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  • 마이크로플루다이저를 이용한 아클라루비신 리포좀의 제조 및 평가
  • Preparation and Evaluation of Aclarubicin Liposome using Microfluidizer
저자명
박목순,박진규,이계원,백명기,지웅길,Park. Mork-Soon,Park. Jin-Kyu,Lee. Gye-Won,Baek. Myoung-Ki,Jee. Ung-Kil
간행물명
약학회지
권/호정보
1998년|42권 3호|pp.265-274 (10 pages)
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

In order to attain a sustained release at targeted organs in a prolonged time which can reduce the side effects and maximize the therapeutic effect, aclarubicin (ACL) was entrap ped into liposomes of different lipid compositions using Microfluidizer, and dry liposomes were prepared by lyophilization. The dry aclarubicin-entrapped liposomes were evaluated in terms of mean particle size and size distribution, entrapment efficiency and in vitro drug release profile. The Entrapment efficiency of liposome, when the concentration of aclarubicin and lipid were 0.5 to 1.0mg/ml and $200{mu}mol$/ml, respectively, was over 80% using Microfluidizer, in contrast to 70% of entrapment efficiency using hand-shaking method. Mean particle size and size distribution of aclarubicin-entrapped liposomes of various lipid compositions did not change considerably by the freeze drying. The range of particle size was between 80 and 200nm. Among aclarubicin-entrapped liposomes, ACL-liposome of PC/DPPC/CH0L/TA displayed the most significant sustained release. The addition of DPPC appeared to be favorable for the control of release. In general, aclarubicin entrapped in liposomes was less stable than free aclarubicin either in pH 7.4 phosphate buffer or in human plasma. Formulation I($t_{1/2}$, 20.3 hr) devoid of lipid additive was the most unstable in the phosphate-buffer solution while formulation II($t_{1/2}$, 40.7 hr) with cardiolipin was the most stable. Half lives of aclarubicin-entrapped liposomes in human plasma were 43.2, 50.7, 35.9 and 35.3 hr for formulation I. II, III and IV, respectively, in contrast to 57.8 hr for free aclarubicin.