• Title/Summary/Keyword: drug carriers

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Design and decoration of heparin on porous nanosilica via reversible disulfide linkages for controlled drug release

  • Nguyen, Dai Hai
    • Journal of IKEEE
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    • v.21 no.3
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    • pp.320-330
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    • 2017
  • Porous nanosilica (PNS) has been identified as a potential candidate for controlled drug delivery. However, unmodified PNS-based carriers exhibited an initial release of loaded bioactive agents, which may limit their potential clinical applications. In this study, the surface of PNS was functionalized with adamantylamine (ADA) via disulfide bonds (-S-S-), PNS-S-S-ADA, which was then modified with cyclodextrin (CD)-heparin (Hep) (CD-Hep), PNS-S-S-CDH, for redox triggered rhodamine B (RhB) delivery. The obtained samples were then characterized by proton nuclear magnetic resonance ($^{1}H\;NMR$), Fourier transform infrared (FTIR), and transmission electron microscope (TEM). These results showed that PNS-S-S-CDH was successfully formed with spherical shape and average diameter of $45.64{\pm}2.33nm$. In addition, RhB was relatively encapsulated in the PNS-S-S-CDH (RhB@PNS-S-S-CDH) and slowly released up to 3 days. The release of RhB, in particular, was triggered due to the cleavage of -S-S- in the presence of dithiothreitol (DTT). It might be anticipated that the modified PNS can be used as redox-responsive drug delivery system in cancer therapy.

Effect of Bovine Serum Albumin on the Stability of Methotrexate-encapsulated Liposomes

  • Kim, Chong-Kook;Kim, Han-Sung;Lee, Beum-Jin;Han, Jeong-Hee
    • Archives of Pharmacal Research
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    • v.14 no.4
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    • pp.336-341
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    • 1991
  • The effect of bovine serum albumin (BSA) on the encapsulation efficiency and stability of liposomes containing methotrexate (MTX) having different surface charges and cholesterol contents were investigated. The encapsulation efficiency of MTX was lower and the release of MTX was faster by the addition of BSA. The leaking of MTX from lipid bilayer depends upon the BSA concentrations. These results may be derived from the interaction of BSA with lipid bilayers. The dynamic structural changes of BSA were monitored indirectly using circular dichroism spectra. Observed dynamic structural changes of BSA with liposomes are presumed to reflect the interaction of BSA with liposomes. Negatively charged liposomes have more strong interaction with BSA than neutral and positively charged liposomes. BSA attacks lipid bilayers whether it is at the inner or at the outer phase of lipid bilayer and induces leakage of entrapped MTX. Especially, negatively charged liposomes are more sensitive than others. The inclusion of cholesterol in the lipid layers inhibits the interaction of BSA with liposomes and shows protective effect against BSA-induced leakage of MTX. To endure the attacking of BSA liposomes as drug carriers should be made using cholesterol.

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Efficacy of nano-drugs in muscle injury rehabilitation and fatigue relief

  • Zicheng Wang;Yanqing Liu;Haibo Wang;Dai Liu;Niuniu Yang;Mengying Lv
    • Advances in nano research
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    • v.14 no.1
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    • pp.17-25
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    • 2023
  • Gold nanoparticles have recognized a promising drug carriers in many diseases. These nanoparticles could carry anti-inflammatory drugs in the case of muscle injury and for fatigue relief. On the other hand, specific surface of this kind of nanoparticles could be critical in amount of drug they could carry. Therefore, in this study, we explore different methodology and influencing parameters on the specific surface of gold nanoparticles. After specifying the main parameters, different machine learning and artificial neural network are adopted to model the effects of different parameters. Furthermore, response surface methodology is utilized to obtain a quadrilateral relationship between different parameters and specific surface. The results indicate that concentration of the gold salt solution is the most important parameter in increasing the size of gold nanoparticle and, as a consequence, increasing specific surface. Moreover, the ability of gold nanoparticles in prolonging retention of the drugs is discussed in detail.

