Internal morphology of poly(D,L-lactide-co-glycolide) BCNU-loaded microspheres. Influence on drug stability. 1998

T Painbeni, and M C Venier-Julienne, and J P Benoit
UPRES EA 2169, University of Angers, France.

The solvent extraction/evaporation process has been used to form poly(D,L-lactide-co-glycolide) (PLAGA) BCNU-loaded microspheres designed for use as intracranial controlled-release implants. Their actual payload could reach 25% with a 20-50 microns size distribution. Scanning electron microscopy showed that such carriers had a smooth surface and a spherical geometry. Differential scanning calorimetry analyses carried out on drug-loaded microspheres established that the PLAGA Tg was markedly shifted towards the low temperatures along with the disappearance of the BCNU melting endotherm. Annealing experiments performed at room temperature did not induce any change of the loaded microsphere DSC profiles. These features indicated that the BCNU acted as a plasticizer for the coating material and formed with it a solid solution. Similarly, stability of encapsulated BCNU was assessed in different conditions of storage. It appeared that drug degradation increased with temperature increase: 5.4, 8.8, 32.4 and 51.2% of decomposition after 3 month storage at -18, 4, room temperature (RT) and 37 degrees C respectively. Since the free drug was stable at 4 degrees C and experienced only 10.6% decomposition at RT during the same storage time, the state of solid solution involving the intimate mixing of the drug and the polyester in the matrix favors a progressive decomposition of BCNU. However, keeping the microspheres 6 months at -18 degrees C or 3 months at 4 degrees C prevents a loss of drug superior to 10%.

