A PHYSICOCHEMICAL STUDY OF THE MORPHOLOGY OF PROGESTERONE-LOADED MICROSPHERES FABRICATED FROM POLY(D,L-LACTIDE-CO-GLYCOLIDE)

被引:36
作者
ROSILIO, V
BENOIT, JP
DEYME, M
THIES, C
MADELMONT, G
机构
[1] UNIV PARIS SUD, PHYSICOCHIM SURFACES & INNOVAT PHARMACOTECH LAB, CNRS, URA 1218, F-92296 CHATENAY MALABRY, FRANCE
[2] FAC PHARM ANGERS, PHARM GALEN LAB, F-49100 ANGERS, FRANCE
[3] WASHINGTON UNIV, BIOL TRANSPORT LAB, ST LOUIS, MO 63130 USA
来源
JOURNAL OF BIOMEDICAL MATERIALS RESEARCH | 1991年 / 25卷 / 05期
关键词
D O I
10.1002/jbm.820250509
中图分类号
R318 [生物医学工程];
学科分类号
0831 ;
摘要
Progesterone-loaded microspheres are fabricated by a solvent evaporation process from a poly(D,L-lactide-co-glycolide) (85/15 PLG) and from alpha-progesterone. Methylene chloride is used as solvent and polyvinyl alcohol and methylcellulose are used as surfactants. The microspheres are characterized by scanning electron microscopy, differential scanning calorimetry, and x-ray powder diagrams. Our study shows that the morphology and the thermal behavior of PLG microspheres can vary significantly with progesterone loading and sample thermal history. Below and at 16.5% loading the microspheres exhibit a smooth outer surface. Above 23% loading, the surface becomes rough, embedded by copolymer particles or well-defined crystals. Pores and cracks can also be observed. Below 35% the progesterone is molecularly dispersed. At 35% and above crystal domains of the steroid appear and two crystalline forms are found: alpha- and beta-progesterone. The physical state of progesterone and the nature of its crystal domains dispersed in the PLG matrix can change during storage. Also a progressive development of an endothermic peak at the T(g) event of the copolymer is observed during storage. No well defined relationship of peak size to progesterone loading can be shown.
引用
收藏
页码:667 / 682
页数:16
相关论文
共 12 条
[1]   STRUCTURAL CHANGES IN GLASSY POLYMERS [J].
ALI, MS ;
SHELDON, RP .
JOURNAL OF APPLIED POLYMER SCIENCE, 1970, 14 (10) :2619-&
[2]   CHARACTERIZATION OF DRUG-LOADED POLY(D,L-LACTIDE) MICROSPHERES [J].
BENITA, S ;
BENOIT, JP ;
PUISIEUX, F ;
THIES, C .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1984, 73 (12) :1721-1724
[3]   A PHYSICOCHEMICAL STUDY OF THE MORPHOLOGY OF PROGESTERONE-LOADED POLY (D,L-LACTIDE) MICROSPHERES [J].
BENOIT, JP ;
COURTEILLE, F ;
THIES, C .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1986, 29 (2-3) :95-102
[4]  
CAMERONI R, 1973, IL FARMACO ED PR, V28, P636
[5]   THE FORMATION AND CHARACTERIZATION OF HYDROCORTISONE-LOADED POLY((+/-)-LACTIDE) MICROSPHERES [J].
CAVALIER, M ;
BENOIT, JP ;
THIES, C .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1986, 38 (04) :249-253
[6]   TOXICITY OF POLYALKYLCYANOACRYLATE NANOPARTICLES .2. DOXORUBICIN-LOADED NANOPARTICLES [J].
COUVREUR, P ;
KANTE, B ;
GRISLAIN, L ;
ROLAND, M ;
SPEISER, P .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1982, 71 (07) :790-792
[7]   DTA EVIDENCE FOR PHYSICAL ORIENTATION (CRYSTALLINITY) IN PVC [J].
MCKINNEY, PV ;
FOLTZ, CR .
JOURNAL OF APPLIED POLYMER SCIENCE, 1967, 11 (07) :1189-&
[8]   THERMAL BEHAVIOR OF ANNEALED ORGANIC GLASSES [J].
PETRIE, SEB .
JOURNAL OF POLYMER SCIENCE PART A-2-POLYMER PHYSICS, 1972, 10 (07) :1255-&
[9]   CONTROLLED RELEASE OF POLYPEPTIDES AND OTHER MACROMOLECULES [J].
SIEGEL, RA ;
LANGER, R .
PHARMACEUTICAL RESEARCH, 1984, (01) :2-10
[10]  
VERT M, 1978, Patent No. 299978