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Preparation and In vitro Release Characteristics of Hydrophilic Albumin Microspheres Containing Methotrexate and Methotrexate-Human Serum Albumin Conjugates

Hwang, Sung-Joo   (College of Pharmacy. Chungnam National UniversityUU0001302  ); Lee, Myung-Gulll   (College of Pharmacy, Seoul National UniversityUU0000691  ); Kim, Chong-Kook   (College of Pharmacy, Seoul National UniversityUU0000691  );
  • 초록

    Release characteristics of five different types of hydrophilic albumin microspheres (HAM) containing different ratios of methotrexate-albumin (MTX-HSA) conjugates to free MTX: 1 : 0 (HAMC), 3 :1 (HAMC 3F), 1 :1 (HAMCF), 1:3 (HAMCF3) and 0 : 1 (HAMF) were investigated in the absence or presence of protease using dissolution tester. In all the HAMs studied except HAMC, the MTX was released bi-exponentially in the absence of protease; an initial fast release period up to approximately 6h, and thereafter the release rate was very much slower. The fast release of MTX from the HAMs (such as HAMC3F, HAMCF, HAMCF3 and HAMF) at the initial phase in probably due to the release of "physically associated" MTX from the core of the HAMs. The initial rate constants were 7.2, 8.7, 8.5 and 5.9 times greater than the second rate constants for HAMF, HAMCF3, HAMCF and HAMC3F, respectively. MTX release from HAMC was very slow and mono-phasic. It was at most 2.2% of the total entrapped amount by 24 h. The protease accelerated the release of MTX from the HAMs. The percentages of MTX released from HAMs up to 24 h were 100, 89.0, 75.0, 66.0 and 61.0% for HAMF, HAMCF3, HAMCF, HAMC3F and HAMC, respectively in the presence of protease and the corresponding values in the absence of protease were 30.2 19.0, 10.0, 6.5 and 2.2%, respectively. In vitro release of MTX in the presence of protease varied according to the ratios of MTX-HSA conjugates to MTX; the data set from HAMF, HAMCF3 and HAMCF fits better to monophasic first-order profile more adequately than to zero-order profile, that of HAMC3 monophasic first-order, and that of HAMC to bi-phasic zero-order. Above results suggested that zero-order release rate can be achieved by adjusting the ratio of MTX-HSA conjugates to MTX in the preparation of HAMs such as HAMC3F.as HAMC3F.


  • 주제어

    Hydrophilic albumin microspheres .   methotrexate .   methotrexate-human serum albumin conjugates .   in virto drug release .   drug release by protease .   zero-order release.  

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  • 황성주 (47)

    1. 1991 "Microencapsulation of Isoprinosine with Ethylcellulose" Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea 14 (4): 298~304    
    2. 1992 "수종의 붕해제가 살리실아미드정제의 제제특성에 미치는 영향" 藥劑學會誌 = Journal of Korean pharmaceutical sciences 22 (1): 41~48    
    3. 1993 "Alginate Bead를 이용한 고분자 약물의 제어방출형 약물수송체" 藥劑學會誌 = Journal of Korean pharmaceutical sciences 23 (1): 19~26    
    4. 1993 "치아 연마용 인산일수소칼슘의 합성 및 물리화학적 성질" 약학회지 = Yakhak hoeji 37 (1): 66~75    
    5. 1993 "오메프라졸과 Hydroxypropyl-$\beta$-cyclodextrin의 포접화합물의 형성과 특성" 약학회지 = Yakhak hoeji 37 (4): 331~340    
    6. 1993 "오메푸라졸 함유 직장좌제의 제제설계" 약학회지 = Yakhak hoeji 37 (4): 370~382    
    7. 1993 "오메프라졸 함유 직장좌제의 약물속도론적 연구" 약학회지 = Yakhak hoeji 37 (5): 427~436    
    8. 1994 "이온교환수지를 이용한 새로운 오메프라졸 복합체 개발" 약학회지 = Yakhak hoeji 38 (3): 250~264    
    9. 1995 "오메프라졸-에칠렌디아민 복합체를 이용한 제제설계" 藥劑學會誌 = Journal of Korean pharmaceutical sciences 25 (1): 19~29    
    10. 1995 "메토트렉세이트가 표면수식된 알부민 미립구의 제조 및 특성" 藥劑學會誌 = Journal of Korean pharmaceutical sciences 25 (2): 101~108    
  • Kim, Chong-Kook (105)

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