Development of Radiopharmaceutical DW-166HC for Anticancer drug

  • Man, Ryu-Jei
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1999.04a
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    • pp.53-61
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    • 1999
  • Radiation therapy has been used for the cancer treatment and radiation synovectomy$\^$1-3)/. There are two kinds of radiation therapy; the external radiation therapy and the internal radiation therapy. Hitherto, the external radiation therapy has been widely used, but for the lack of its selectivity it requires strong radiation dose and causes the irritation and damage of the normal tissue or organ. Therefore many researchers give their interests to the internal radiation therapy in which the radioactive materials are injected directly into the target organ or tissue. Many ${\beta}$-emitting radionuclides have been studied for the application of the internal radiation theraily. Among them, Holmium-166 has the many beneficial physical characteristics for the internal radiation therapy such as appropriate half life (26.8hr), high ${\beta}$ energy (max. 1.85 MeV(51%), 1.77 MeV (48%), mean 0.67MeV), and low ${\gamma}$ energy (0.081MeV) easily detected by ${\gamma}$-camera. In the internal radiation therapy, the administered radioactive materials should be retained in the target long enough to increase the therapeutic effects and avoid the damage in the normal tissue or organ. For this purpose, radionuclides are used as complex form with carriers. Carriers should have a high affinity with radionuclides in vivo and in vitro, so the complex can be evenly distributed in the lesion but can not be leaked out from the lesion.

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Perspectives on Bovine Milk-Derived Extracellular Vesicles for Therapeutic Applications in Gut Health

  • Mun, Daye;Oh, Sangnam;Kim, Younghoon
    • Food Science of Animal Resources
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    • v.42 no.2
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    • pp.197-209
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    • 2022
  • Extracellular vesicles (EVs) are nanosized vesicles secreted from cells into the extracellular environment and are composed of a lipid bilayer that contains cargos with biological activity, such as lipids, proteins, mRNAs, and noncoding microRNAs (miRNAs). Due to their biological activity and their role in cell-to-cell communication, interest in EVs is rapidly increasing. Bovine milk is a food consumed by people of all ages around the world that contains not only a significant amount of nutrients but also EVs. Milk-derived EVs also exhibit biological activity similar to other source-derived EVs, and studies on bovine milk EVs have been conducted in various research fields regarding sufficient milk production. In particular, not only are the effects of milk EVs themselves being studied, but the possibility of using them as drug carriers or biomarkers is also being studied. In this review, the characteristics and cargo of milk EVs are summarized, as well as their uptake and stability, efficacy and biological effects as carriers, and future research directions are presented.

Preparation and Characterization of Casein Nanoparticles with Various Metal Ions as Drug Delivery Systems (다양한 금속 이온을 이용한 카세인 단백질 나노입자 형성 및 약물 전달체 특성 연구)

  • Minju Kim;Seulgi Lee;Joon Sig Choi
    • Applied Chemistry for Engineering
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    • v.34 no.2
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    • pp.121-125
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    • 2023
  • Casein is a milk protein and one of the most important nutrients in milk. The composition is over 80% in cow's milk and about 20~45% in human's milk. Casein is highly biocompatible and biodegradable, so it has been studied for various biomedical materials applications as well as drug delivery systems. It is widely known that casein can be prepared as nanoparticles in the presence of the Ca2+ metal ion. Because casein is amphiphilic, hydrophobic drugs could be loaded inside to form a protein-based drug delivery system. In this study, we studied the optimum conditions for casein nanoparticle formation using natural metal ions present in the body, such as calcium, magnesium, zinc, and iron. It was confirmed that nanoparticles have a uniform size of around 150 nm and negative zeta potential values. In addition, it was demonstrated that casein nanoparticles have a cell viability of more than 80% and efficient intracellular uptake properties using confocal microscopy. From the results, it was also shown that the casein nanoparticles prepared using various metal ions have the potential to be biocompatible drug delivery carriers.

