparation of Sustained Release Pellet for Alfuzosin HCI Using Fluid-bed coater (유동층 코팅기를 이용한 염산알푸조신의 서방형 과립 설계 및 제조)

  • Na, Jin-Sang;Yoon, Yang-No;Seo, Hui;Jeong, Sang-Young;Park, Eun-Seok;Hwan, Sung-Joo;Shin, Byung-Cheol;Kim, Sung-Hoon;Cho, Sun-Hang
    • Journal of Pharmaceutical Investigation
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    • v.38 no.6
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    • pp.387-392
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    • 2008
  • Alfuzosin, an Alphal-adrenoceptor antagonist is used for the treatment of patients with voiding and in a lesser extent storage lower urinary tract symptoms (LUTS) associated to benign prostatic hyperplasia (BPH). The objective of this study was to formulate sustained release alfuzosin HCl granules and assess their formulation variables. The $Eudragit^{(R)}$ as a polymer, sustained release membrane, and dibutyl sebacate (DBS) as a plasticizer were used. Multi-coated alfuzosin HCl delivery systems composed of sugar sphere, various excipients, $Eudragit^{(R)}$ and HPMC (hydroxy propyl methyl cellulose), Cellulose Acetate were prepared by fluid-bed coater. Membrane layer were used $Eudragit^{(R)}$ RS PO and NE 30D. And the alfuzosin HCl coated beads were coated immediate release drug layer for initial burst. Its dissolution test was carried out compared to conventional products ($XATRAL^{(R)}$ XL). The release rate of drug from coated beads was higher than that from $XATRAL^{(R)}$ XL in pH 6.8.

Fabrication of Luminescent Hydroxyapatite Microspheres for Drug Loading and Release

  • Park, So Yeon;Kwon, Seung Lee;Baek, Mi Yeon;Yoo, Jin Sun;Kim, Min-Cheol;Jung, Hyun Suk
    • Proceedings of the Korean Vacuum Society Conference
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    • 2016.02a
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    • pp.360.1-360.1
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    • 2016
  • Hydroxyapatite (Ca10(PO4)6(OH)2, HAP) particles have attracted a great deal of attention in biomedical fields due to their good biocompatibility, bioactivity and fairly broad applications as drug delivery, dental implant, bone cement, and etc. Thus, many researchers have made an effort to add new functionalities such as luminescence, drug delivery, and bone regeneration properties up to HAP powders by controlling their nanostructure as well as composition. In this research, the mesoporous strontium substituted HAP (Sr-HAP) microspheres were synthesized using a hydrothermal method. In this synthesis, aspartic acid monomers were utilized to form microsphere by controlling surface energy of HAP particles and Sr ions were substituted into Ca ion sites, which induced luminescence property in HAP powders. Moreover, the change in the amount of Sr substitution was found to influence the particle size, morphology, and concurrently surface area, which led to changing drug loading as well as drug release property. The amount of Sr influences the morphology, luminescent properties, particle size, surface area cell viability and drug loading property, which are investigated by SEM, TEM, XRD, FTIR, BET, XPS and in vitro test such as MTT assay and drug release test. In particular, the multifunctional Sr-HAP with molar ratios of 0.25 (Sr/(Ca+Sr)) possessed the strongest luminescent property as well as the superior drug loading and sustained release properties that were correspondent with large surface area and pore size. Our study indicates that the fabricated multifunctional Sr-HAP microspheres are quite useful for bone regeneration and drug delivery.

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Release of Calcein from Temperature-Sensitive Liposomes in a Poly(N-isopropylacrylamide) Hydrogel

  • Han Hee Dong;Kim Tae Woo;Shin Byung Cheol;Choi Ho Suk
    • Macromolecular Research
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    • v.13 no.1
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    • pp.54-61
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    • 2005
  • We prepared temperature-sensitive liposomes (TS-liposomes) modified with a thermo sensitive polymer, such as poly(N-isopropylacrylamide) (PNIPAAm), to increase the degree of drug release from liposomes at the hyperthermic temperature. A PNIPAAm hydrogel containing TS-Iiposomes was also prepared to obtain a hydrogel complex at body temperature. In addition, a depot system for local drug delivery using the polymer hydrogel was developed to enhance therapeutic efficacy and prevent severe side effects in the whole body. The PNIPAAm-mod­ified TS-liposome was fixed into the PNIPAAm hydrogel having a high temperature-sensitivity. The release behavior of calcein, a model drug, from TS-liposomes in the PNIPAAm hydrogel was then initiated by external hyperthermia; the results indicated that sustained release as a function of temperature and time was caused by the thermosensitivity of the liposome surface and diffusion of the drug into the PNIPAAm hydrogel. Our results indicated that TS-liposomes in a PNIPAAm hydrogel represented a plausible system for local drug delivery.

