STABILITY STUDY OF DRUG-LOADED PROTEINOID MICROSPHERE FORMULATIONS DURING FREEZE-DRYING

被引：29

作者：

MA, XH ^{[1
]}

SANTIAGO, N ^{[1
]}

CHEN, YS ^{[1
]}

CHAUDHARY, K ^{[1
]}

MILSTEIN, SJ ^{[1
]}

BAUGHMAN, RA ^{[1
]}

机构：

[1] COLLABORAT LABS,E SETAUKET,NY 11733

来源：

JOURNAL OF DRUG TARGETING | 1994年 / 2卷 / 01期

关键词：

FREEZE-DRYING; PROTEINOID MICROSPHERE FORMULATION; STABILITY OF PROTEINOID MICROSPHERES;

D O I：

10.3109/10611869409015889

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Drug-loaded proteinoid microspheres were freeze-dried to facilitate shipping and handling and to enable long term storage. Heparin was chosen as the model drug in developing the optimum lyophilization process. The factors influencing the integrity of either heparin-loaded or unloaded ('empty') proteinoid microspheres during freeze-drying were determined, with emphasis on: selecting an optimum freezing and resuspending temperature; choosing an appropriate cryoprotectant and its optimum concentration in the formulation; and, designing a suitable method for formulating the microspheres. Freezing at/below -70-degrees-C was found to minimize damage to the microspheres. Addition of sugars, such as trehalose and lactose, as cryoprotectants, further increased the stability of the heparin-loaded microspheres during freeze-drying. The optimum trehalose or lactose concentrations were determined to be 5% (w/v). Using the optimumized lyophilization process described in this manuscript, microspheres remained intact during freeze-drying. The freeze-dried microspheres were stable for at least three months post-lyophilization.

引用

页码：9 / 21

页数：13

共 26 条

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