Formulation and In vitro Characterization of Eudragit® L100 and Eudragit® L100-PLGA Nanoparticles Containing Diclofenac Sodium

The aim of this study was to formulate and characterize Eudragit® L100 and Eudragit® L100-poly(lactic-co-glycolic acid) (PLGA) nanoparticles containing diclofenac sodium. Diclofenac generates severe adverse effects with risks of toxicity. Thus, nanoparticles were prepared to reduce these drawbacks i...

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Bibliographic Details
Published in:AAPS PharmSciTech 2010-09, Vol.11 (3), p.1250-1256
Main Authors: Cetin, Meltem, Atila, Alptug, Kadioglu, Yucel
Format: Article
Language:English
Subjects:
Anti-Inflammatory Agents, Non-Steroidal - administration & dosage
Anti-Inflammatory Agents, Non-Steroidal - chemistry
Biochemistry
Biomedical and Life Sciences
Biomedicine
Biotechnology
Delayed-Action Preparations - chemical synthesis
Diclofenac - administration & dosage
Diclofenac - chemistry
Diffusion
Drug Compounding - methods
Indexing in process
Lactic Acid - chemistry
Nanocapsules - chemistry
Nanocapsules - ultrastructure
Pharmacology/Toxicology
Pharmacy
Polyglycolic Acid - chemistry
Polymethacrylic Acids - chemistry
Research Article
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Summary:The aim of this study was to formulate and characterize Eudragit® L100 and Eudragit® L100-poly(lactic-co-glycolic acid) (PLGA) nanoparticles containing diclofenac sodium. Diclofenac generates severe adverse effects with risks of toxicity. Thus, nanoparticles were prepared to reduce these drawbacks in the present study. These nanoparticles were evaluated for surface morphology, particle size and size distribution, percentage drug entrapment, and in vitro drug release in pH 6.8. The prepared nanoparticles were almost spherical in shape, as determined by atomic force microscopy. The nanoparticles with varied size (241–274 nm) and 25.8–62% of entrapment efficiency were obtained. The nanoparticles formulations produced the release profiles with an initial burst effect in which diclofenac sodium release ranged between 38% and 47% within 4 h. The extent of drug release from Eudragit® L100 nanoparticles was up to 92% at 12 h. However, Eudragit®/PLGA nanoparticles showed an initial burst release followed by a slower sustained release. The cumulative release at 72 h was 56%, 69%, and 81% for Eudragit®/PLGA (20:80), Eudragit®/PLGA (30:70) and Eudragit®/PLGA (50:50) nanoparticles, respectively. The release profiles and encapsulation efficiencies depended on the amount of Eudragit in the blend. These data demonstrated the efficacy of these nanoparticles in sustaining the diclofenac sodium release profile.
ISSN:1530-9932
1530-9932
DOI:10.1208/s12249-010-9489-6