PMID- 20697984 OWN - NLM STAT- MEDLINE DCOM- 20110307 LR - 20220317 IS - 1530-9932 (Electronic) IS - 1530-9932 (Linking) VI - 11 IP - 3 DP - 2010 Sep TI - Formulation and in vitro characterization of Eudragit(R) L100 and Eudragit(R) L100-PLGA nanoparticles containing diclofenac sodium. PG - 1250-6 LID - 10.1208/s12249-010-9489-6 [doi] AB - The aim of this study was to formulate and characterize Eudragit(R) L100 and Eudragit(R) 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(R) L100 nanoparticles was up to 92% at 12 h. However, Eudragit(R)/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(R)/PLGA (20:80), Eudragit(R)/PLGA (30:70) and Eudragit(R)/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. FAU - Cetin, Meltem AU - Cetin M AD - Department of Pharmaceutical Technology, Faculty of Pharmacy, Ataturk University, 25240, Erzurum, Turkey. melcetin@hotmail.com FAU - Atila, Alptug AU - Atila A FAU - Kadioglu, Yucel AU - Kadioglu Y LA - eng PT - Journal Article DEP - 20100810 PL - United States TA - AAPS PharmSciTech JT - AAPS PharmSciTech JID - 100960111 RN - 0 (Anti-Inflammatory Agents, Non-Steroidal) RN - 0 (Delayed-Action Preparations) RN - 0 (Nanocapsules) RN - 0 (Polymethacrylic Acids) RN - 144O8QL0L1 (Diclofenac) RN - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer) RN - 25086-15-1 (methylmethacrylate-methacrylic acid copolymer) RN - 26009-03-0 (Polyglycolic Acid) RN - 33X04XA5AT (Lactic Acid) SB - IM MH - Anti-Inflammatory Agents, Non-Steroidal/administration & dosage/chemistry MH - Delayed-Action Preparations/*chemical synthesis MH - Diclofenac/administration & dosage/*chemistry MH - Diffusion MH - Drug Compounding/methods MH - Lactic Acid/*chemistry MH - Nanocapsules/*chemistry/ultrastructure MH - Polyglycolic Acid/*chemistry MH - Polylactic Acid-Polyglycolic Acid Copolymer MH - Polymethacrylic Acids/*chemistry PMC - PMC2974120 EDAT- 2010/08/11 06:00 MHDA- 2011/03/08 06:00 PMCR- 2011/08/10 CRDT- 2010/08/11 06:00 PHST- 2009/07/10 00:00 [received] PHST- 2010/07/23 00:00 [accepted] PHST- 2010/08/11 06:00 [entrez] PHST- 2010/08/11 06:00 [pubmed] PHST- 2011/03/08 06:00 [medline] PHST- 2011/08/10 00:00 [pmc-release] AID - 9489 [pii] AID - 10.1208/s12249-010-9489-6 [doi] PST - ppublish SO - AAPS PharmSciTech. 2010 Sep;11(3):1250-6. doi: 10.1208/s12249-010-9489-6. Epub 2010 Aug 10.