UI MeSH Term Description Entries
D008863 Microspheres Small uniformly-sized spherical particles, of micrometer dimensions, frequently labeled with radioisotopes or various reagents acting as tags or markers. Latex Beads,Latex Particles,Latex Spheres,Microbeads,Bead, Latex,Beads, Latex,Latex Bead,Latex Particle,Latex Sphere,Microbead,Microsphere,Particle, Latex,Particles, Latex,Sphere, Latex,Spheres, Latex
D011100 Polyglycolic Acid A biocompatible polymer used as a surgical suture material. Polyglycolide,Biofix,Dexon (Polyester),Dexon-S,Dexon S,DexonS
D011108 Polymers Compounds formed by the joining of smaller, usually repeating, units linked by covalent bonds. These compounds often form large macromolecules (e.g., BIOPOLYMERS; PLASTICS). Polymer
D002330 Carmustine A cell-cycle phase nonspecific alkylating antineoplastic agent. It is used in the treatment of brain tumors and various other malignant neoplasms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p462) This substance may reasonably be anticipated to be a carcinogen according to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (From Merck Index, 11th ed) BCNU,1,3-Bis(2-Chloroethyl)-1-Nitrosourea,BiCNU,FIVB,N,N'-Bis(2-Chloroethyl)-N-Nitrosourea,Nitrumon
D004337 Drug Carriers Forms to which substances are incorporated to improve the delivery and the effectiveness of drugs. Drug carriers are used in drug-delivery systems such as the controlled-release technology to prolong in vivo drug actions, decrease drug metabolism, and reduce drug toxicity. Carriers are also used in designs to increase the effectiveness of drug delivery to the target sites of pharmacological actions. Liposomes, albumin microspheres, soluble synthetic polymers, DNA complexes, protein-drug conjugates, and carrier erythrocytes among others have been employed as biodegradable drug carriers. Drug Carrier
D004339 Drug Compounding The preparation, mixing, and assembly of a drug. (From Remington, The Science and Practice of Pharmacy, 19th ed, p1814). Drug Formulation,Drug Preparation,Drug Microencapsulation,Pharmaceutical Formulation,Compounding, Drug,Formulation, Drug,Formulation, Pharmaceutical,Microencapsulation, Drug,Preparation, Drug
D004355 Drug Stability The chemical and physical integrity of a pharmaceutical product. Drug Shelf Life,Drugs Shelf Lives,Shelf Life, Drugs,Drug Stabilities,Drugs Shelf Life,Drugs Shelf Live,Life, Drugs Shelf,Shelf Life, Drug,Shelf Live, Drugs,Shelf Lives, Drugs
D000077182 Polylactic Acid-Polyglycolic Acid Copolymer A co-polymer that consists of varying ratios of polylactic acid and polyglycolic acid. It is used as a matrix for drug delivery and for BONE REGENERATION. PLGA Acid,LactoSorb,PL-PG Copolymer,PLG Polymer,PLGA Compound,Poly (D,L-lactic-co-glycolic Acid),Poly (Lactic-co-glycolic Acid) -,Poly(D,L-lactide-co-glycolide),Poly(DL-lactide-co-glycolic Acid),Poly(Glycolide-co-lactide),Poly(L-lactide)-co-glycolide,Poly(Lactic-co-glycolic Acid),Poly-L-lactic-polyglycolic Acid,Polylactic-co-glycolic Acid Copolymer,RG 502,Acid, PLGA,Acids, PLGA,Copolymer, PL-PG,Copolymer, Polylactic-co-glycolic Acid,Copolymers, PL-PG,Copolymers, Polylactic-co-glycolic Acid,PL PG Copolymer,PL-PG Copolymers,PLG Polymers,PLGA Acids,PLGA Compounds,Poly L lactic polyglycolic Acid,Poly-L-lactic-polyglycolic Acids,Polylactic Acid Polyglycolic Acid Copolymer,Polylactic co glycolic Acid Copolymer,Polylactic-co-glycolic Acid Copolymers,Polymer, PLG,Polymers, PLG
D000970 Antineoplastic Agents Substances that inhibit or prevent the proliferation of NEOPLASMS. Anticancer Agent,Antineoplastic,Antineoplastic Agent,Antineoplastic Drug,Antitumor Agent,Antitumor Drug,Cancer Chemotherapy Agent,Cancer Chemotherapy Drug,Anticancer Agents,Antineoplastic Drugs,Antineoplastics,Antitumor Agents,Antitumor Drugs,Cancer Chemotherapy Agents,Cancer Chemotherapy Drugs,Chemotherapeutic Anticancer Agents,Chemotherapeutic Anticancer Drug,Agent, Anticancer,Agent, Antineoplastic,Agent, Antitumor,Agent, Cancer Chemotherapy,Agents, Anticancer,Agents, Antineoplastic,Agents, Antitumor,Agents, Cancer Chemotherapy,Agents, Chemotherapeutic Anticancer,Chemotherapy Agent, Cancer,Chemotherapy Agents, Cancer,Chemotherapy Drug, Cancer,Chemotherapy Drugs, Cancer,Drug, Antineoplastic,Drug, Antitumor,Drug, Cancer Chemotherapy,Drug, Chemotherapeutic Anticancer,Drugs, Antineoplastic,Drugs, Antitumor,Drugs, Cancer Chemotherapy
D001672 Biocompatible Materials Synthetic or natural materials, other than DRUGS, that are used to replace or repair any body TISSUES or bodily function. Biomaterials,Bioartificial Materials,Hemocompatible Materials,Bioartificial Material,Biocompatible Material,Biomaterial,Hemocompatible Material,Material, Bioartificial,Material, Biocompatible,Material, Hemocompatible

Related Publications

T Painbeni, and M C Venier-Julienne, and J P Benoit
May 1998, Pharmaceutical research,
T Painbeni, and M C Venier-Julienne, and J P Benoit
May 1991, Journal of biomedical materials research,
T Painbeni, and M C Venier-Julienne, and J P Benoit
January 1998, Journal of microencapsulation,
T Painbeni, and M C Venier-Julienne, and J P Benoit
December 1984, Journal of pharmaceutical sciences,
T Painbeni, and M C Venier-Julienne, and J P Benoit
October 1997, Pharmaceutical research,
T Painbeni, and M C Venier-Julienne, and J P Benoit
December 2012, AAPS PharmSciTech,
T Painbeni, and M C Venier-Julienne, and J P Benoit
May 1995, Journal of pharmaceutical and biomedical analysis,
Copied contents to your clipboard!