Abstract:
:Implantable polymeric device that can release chemotherapeutic agent directly into central nervous system (CNS) has had an impact on malignant glioma therapy. The purpose of our study was to develop an implantable polymeric device, which can release intact 1,3-bis(2-chloroethyl)-1-nitrosourea (BCNU) for long-term period over 1 month, and to evaluate its cytotoxicity against XF 498 human CNS tumor cells in vitro. BCNU was incorporated into biodegradable poly(D,L-lactide-co-glycolide) (PLGA), by using spray-drying method. BCNU-loaded PLGA microparticles were characterized by scanning electron microscopy (SEM), powder X-ray diffraction, and differential scanning calorimetry. SEM observation of the microparticles showed that the microparticles were spherical, i.e. microspheres. Homogeneous distribution of BCNU in PLGA microsphere was confirmed by significant reduction of crystallinity of BCNU. Microspheres were fabricated into wafers with flat and smooth surface by direct compression method. In vitro release of BCNU in pH 7.4 phosphate buffered saline was prolonged up to 8 weeks after short initial burst period. Antitumor activity of BCNU-loaded PLGA wafer against XF 498 human CNS tumor cells continued over 1 month and, PLGA only did not affect the growth of the cells. Meanwhile, the cytotoxic activity of BCNU powder disappeared within 12 h. These results strongly suggest that the BCNU/PLGA formulations increase release period of carmustine in vivo and also be useful in the development of implantable polymeric device for malignant glioma.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Seong H,An TK,Khang G,Choi SU,Lee CO,Lee HBdoi
10.1016/s0378-5173(02)00543-4keywords:
subject
Has Abstractpub_date
2003-01-30 00:00:00pages
1-12issue
1-2eissn
0378-5173issn
1873-3476pii
S0378517302005434journal_volume
251pub_type
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journal_title:International journal of pharmaceutics
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更新日期:2007-07-18 00:00:00
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更新日期:2012-09-15 00:00:00
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更新日期:2017-12-20 00:00:00
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pub_type: 杂志文章,评审
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