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- 1 1 2 1 3* 2* 2 3100533. 100053 2 1. 5500252. - - - Zeta 20 000 90% Zeta Zeta 202. 62 ± 1. 52nm 0. 17 ± 0. 12mV 58. 20 ± 2. 43% 1. 25 ± 0. 13% t 1 /2 1. 1 h10. 0 h 74. 0% Zeta - doi10. 11669 /cpj. 2013. 09. 010 R944 A 1001-2494201309 - 0700-05 Preparation and Evaluation of Triptolide-Loaded Chitosan / PEG-PLA Nanoparticles LI Jing 1 ZHOU Ying 1 XU Xiu-ling 2 WANG Hai-nan 1 3* WEI Ying-hui 2* GUO Man-man 2 LI Fan-zhu 2 1. College of Life SciencesGuizhou UniversityGuiyang 550025China2. College of Pharmaceutical ScienceZhejiang Chinese Medical UniversityHangzhou 310053China3. China Food and Drug Adminstration Beijing 100053China ABSTRACTOBJECTIVE to evaluate their quality. METHODS To prepare triptolide-loaded chitosan /polyethylene glycol-polylactic acid PEG-PLAnanoparticles and Low molecular weight chitosan was obtained by degradation reactionand the viscosity-average molecular weight and degree of deacetylation were determined by viscometry and acid-base titration methodrespectively. The PEG- PLA nanoparticles were prepared by emulsification solvent evaporation method with chitosan as modifying agent. Then the influence of modification of chitosan on the nanoparticles was investigated. The morphological characteristicsparticle sizezeta potentialencapsulation efficiencydrug loading and release in vitro of the prepared nanoparticles were evaluated. RESULTS The viscosity-average molecular weight and degree of deacetylation of chitosan were 20 000 and 90% respectively. The particle size and Zeta potential of the nanoparticles increased after the modification of chitosanwhile the encapsulation efficiency was almost the same. The shape of the prepared nanoparticles was sphericaland the mean particle sizezeta potentialencapsulation efficiency and drug loading were 202. 62 ± 1. 52nm 0. 17 ± 0. 12mV 58. 20 ± 2. 43% and 1. 25 ± 0. 13% respectively. The release profiles showed that the accumulated release rate of the nanoparticles was 50. 0% at 1. 1 h and reached 74. 0% at 10. 0 h. CONCLUSION Chitosan modification can affect the particle size and Zeta potential. The nanoparticles show a certain sustained release characteristics with welldistributed particle size as well as high entrapment efficiency. KEY WORDStriptolidechitosanPEG-PLA nanoparticlequality evaluation triptolide TP Tripterygium wilfoidii Hook. F 2 3 Li 3 1 TP 30902007 2012R10044-05 * Tel 01088330772 Fax 01088331242-806 E-mailmd_wanghainan@ yahoo. com. cn Tel 057186633173 Fax 057186633030 E-mailweiyinghui@ 163. com 700 2013 5 48 9

