Evaluation of the degradation of clonidine-loaded PLGA microspheres

• Published in: Journal of microencapsulation Vol. 30; no. 7; pp. 681 - 691
• Main Authors: Gaignaux, Amélie, Réeff, Jonathan, De Vriese, Carine, Goole, Jonathan, Amighi, Karim
• Format: Journal Article
• Language: English
• Published: Colchester Informa UK Ltd 01-01-2013; Taylor & Francis; Informa
• Subjects: Acidic degradation; Analgesics - administration & dosage; Biological and medical sciences; Buffers; Clonidine - administration & dosage; controlled release; Drug Carriers - chemistry; erosion; General pharmacology; Hydrogen-Ion Concentration; Lactic Acid - chemistry; Medical sciences; microparticles; Microspheres; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; poly(d,l-lactide-co-glycolide acid); Polyglycolic Acid - chemistry; Transition Temperature; X-Ray Diffraction; Imidazole derivatives; Agonist; Lactic acid copolymer; Glycolic acid polymer; poly(D,L-lactide-co-glycolide acid); Imidazoline receptor; Degradation; Aliphatic polymer; Microparticle; Clonidine; Copolymer; Erosion; α2-Adrenergic receptor; Glycolic acid copolymer; Evaluation; Lactone copolymer; Microsphere; Pharmaceutical technology; Controlled release form; Control release polymer; microparticles; Lactic acid polymer; controlled release; Acids; Acidic degradation; Dosage form; Antihypertensive agent; α-Adrenergic receptor agonist
• ISSN: 0265-2048; 1464-5246
• DOI: 10.3109/02652048.2013.778905

Abstract
Context: The release of an encapsulated drug is dependent on diffusion and/or degradation/erosion processes.
Objective: This work aimed to better understand the degradation mechanism of clonidine-loaded microparticles.
Methods: Gel permeation chromatography was used to evaluate the degradation of the polymer. The water-uptake and the weight loss were determined gravimetrically. The swelling behaviour and the morphological changes of the formulations were observed by microscopy. The glass transition temperature and the crystallinity were also determined by differential scanning calorimetry and X-ray diffraction, respectively. The pH of the medium and inside the microspheres was assessed.
Results: The microspheres captured a large amount of water, allowing a decrease in the molecular weight of the polymer. The pH of the medium decreased after release of the degradation products and the pH inside the microparticles remained constant due to the neutralization of these acidic products.
Conclusion: Clonidine and buffers both had an action on the degradation.