INFLUENCE OF AVERAGE MOLECULAR-WEIGHTS OF POLY(DL-LACTIC ACID-CO-GLYCOLIC ACID) COPOLYMERS 50/50 ON PHASE-SEPARATION AND INVITRO DRUG RELEASE FROM MICROSPHERES

被引:47
作者
RUIZ, JM
BUSNEL, JP
BENOIT, JP
机构
[1] FAC PHARM ANGERS,PHARM GALEN LAB,16 BLVD DAVIERS,ANGERS,FRANCE
[2] UNIV PARIS 11,PHARM GALEN & BIOPHARM LAB,CNRS,UA 1218,F-92290 CHATENAY MALABRY,FRANCE
[3] UNIV MAINE,FAC SCI,PHYS CHIM MACROMOLEC LAB,UA 509,F-72017 LE MANS,FRANCE
关键词
average molecular weight; drug release; microencapsulation; poly(DL-lactic acid-co-glycolic acid) copolymers 50/50; polymer–solvent affinity;
D O I
10.1023/A:1015945806917
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The phase separation of fractionated poly(DL-lactic acid-co-glycolic acid) copolymers 50/50 was determined by silicone oil addition. Polymer fractionation by preparative size exclusion chromatography afforded five different microsphere batches. Average molecular weight determined the existence, width, and displacement of the “stability window” inside the phase diagrams, and also microsphere characteristics such as core loading and amount released over 6 hr. Further, the gyration and hydro-dynamic radii were measured by light scattering. It is concluded that the polymer–solvent affinity is largely modified by the variation of average molecular weights owing to different levels of solubility. The lower the average molecular weight is, the better methylene chloride serves as a solvent for the coating material. However, a paradoxical effect due to an increase in free carboxyl and hydroxyl groups is noticed for polymers of 18,130 and 31,030 SEC (size exclusion chromatography) Mw. For microencapsulation, polymers having an intermediate molecular weight (47,250) were the most appropriate in terms of core loading and release purposes. © 1990, Plenum Publishing Corporation. All rights reserved.
引用
收藏
页码:928 / 934
页数:7
相关论文
共 12 条
[1]  
Berne B J, 1976, DYNAMIC LIGHT SCATTE
[2]   PHOTON CORRELATION STUDY OF POLYDISPERSE SAMPLES OF POLYSTYRENE IN CYCLOHEXANE [J].
BROWN, JC ;
PUSEY, PN ;
DIETZ, R .
JOURNAL OF CHEMICAL PHYSICS, 1975, 62 (03) :1136-1144
[3]   DATA HANDLING IN GPC FOR ROUTINE OPERATIONS [J].
BUSNEL, JP .
POLYMER, 1982, 23 (01) :137-141
[4]   BIODEGRADABLE POLYMERS FOR USE IN SURGERY - POLYGLYCOLIC-POLY(ACTIC ACID) HOMOPOLYMERS AND COPOLYMERS .1. [J].
GILDING, DK ;
REED, AM .
POLYMER, 1979, 20 (12) :1459-1464
[5]   BIODEGRADABLE CARRIERS FOR THE SUSTAINED-RELEASE OF POLYPEPTIDES [J].
HUTCHINSON, FG ;
FURR, BJA .
TRENDS IN BIOTECHNOLOGY, 1987, 5 (04) :102-106
[6]  
KISSEL T, 1988, P INT S CONTROL REL, V15, P260
[7]   SYNTHESIS AND BIOLOGICAL-ACTIVITY OF SOME VERY HYDROPHOBIC SUPERAGONIST ANALOGS OF LUTEINIZING-HORMONE-RELEASING HORMONE [J].
NESTOR, JJ ;
HO, TL ;
SIMPSON, RA ;
HORNER, BL ;
JONES, GH ;
MCRAE, GI ;
VICKERY, BH .
JOURNAL OF MEDICINAL CHEMISTRY, 1982, 25 (07) :795-801
[8]  
ORVOEN JB, 1985, SPECTRA, V13, P104
[9]   MICROENCAPSULATION OF PEPTIDE - A STUDY OF THE PHASE-SEPARATION OF POLY(D,L-LACTIC ACID CO-GLYCOLIC ACID) COPOLYMERS 50/50 BY SILICONE OIL [J].
RUIZ, JM ;
TISSIER, B ;
BENOIT, JP .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1989, 49 (01) :69-77
[10]   CLASSIFICATION OF SOLVENT PROPERTIES OF COMMON LIQUIDS [J].
SNYDER, LR .
JOURNAL OF CHROMATOGRAPHY, 1974, 92 (02) :223-230