2. 1. 1 CS CS chitosan CS 80 ml g - 1 5. 0% 3 h 5 mol L - 1 ph 11 4 2 5 - polyethylene glycol-polylactic acid PEG-PLA 7 6 10. 0 g 1 500 ml 0. 45% PEG-PLA 55 2 h 15 ml 30% - 0. 3% 2 h 5 mol triptolide-loaded chitosan /PEG-PLA nanoparticles L - 1 ph 11 4 000 r CS /TP-NPs min - 1 1 Agilent 1200 Agilent CP225D Sartorius JEM- 1200EX Jeol Nano - ZS 1. 1 8 Mark-Houwink 0. 88 CS M w = 650 000 90% CS η= 0. 006 589 M η M η = 20 000 90% PEG-PLA M w = 10 000 PEG Daton M w = 2 000 degree of deacetylation DD > 98% 101115 9-111567- DD 200502 Poloxamer 188 BASF WP- WA544C 1. 2 Malvern HJ - 6B mol L - 1 g 9. 94% HZ - 9212S 2. 2 DZG - 6050 TP PEG-PLA TGL - 16B 1 500 r min - 1 DL5M 30 g L - 1 poloxamer 188 99 -ⅡDN 2 min360 W 2 s1 s FJ - 200 FJ - 200 3 Viskase h 900 bar 10 7 000 ATS ATS 10 g L - 1 Labconco Labconco poloxamer 188 2 mg ml - 1 5 ml L - 1 2 45 4 h 2. 1. 2 η dl g - 1 M η DD% = c HClV HCl - c NaOH V NaOH 0. 016 m chitosan 9. 94% 100% c HCl mol L - 1 c NaOH mol L - 1 V HCl ml V NaOH ml 0. 016 1 ml 1 HCl g m Chitosan CS /TP-NPs 2. 3 CS 2. 1 CS CS CS /TP-NPs 2. 2 2013 5 48 9 701

TP-NPs Nano-ZS 2. 2 polydispersity PDIZeta Zeta 2. 5. 2 CS /TP-NPs 1 ml 13 000 r min - 1 2. 4 2. 4. 1 HPLC Hypersil ODS2 4. 6 mm 200 mm 5 μm -43 CS /TP- 57 1. 0 ml min - 1 25 NPs CS /TP-NPs 1 ml 218 nm 20 μl 2. 4. 2 TP 0. 22 μm 2. 4. 1 CS /TP-NPs CS /TP-NPs TP 2. 4. 1 HPLC CS /TP-NPs encapsulation effi- 2. 4. 3 TP ciency EE drug loading DL 5. 0 mg 10 ml EE% = W 0 - W 1 /W 0 100% 500. 00 μg ml - 1 TP DL% = W 0 - W 1 /W t 100% 0. 25 0. 50 1. 00 2. 00 4. 00 ml 10 ml TP-NPs W t CS /TP-NPs 12. 50 25. 00 50. 00 100. 00 200. 00 μg ml - 1 2. 4. 1 HPLC CS /TP-NPs 4. 0 ml A ρ 2. 4. 4 TP ph 7. 4 PBS 37 ± 0. 5 12. 50 50. 00 200. 00 μg ml - 1 75 r min - 1 1. 0 ml 3 2. 4. 1 2. 4. 1 HPLC HPLC 1 d 5 d 5 2. 4. 5 CS /TP-NPs 3 6 1 ml 10 ml 3. 1 CS 2. 4. 1 HPLC 2. 4. 6 CS /TP-NPs 90% 0 2 4 8 12 24 h 2. 4. 1 3. 2 HPLC 2. 5 40 min 0. 22 μm 2. 4. 1 TP 10 ml W 0 CS /TP-NPs W 1 CS / 2. 5. 3 TP 300 ml 20% 2. 1. 1 CS M η 20 000 DD 2. 4. 1 HPLC TP 2. 4. 7 CS /TP- 6. 9 min NPs 1. 0 ml 500. 0 μg 1 12. 5 ~ 200 μg ml - 1 ml - 1 TP 0. 25 1. 00 4. 0 ml 10 TP A = 57. 330ρ - 301. 783 r = ml 0. 999 9 TP 12. 5 ~ 200 μg ml - 1 3 0. 22 μm 2. 4. 1 2. 4. 4 3 TP RSD 1. 84% 1. 05% 1. 70% RSD 2. 5. 1 Zeta 1. 67% 1. 51% 2. 69% 2. 4. 5 CS /TP-NPs RSD 1. 93% 2. 4. 6 2 min TP 2. 0% 2 min RSD 2. 04% 2. 4. 7 JEM - 1200EX 3 702 2013 5 48 9

97. 6% 99. 7% 98. 6% RSD 1. 80% 1. 22% 1. 93% 97% 3. 3 CS CS 1 1 CS TP-NPs Zeta 3. 4 3. 4. 1 CS /TP-NPs Zeta CS /TP-NPs CS /TP-NPs 202. 62 ± 1. 52nmPDI 0. 232 ± 0. 009 Zeta 0. 17 ± 0. 12mV 2 3 3. 4. 2 CS /TP-NPs CS /TP-NPs 58. 20 ± 2. 43 % 1. 25 ± 0. 13% 3. 4. 3 20% ph 7. 4 PBS TP t 1 /2 0. 6 h 2. 5 h 99. 9% CS /TP-NPs t 1 /2 1. 1 h 10. 0 h 74. 0% 4 10 CS CS 1 NPsA TP B CS /TP-NPsC 4 4. 1 CS Fig. 1 HPLC Chromatograms of blank nanoparticles A TP standard solution B CS /TP-NPs C 1 Tab. 1 TP-NPs CS /TP-NPs. n = 3 x 珋 ± s Characteristics of TP-NPs and CS /TP-NPs. n = 3 珋 x ± s Type of nanoparticles Particle size /nm PDI Encapsulation efficiency /% Zeta potential /mv TP-NPs 287. 3 ± 8. 7 0. 208 ± 0. 017 40. 9 ± 1. 94-4. 33 ± 0. 21 CS /TP-NPs 302. 9 ± 5. 1 0. 260 ± 0. 019 38. 5 ± 2. 83 0. 14 ± 0. 13 2 Fig. 2 CS /TP-NPs 100 000 TEM Photograph of CS /TP-NPs 100 000 3 Fig. 3 CS /TP-NPs Particle size distribution of CS / TP-NPs 2013 5 48 9 703

