• Title/Summary/Keyword: BCNU

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Effect of Hydrophilic Polymers on the Release of BCNU from BCNU-loaded PLGA Wafer (친수성 고분자가 BCNU 함유 PLGA 웨이퍼로부터 BCNU의 방출에 미치는 효과)

  • 안태군;강희정;문대식;이진수;성하수
    • Polymer(Korea)
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    • v.26 no.5
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    • pp.670-679
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    • 2002
  • 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU, carmustine) is one of the effective chemotherapeutic agents which has been used clinically for treating malignant glioma. Poly(D,L-lactide-co-glycolide) (PLGA, molecular weight: 20000 g/mole. mole ratio of lactide to glycolide 75 : 15) is a well known biodegradable polymer used as a drug carrier for drug delivery system. In this study, we investigated the BCNU release behaviour of BCNU-loaded PLGA wafers containing poly (N-vinylpyrrolidone) (PVP) or polyethyleneoxide (PEO) and the effect of hydrophilic polymers incoporated in the wafers. BCNU-loaded PLGA microparticles with or without hydrophilic polymers were prepared by a spray drying method and fabricated into wafers by direct compression. Encapsulation efficiency of BCNU-loaded PLGA microparticles containing PVP and PEO was 85 ∼ 97% and crystallinity of BCNU encapsulated in PLGA decreased significantly initial release amount and release rate of BCNU increased with the increasing PVP or PEO amount. Morphological change and mass loss of wafers during the release test were confirmed that hydration and degradation of PLGA would be facilitated with an increase of hydrophilic polymers.

Peptide Micelles for Anti-cancer Drug Delivery in an Intracranial Glioblastoma Animal Model

  • Yi, Na;Lee, Minhyung
    • Bulletin of the Korean Chemical Society
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    • v.35 no.10
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    • pp.3030-3034
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    • 2014
  • Bis-chloroethylnitrosourea (BCNU) is currently used as an anti-cancer drug for glioblastoma therapy. In this study, BCNU was loaded into the hydrophobic cores of R3V6 amphiphilic peptide micelles for efficient delivery into brain tumors. The scanning electron microscope (SEM) study showed that the BCNU-loaded R3V6 peptide micelles (R3V6-BCNU) formed spherical micelles. MTT assay showed that R3V6-BCNU more efficiently induced cell death in C6 glioblastoma cells than did BCNU. In the Annexin V assay, R3V6-BCNU more efficiently induced apoptosis than did BCNU alone. Furthermore, the results showed that R3V6 was not toxic to cells. The positive charges of the R3V6 peptide micelles may facilitate the interaction between R3V6-BCNU and the cellular membrane, resulting in an increase in cellular uptake of BCNU. In vivo evaluation with an intracranial glioblastoma rat model showed that R3V6-BCNU more effectively reduced tumor size than BCNU alone. The results suggest that R3V6 peptide micelles may be an efficient carrier of BCNU for glioblastoma therapy.

Preparation of BCNU-loaded PLGA Wafers and In Vitro Release Behavior (BCNU 함유 PLGA 웨이퍼의 제조와 생체외 방출거동)

  • 성하수;문대식;강길선;이정식;이해방
    • Polymer(Korea)
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    • v.26 no.1
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    • pp.128-138
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    • 2002
  • 1,3-Bis(2-chloroethyl)-1-nitrosourea (BCNU, Carmustine)-loaded poly(D, L-lactide-co-glycolide) (PLGA, lactide/glycolide mole ratio 75 : 25) microparticles were prepared and fabricated into wafers in an attempt to study the possibility for the treatment of malignant glioma by direct inserting the wafers to the tumor or the cavity remained after surgical resection of the tumor. SEM observation of the microparticles prepared by spray drying method revealed that the microparticles were spherical, i. e. microspheres. Significant reduction of the crystallinity of BCNU encapsulated in PLGA was confirmed by X-ray diffraction and differential scanning calorimetry analyses of the BCNU-loaded PLGA microparticles. Release pattern of BCNU was dependent on several preparation parameters, such as the molecular weight and concentration of PLGA, and initial BCNU loading amount, etc. In vitro release of BCNU was prolonged over 8 weeks with close to zero-order release pattern after initial burst effect. Observations of morphological change of wafers and pH change of release media during release test period confirmed that hydration and degradation of PLGA would be facilitated with an increase of BCNU-loading amount.