Preparation and In Vitro Release of Ramose Chitosan-Based-5-Fluorouracil Microspheres

  • Li, He-Ping;Li, Hui;Wang, Zhou-Dong;Zhang, Juan-Juan;Deng, Man-Feng;Chen, San-Long
    • Journal of the Korean Chemical Society
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    • v.57 no.1
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    • pp.88-93
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    • 2013
  • In order to construct a controlled release system of drugs and to reduce toxic side effects of 5-fluorouracil, the novel ramose chitosan-based-5-fluorouracil microspheres (CS-FU-MS) were prepared. Firstly, using chitosan (CS) as carriers and 5-fluorouracil (5-FU) as a model drug, ramose chitosan-based-5-fluorouracil (CS-FU) was efciently synthesized by chemical crosslinking method through microwave irradiation, drug loading was 10.6%; Secondly, CS-FU-MS were prepared by CS-FU self-assembled under the dialysis conditions and the free 5-FU was encapsulated further at the same time. The size dispersivity of particles is uniform, and the average diameter of the CS-FU-MS was $4{\mu}m$. The drug encapsulation efficiency was 76.1%, and the drug loading was increased to 26.22%. CS-FU-MS maintain the zero-order release time in PBS (pH = 7.4) and HCl/KCl (pH = 1.2) dialysis medium was 40h and 34h respectively, and the cumulative release were 58.89% and 79.33% in 182 h. The results showed that CS-FU-MS have excellent sustained release properties.

Preparation and Evaluation of Ketoprofen-incorporated Solid Lipid Nanoparticles (SLN) (케토프로펜을 함유하는 고형 지질 나노파티클의 제조 및 평가)

  • Baek, Myoung-Ki;Lee, Sang-Young;Jee, Ung-Kil
    • Journal of Pharmaceutical Investigation
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    • v.26 no.4
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    • pp.245-256
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    • 1996
  • Solid lipid nanoparticles (SLN) have been developed as a new drug delivery system. Although many particulate drug carriers, such as microsphere, liposome, niosome, emulsion, etc. have been introduced, they have some disadvantage; low efficiency of incorporation and stability, lack of reproducibility, and so on. Meanwhile, SLN as a new drug delivery system is known to entrap rugs with a high efficiency and a good reproducibility. Moreover, small size SLN can circulate in blood for a prolonged time. Although many preparation methods were introduced, microfluidization method is recommended to be the most useful. This study was attempted to prepare and evaluate ketoprofen-incorporated SLNs (keto-SLN), which were prepared by two methods, ultrasonication and microfluidization. Keto-SLN was evaluated by measurement of particle size and zeta potential, efficacy of entrapment, sedimentation volume, in virto release pattern. The mean particle size was about $0.1\;{\mu}m$, and the size was dependent on the type and the amount of emulsifier. Zeta potential was negative, $-9{\sim}-13mV$ and entrapment efficacy was very high and stability was good for at least 60 days in the respect of particle size and sedimentation volume ratio. Analgesic effect was also determined as well as pharmacokinetic parameters. The former was comparable to that of that of ketoprofen loaded suspension (keto-sus) and the latter revealed that consistent with the delayed release of keto-SLN. $T_{max}$ was longer than keto-sus. Therefore, keto-SLN was favourable dosage forms in the field of drug delivery system such as anti-cancer, analgesics and anti-inflammatory agents.

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Preparation and Characterization of Rosiglitazone-loaded PLGA Nanoparticles (Rosiglitazone약물을 함유한 PLGA 나노입자 제조 및 분석)

  • Shin, Ko-Eun;Huh, Kang-Moo;Lee, Yong-Kyu
    • KSBB Journal
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    • v.23 no.5
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    • pp.408-412
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    • 2008
  • The rosiglitazone loaded poly (lactide-co-glycolide) (PLGA) nanoparticles (NPs) were prepared by the emulsion-evaporation method and optimized for particle size and entrapment efficiency. The optimized particles were 140-180 nm in size with narrow size distribution and 80% entrapment efficiency at 1% w/w initial drug loading when prepared with 1-3% w/v of PVA as a surfactant. These particulate carriers exhibited controlled in vitro release of rosiglitazone for 36 hrs at a nearly constant rate after 4 hrs release. In conclusion, these results indicate that PLGA NPs have greater potential for oral delivery of rosiglitazone.

Release, Biocompatibility and Pharmacokinetics of Semi-solid Naloxone Implants of Poly(ortho ester) (폴리오르소에스텔을 이용한 나록손의 반고형 이식제제의 방출, 생체적합성 및 약물동력학적 연구)

  • Lim, Sang-Hee;Park, Joo-Ae;Kim, Kil-Soo
    • Journal of Pharmaceutical Investigation
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    • v.29 no.1
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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.

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