• Title/Summary/Keyword: drug-release

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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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Mechanisms involved in adenosine pharmacological preconditioning-induced cardioprotection

  • Singh, Lovedeep;Kulshrestha, Ritu;Singh, Nirmal;Jaggi, Amteshwar Singh
    • The Korean Journal of Physiology and Pharmacology
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    • v.22 no.3
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    • pp.225-234
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    • 2018
  • Adenosine is a naturally occurring breakdown product of adenosine triphosphate and plays an important role in different physiological and pathological conditions. Adenosine also serves as an important trigger in ischemic and remote preconditioning and its release may impart cardioprotection. Exogenous administration of adenosine in the form of adenosine preconditioning may also protect heart from ischemia-reperfusion injury. Endogenous release of adenosine during ischemic/remote preconditioning or exogenous adenosine during pharmacological preconditioning activates adenosine receptors to activate plethora of mechanisms, which either independently or in association with one another may confer cardioprotection during ischemia-reperfusion injury. These mechanisms include activation of $K_{ATP}$ channels, an increase in the levels of antioxidant enzymes, functional interaction with opioid receptors; increase in nitric oxide production; decrease in inflammation; activation of transient receptor potential vanilloid (TRPV) channels; activation of kinases such as protein kinase B (Akt), protein kinase C, tyrosine kinase, mitogen activated protein (MAP) kinases such as ERK 1/2, p38 MAP kinases and MAP kinase kinase (MEK 1) MMP. The present review discusses the role and mechanisms involved in adenosine preconditioning-induced cardioprotection.

Norfloxacin-Incorporated Polymeric Micelle Composed of Poly(ε-caprolactone)/Poly(ethylene glycol) Diblock Copolymer (Norfloxacin이 담지된 Poly(ε-caprolactone)/Poly(ethylene glycol) 이중블록공중합체 미셀의 제조)

  • Jeong, Young-Il;Jang, Mi-Kyeong;Nah, Jae-Woon
    • Polymer(Korea)
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    • v.33 no.2
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    • pp.137-143
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    • 2009
  • We prepared norfloxacin (NFX)-incorporated polymeric micelle using poly ($\varepsilon$-caprolactone)/poly(ethylene glycol) (PCL/PEG, CE) diblock copolymers. Particle size was from 60 to 200 nm according to the PCL block length. Their critical association concentration (CAC) was decreased according to the increase of PCL block length. $^1H$-NMR study showed core-shell type micelle structures of CE diblock copolymers in the aqueous environment. Drug release from polymeric micelle was continued over 2 days. Duration of drug release was varied according to the PCL block length and drug contents. At antimicrobial activity test, polymeric micelle showed almost similar cytotoxicity compared to NFX itself.

Photoresponsive Nanocontainers with Ordered Porous Channels

  • Cho, Wansu;Kwon, Youngje;Park, Chiyoung
    • Elastomers and Composites
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    • v.54 no.2
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    • pp.149-155
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    • 2019
  • Controlled mass transport in response to stimuli is essential for drug carriers. The complexity of the signaling system under physiological conditions has led researchers to develop precise nanocontainers that respond to stimuli in the physiological environment. Owing to several reasons, soft nanocontainers such as liposomes and micelles have been investigated for use as drug delivery systems. However, such carriers often suffer from the undesired leakage of drug molecules. In contrast, inorganic nanocontainers are robust, and their surfaces can be easily functionalized. For example, mesoporous silica nanoparticles equipped with gatekeeper molecules are increasingly being used for the controlled release of drug molecules in response to the desired stimuli. Since the development of the first hybrid nanocontainer comprising molecular machines, multiple versions of such gatekeeper systems featuring significantly improved stability and precise response to stimuli have been reported. In this study, various methods for incorporating photoresponsive nanocontainers with porous channels are developed.

Preparation and Characterization of Alginate-Chitosan Microsphere for Controlled Delivery of Silver Sulfadiazine (설파디아진은의 방출제어를 위한 알지네이트-키토산 미립구의 제조 및 특성)

  • Cho, Ae-Ri
    • Journal of Pharmaceutical Investigation
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    • v.31 no.2
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    • pp.101-106
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    • 2001
  • Alginate-chitosan (anion-cationic polymeric complex) was prepared to control the release rate of silver sulfadiazine (AgSD). Na-alginate (2%) solution containing AgSD was gelled in $CaCl_2$ solution. The gel beads formed were immediately encapsulated with chitosan (CS). The gel matrix and membrane were then reinforced with chondroitin-6-sulfate (Ch6S). Release rate of AgSD from the gel matrix was investigated by placing alginate beads in the sac of cellulose membrane simmered in HEPES-buffer solution. The concentration of AgSD released was analyzed by UV at 264 nm. Incorporation capacity of AgSD in Ca-alginate gel was more than 90%. Alginate-Ch6S-CS could control the release rate of AgSD. The amount of AgSD release was dependent on the AgSD loading dose. Incorporation of tripolyphosphate (polyanionic crosslinker) onto the alginate-Ch6S-CS bead increased the release rate of AgSD. Collagen-coating had no influence on the AgSD release rate. Alginate-Ch6S-CS beads with a sufficiently high AgSD encapsulation were capable of controlling the release of the drug over 10 days. In summary, alginate-Ch6S-CS beads could be used as a sustained delivery for AgSD and provide local targeting with low silver toxicity and patient discomfort.

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Testosterone-encapsulated Surfactant-free Nanoparicles of Poly(DL-lactide-co-glycolide): Preparation and Release Behavior

  • Jeong, Young-Il;Shim, Yong-Ho;Song, Ki-Chan;Park, Youeng-Guen;Ryu, Hwa-Won;Nah, Jae-Woon
    • Bulletin of the Korean Chemical Society
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    • v.23 no.11
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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.

Controlled Release of Gentamicin Sulfate from Poly(3-hydroxybu-tyrate-co-3-hydroxyvalerate) Wafers for the Treatment of Osteomyelitis

  • Gilson Khang;Park, Hak-Soo;John M. Rhee;Yoon, Sung-Chul;Cho, Jin-Cheol;Lee, Hai-Bang
    • Macromolecular Research
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    • v.8 no.6
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    • pp.253-260
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    • 2000
  • Biodegradable wafers were prepared with poly (hydroxybutyrate-co-hydroxyvalerate) (PHBV;5, 10, and 15 mole% for 3-hydroxyvalerate) by simple heat pressing method for the sustained release of antibiotic agent, gentamicin sulfate (GS) to investigate the possibility of the treatment for osteomyelitis. The effects of hydroxyvalerate (HV) content, thickness of wafers, various types of additives such as sodium dodecyl sulfate (SDS), microcrystalline cellulose, polyvinylpyrrolidone, and hydroxypropylcellulose (HPC), and different initial drug loading ratio on the release profile have been investigated. In vitro release studies showed that different release patterns and rates could be achieved by simply modifying factors in the preparation conditions. PHBV wafers with 3 mm thickness, 10% of GS initial loading, 15% of HV content and addition of 5% of SDS and HPC were free from initial burst and a near-zero-order sustained release was observed for over 30 days. It might be suggested that the mechanisms of G5 release may be more predominant simple dissolution and diffusion of GS than erosion of PHBV in our system.

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