In Vitro Antitumor Activity of BCNU-Loaded PLGA Wafer Containing Additives (첨가제 함유 BCNU/PLGA웨이퍼의 in vitro 항암 활성)

  • Lee, Jin-Soo;An, Tae-Kun;Shin, Phil-Kyung;Chae, Ghang-Soo;Jeong, Je-Kyo;Lee, Bong;Cho, Sun-Hang;Khang, Gil-Son;Lee, Hai-Bang
    • Polymer(Korea)
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    • v.27 no.3
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    • pp.217-225
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    • 2003
  • We fabricated the 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU, carmustine)-loaded PLGA wafers containing poly(N-vinylpyrrolidone) (PVP) or tedium chloride (NaCl) in order to control the release profile of drug in special shape (3 in diameter, 1 mm in thickness) by direct compression method. In vitro release profiles of BCNU could be controlled by additives contained in the wafers. Initial release amount, release rate and duration of BCNU could be controlled with presence of PVP or NaCl. In vitro antitumor activity accessed using 9L gliosarcoma cell line has been evaluated by assaying the viability of cells treated with BCNU released from the wafers containing additives resulting in continuous growth inhibition of 9L gliosarcoma tumor cells. Specially, the continuous growth inhibition of BCNU-loaded PLGA wafers containing additives was more effective than that of non-additive BCNU-loaded PLGA wafers. The cytotoxic effect of the drug from the wafers containing NaCl as compared to wafers containing PVP was more enhanced.

Toluene Tolerance in Solvent Tolerant Pseudomonas sp. Strains By Antioxidant Defense Systems (항산화 방어 시스템에 의한 유기용매 내성세균 Pseudomonas sp. 균주에서의 톨루엔 내성)

  • Joo, Woo Hong;Choi, Hye Jung;Kim, Da Som;Cho, Yong-Kweon;Kim, Dong Wan
    • Journal of Life Science
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    • v.29 no.12
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    • pp.1401-1407
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    • 2019
  • To elucidate whether or not solvent-tolerant bacteria use anti-oxidative defense systems to defend themselves against toxic solvents, oxidative enzyme activity and total anti-oxidative capacity (T-AOC) were investigated in two tolerant strains of Pseudomonas sp. under toluene stress. The superoxide dismutase (SOD) activities of solvent tolerant BCNU 106 exhibited relatively increased levels at a toluene concentration of 100 mg/l, where those of solvent tolerant BCNU 171 increased at 200 mg/l. A greater than three-fold increase in catalase (CAT) levels was observed at concentrations of 200 and 300 mg/l in BCNU 106, and a two-fold increase was monitored at the same concentrations in BCNU 171. High glutathione S-transferase (GST) levels were also observed in the solvent tolerant bacteria. Higher levels of T-AOC was expressed in the solvent tolerant strains than in the ordinary non-tolerant KACC 10266. The highest plateau of SOD in BCNU 171 was observed at 1 hr of toluene exposure. CAT levels plateaued at 1 hr and 14 hr in BCNU 106 and reached the highest plateau at 3 hr in BCNU 171. The highest peak of T-AOC occurred at 9 hr in BCNU 106, and two high peaks occurred in BCNU 171, at 1 hr and at 9 hr of toluene exposure. The solvent-tolerant bacteria showed active antioxidant responses and could survive under harsh environments, including the presence of solvents, through means of antioxidant defense systems.

Evaluation of the Potential of Organic Solvent Tolerant Bacillus sp. BCNU 5005 (유기용매내성 세균 Bacillus sp. BCNU 5005의 유용성에 대한 검증)

  • Choi, Hye-Jung;Hwang, Min-Jung;Jeong, Young-Kee;Joo, Woo-Hong
    • Journal of Life Science
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    • v.21 no.5
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    • pp.700-705
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    • 2011
  • Using enrichment procedures, we isolated organic solvent-tolerant Bacillus sp. BCNU 5005 from waste water and soil in the Ulsan industrial plant region. BCNU 5005 had a maximum similarity of 98% with B. subtilis and was designated as B. subtilis based on phylogenetic analyses using 16S rDNA sequences. Generally, most bacteria and their enzymes are destroyed or inactivated in the presence of high concentrations of organic solvents. However, the lipase activity of B. subtilis BCNU 5005 was very stable in the presence of various kinds of solvents (25%, v/v) except chloroform, ethylbenzene and decane. Furthermore, BCNU 5005 was determined to have a degradative ability towards organic solvents. This organic solvent tolerant Bacillus sp. BCNU 5005 could be used as a new potential resource for biotransformation and bioremediation.