Enhanced Transdermal Delivery of Pranoprofen from the Bioadhesive Gels

  • Shin, Sang-Chul;Cho, Cheong-Weon
    • Archives of Pharmacal Research
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    • v.29 no.10
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    • pp.928-933
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    • 2006
  • Percutaneous delivery of NSAIDs has advantages of avoiding hepatic first pass effect and delivering the drug for extended period of time at a sustained, concentrated level at the inflammation site that mainly acts at the joint and the related regions. To develop the new topical formulations of pranoprofen that have suitable bioadhesion, the gel was formulated using hydroxypropyl methylcellulose (HPMC) and poloxamer 407. The effects of temperature on drug release was performed at $32^{\circ}C$, $37^{\circ}C$ and $42^{\circ}C$ according to drug concentration of 0.04%, 0.08%, 0.12%, 0.16%, and 0.2% (w/w) using synthetic cellulose membrane at $37{\pm}0.5^{\circ}C$. The increase of temperature showed the increased drug release. The activation energy (Ea), which were calculated from the slope of lop P versus 1000/T plots was 11.22 kcal/ mol for 0.04%, 10.79 kcal/mol for 0.08%, 10.41 kcal/mol for 0.12% and 8.88 kcal/mol for 0.16% loading dose from the pranoprofen gel. To increase the drug permeation, some kinds of penetration enhancers such as the ethylene glycols, the propylene glycols, the glycerides, the non-ionic surfactants and the fatty acids were incorporated in the gel formulation. Among the various enhancers used, propylene glycol mono laurate showed the highest enhancing effects with the enhancement factor of 2.74. The results of this study suggest that development of topical gel formulation of pranoprofen containing an enhancer is feasible.

Preparation of Poloxamer-based Hydrogels Using Electron Beam and Their Evaluation for Buccal Mucoadhesive Drug Delivery (전자빔을 이용한 폴록사머 하이드로젤의 제조 및 구강 점막부착성 약물전달을 위한 특성 분석)

  • Baek, Eun-Jung;Shin, Baek-Ki;Nho, Young-Chang;Lim, Youn-Mook;Park, Jong-Seok;Park, Jeong-Sook;Huh, Kang-Moo
    • Polymer(Korea)
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    • v.36 no.2
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    • pp.182-189
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    • 2012
  • In this study, poloxamer hydrogels were prepared by electron beam irradiation and evaluated for potential application as a buccal mucoadhesive drug delivery system. Poloxamer, one of typical thermoresponsive polymers, was modified to have vinyl end groups for crosslinking reaction, and its hydrogels were fabricated by irradiation crosslinking reaction. Carbopol as a mucoadhesive polymeric additive was introduced to improve the mucoadhesive property of the hydrogels and its effect on the mucoadhesion and drug release properties was investigated. The results showed that the end group modification of poloxamer and the addition of carbopol improved mucoadhesive force and mechanical properties and led to a sustained drug release behavior.

Development of Drug-Loaded PLGA Microparticles with Different Release Patterns for Prolonged Drug Delivery

  • Choi, Yeon-Soon;Joo, Jae-Ryang;Hong, Areum;Park, Jong-Sang
    • Bulletin of the Korean Chemical Society
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    • v.32 no.3
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    • pp.867-872
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    • 2011
  • For the prolonged delivery and sustained release rates of low molecular weight drugs, poly(lactic-co-glycolic acid) (PLGA) microparticles containing the drug SKL-2020 have been investigated. On increasing polyvinyl alcohol (PVA) concentration (from 0.2% to 5%), the size of microparticles decreased (from $48.02{\mu}m$ to $10.63{\mu}m$) and more uniform size distribution was noticeable due to the powerful emulsifying ability of PVA. A higher drug loading (from 5% to 20%) caused a larger concentration gradient between 2 phases at the polymer precipitation step; this resulted in decreased encapsulation efficiency (from 34.19% to 25.67%) and a greater initial burst (from 61.71% to 70.05%). SKL-2020-loaded PLGA microparticles prepared with different fabrication conditions exhibited unique release patterns of SKL-2020. High PVA concentration and high drug loading led to an initial burst effect by rapid drug diffusion through the polymer matrix. Since PLGA microparticles enabled the slow release of SKL-2020 over 1 week in vitro and in vivo, more convenient and comfortable treatment could be facilitated with less frequent administration. It is feasible to design a release profile by mixing microparticles that were prepared with different fabrication conditions. By this method, the initial burst could be repressed properly and drug release rate could decrease.