4 Fig. 4 珋 x ± s TP CS /TP-NPs. n = 3 x 珋 ± s In vitro release profiles of TP and CS /TP-NPs. n = 3 1. 1 h 50% 1. 1 ~ 10. 0 h TP 13 REFERENCES CS CS CS CS CS 4. 2 CS TP-NPs 11 CS CS TP-NPs CS CS Drug Target2011 CS 5 HE W KUANG C C CS in vitroj CS 438-453. CS PEG-PLA J 1452. 12 PEG-PLA 19964 57-58. J 653. 1 SU M XGAO XSONG Met al. Study on influence of glucoside tripterygium total tablets on metabolism in rats by NMR metabonomic technique J. Chin J Chin Mater Med 201136111449-1452. 2 QIANG ZTAO GXUN Set al. Synthesischaracterization and in vitro evaluation of triptolide-lysozyme conjugate for renal targeting delivery of triptolidej. Arch Pharm Res200629 121164-1170. 3 LI NYANG XZHAI Get al. Multifunctional pluronic /poly ethyleniminenanoparticles for anticancer drugj. J Colloid Interface20103501 117-125. 4 YUAN Z XLI J J ZHU Det al. Enhanced accumulation of low-molecular-weight chitosan in kidneysa study on the influence of N-acetylation of chitosan on the renal targetingj. J 197 540-551. ZHANG H et al. Study on effect of molecular parameters of chitosan on properties of chitosan nanoparticles. Chin Pharm J 2005 40 6 6 ESSA SRABANEL J MHILDGEN P. Characterization of rhodamine loaded PEG-g-PLA nanoparticles NPs Effect of poly ethylene glycolgrafting densityj. Int J Pharm2011 411 1-2 178-187. 7 YUAN Z XGONG TZHANG Z Ret al. Synthesis and characterization of water-soluble chitosan-prednisolone conjugates. Chin Pharm J 2007 42 19 1449-8 CHEN L SZHOU WJIANG Y S. Determination the viscosityaverage molecular weight of chitosanj. Chemistry 9 LIN R XJIANG S HZHANG M S. The methods about degree of deacetylation determination of chitosan J. Chemistry 19923 39-42. 10ZHAO H X JIN HCAI J Y. Microstructure and micromechanical properties of chitosan films under different drying conditions. Acta Phys Chim Sin 2010 263 649-11CHEN H LLV J LYAN J et al. The study of PLGA nanoparticle surface modified with chitosan as protein drug carriers J. J 13LIU M XDONG JYANG Y Jet al. Preparation and toxicity L-lactic acidnanoparticles J. Ac- 556-560. 2012-10-24 4. 3 Func TP Mater 2011 242202-205. PBS of anticancer drugsj 13 TP 2722. PBS of triptolide-loaded polyd 20% ph 7. 4 PBS ta Pharm Sin 2004 397 704 12KHIN Y WFENG S S. Effects of particle size and surface coating on cellular uptake of polymeric nanoparticles for oral delivery. Biomaterials200627 15 2713-2013 5 48 9