Characteristics of BCNU-loaded PLGA Wafers (BCNU를 함유한 생분해성 PLGA 웨이퍼의 특성분석)

  • 안태군;강희정;이진수;성하수;정제교
    • Polymer(Korea)
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    • v.26 no.5
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    • pp.691-700
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    • 2002
  • Interstitial therapy using biodegradable polymeric device loaded with anticancer agent can deliver the drug to the tumor site at high concentration, resulting in an increase of therapeutic efficacy. 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU, carmustine) is most commonly used as chemotherapeutic agent for brain tumors. The design of implantable device is regarded as an important factor lot the efficient delivery of antitumor agent to targeting site. In order to control the release profile of drug, the release pattern of BCNU with the changes of various dimension and additives was investigated. The PLGA wafers containing 3.85, 10, 20 and 30% of BCNU were prepared in various shape (diameter of 3, 5 and 10 mm, thickness of 0.5, 1 and 2 mm) by direct compression method. In vitro drug release profile of BCNU-loaded PLGA wafers could be controlled by changing the dimension of wafers such as initial drug content, weight, diameter, thickness, volume and surface area of wafers, as well as PLGA molecular weight and additives. Drug release from BCNU-loaded PLGA wafers was facilitated with an increase of BCNU-loading amount or presence of poly(N-vinylpyrrolidone)(PVP) or sodium chloride (NaCl). The effects of various geometric factors and additives on the BCNU release pattern were confirmed by the investigation of mass loss and morphology of BCNU-loaded PLGA wafers.

Characteristics of Paenibacillus sp. BCNU 5016 as a Novel Probiotic (신규 프로바이오틱스로서 Peanibacillus sp. BCNU 5016의 특성)

  • Choi, Hye Jung;Kim, Dong Wan;Joo, Woo Hong
    • Journal of Life Science
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    • v.24 no.2
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    • pp.161-166
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    • 2014
  • We screened Paenibacillus sp. strains from Jeotgal, a Korean salted and fermented fish product, for use as a novel probiotic. Among these Paenibacillus sp. isolates, BCNU 5016 was a typical Paenibacillus sp. strain that showed gram-positive, gelatinase-negative, and urease negative activity. On the basis of 16S rDNA sequence comparisons, BCNU 5016 was most closely related phylogenetically to P. polymyxa. When Paenibacillus sp. BCNU 5016 was subjected to the acid tolerance test, this strain showed 91.89% survival after 3 h culture at pH 2.5. Paenibacillus sp. BCNU 5016 also showed excellent bile acid tolerance. Furthermore, its auto-aggregation, coaggregation, and hydrophobic capacities suggest that BCNU 5016 had the capacity to adhere well to the intestinal tract. We conclude that Paenibacillus sp. BCNU 5016 has excellent potential as a probiotic.

Probiotic Potential of Indigenous Bacillus sp. BCNU 9028 Isolated from Meju (메주로부터 분리한 토착 Bacillus sp. BCNU 9028의 프로바이오틱스로서 이용 가능성)

  • Shin, Hwa-Jin;Bang, Ji-Hun;Choi, Hye-Jung;Kim, Dong-Wan;Ahn, Cheol-Soo;Jeong, Young-Kee;Joo, Woo-Hong
    • Journal of Life Science
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    • v.22 no.5
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    • pp.605-612
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    • 2012
  • Spore-forming bacteria are being used as probiotic supplements for human and animal use, due to their low pH stability and ability to survive the gastric barrier. In this study, the BCNU 9028 strain was screened from meju, a Korean fermented soybean food starter. Biochemical and physiological characteristics, as well as 16S rDNA sequence analyses, indicate that this strain belongs to the genus $Bacillus$. $Bacillus$ sp. BCNU 9028 showed a 92% survivability at pH 2.5 and could also withstand 0.3% ox bile. Furthermore, it was postulated that $Bacillus$ sp. BCNU 9028 could prevent biofilm formation and adherence of food-borne pathogens such as $Listeria$ $monocytogenes$, $S.$ $aureus$ and $E.$ $coli$ on the basis of its autoaggregation and coaggregation capacity with food-borne pathogens. It was shown that BCNU 9028 has good abilities to adhere to the intestinal tract from its hydrophobic character (63.3%). The $Bacillus$ sp. BCNU 9028 strain especially elicited antibacterial activity against both Gram-positive and -negative pathogens. These findings suggested that the $Bacillus$ sp. BCNU 9028 strain could be used as a potential probiotic.

Pseudomonas putida BCNU171의 유기용매 내성 및 toluene 내성 관련 유전자의 클로닝

  • Ju, U-Hong;Kim, Sun-Jeong;Lee, Ho-Won;Choe, Seung-Tae;Jeong, Yeong-Gi
    • 한국생물공학회:학술대회논문집
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    • 2002.04a
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    • pp.180-183
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    • 2002
  • Pseudomonns putida BCNU171 had the tolerant ability to several other organic solvents headed by toluene and xylene. Several mutants were made by mating of BCNUl71, pJFF350 to clarify the structure tolerance gene related. From this mutants the 7 of mutants related with toluene sensitive mutants were selected. pBCNUT-2, pBCNUT-4, pBCNUT-9 was transformed, and from this separated plasmid DNA sequences the gene having high homology was searched. In the case of toluene sensitive mutant it was todX gene (pBCNU4) related with cell membrane, ttgE gene (pBCNU2, pBCNU9) and ttgF gene (pBCNU2, pBCNU9).

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