화학공학소재연구정보센터
홈 로그인 로그아웃 연락처 사이트맵
Polymer(Korea), Vol.26, No.5, 670-679, September, 2002
Export Citation
친수성 고분자가 BCNU 함유 PLGA 웨이퍼로부터 BCNU의 방출에 미치는 효과
Effect of Hydrophilic Polymers on the Release of BCNU from BCNU-loaded PLGA Wafer
안태군, 강희정, 문대식, 이진수, 성하수1, 정제교2, 강길선, 이해방1, †
  • 전북대학교 유기신물질공학과, 전주 561-756
  • 1한국화학연구원 생체고분자연구실, 대전 305-340
  • 2삼천당제약 중앙연구소, 서울 150-037
Tae Kun An, Hui Jung Kang, Dae Sik Moon, Jin Soo Lee, Hasoo Seong1, Je Kyo Jeong2, Gilson Khang, and Hai Bang Lee1, †
  • Department of Advanced Organic Materials Engineering, Chonbuk National University, 664-14, Dukjin Ku, Chonju 561-756, Korea
  • 1Biomaterials Laboratories, Korea Research Institute of Chemical Technology, P. O. Box 107, Daejon 305-340, Korea
  • 2Research Center, Samchundang Pharm. Co. Ltd., P.O. Box 289, Youngdeungpo, Seoul 150-037, Korea
E-mail:
초록
1,3-bis[2-chloroethyl]-1-nitrosourea (BCNU, carmustine)는 악성 뇌종양 치료를 위하여 화학요법적 임상에서 널리 사용되는 약물이다. 또한, poly(D,L-lactide-co-glycolide) (PLGA, 분자량: 20000 g/mole, 락타이드와 글리콜라이드 몰비 75 : 25)는 약물전달시스템을 위한 약물 전달체로써 사용되어지는 잘 알려진 생분해성 고분자이다. 본 연구에서 폴리비닐피롤리돈 (PVP) 또는 폴리에틸렌옥사이드 (PEO)를 함유하고 있는 BCNU 함유 PLGA 웨이퍼들의 BCNU 방출거동과 웨이퍼에 포접된 친수성 고분자의 효과를 조사하였다. 친수성 고분자의 첨가 또는 첨가 없이 BCNU 함유 PLGA 미분말은 분사건조법에 의해 제조하였으며, 제조된 BCNU 함유 PLGA 미분말은 압축성형법에 의해 웨이퍼형태로 제조하였다. 친수성 고분자가 첨가된 BCNU 함유 PLGA 미분말의 포접율은 85~97%였고, PLGA에 포접된 BCNU의 결성성은 현저히 감소하였다. 약물 방출 경향과 분해 거동에서 친수성 고분자의 함량이 증가할수록 BCNU의 초기방출량과 방출속도는 증가됨을 확인하였다. 방출시험 기간동안 웨이퍼의 형태변화와 무게변화를 측정함으로써 친수성 고분자의 함량이 증가할수록 PLGA의 수화와 분해가 촉진됨을 관찰하였다.
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 hydorphilic polymers.
Keywords:brain tumor;BCNU;hydrophilic polymers;PLGA;microparticles;wafers
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