Hussain Ali1,2, Benno Weigmann3, Eva-Maria Collnot4, Saeed Ahmad Khan5, Maike Windbergs2,4, Claus-Michael Lehr6,7. 1. Department of Pharmacy, Quaid-i-Azam University, Islamabad, 45320, Pakistan. 2. Biopharmaceutics and Pharmaceutical Technology, Saarland University, Campus A4.1, 66123, Saarbrücken, Germany. 3. Medical Clinic I, University Hospital Erlangen, Research Campus, 91052, Erlangen, Germany. 4. Department of Drug Delivery (DDEL), Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research (HZI), Saarland University, Campus E 8.1, 66123, Saarbrücken, Germany. 5. Department of Pharmacy, Kohat University of Science and Technology, Kohat, KPK, Pakistan. 6. Biopharmaceutics and Pharmaceutical Technology, Saarland University, Campus A4.1, 66123, Saarbrücken, Germany. claus-michael.lehr@helmholtz-hzi.de. 7. Department of Drug Delivery (DDEL), Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research (HZI), Saarland University, Campus E 8.1, 66123, Saarbrücken, Germany. claus-michael.lehr@helmholtz-hzi.de.
Abstract
PURPOSE: The purpose of this study was to evaluate the specifically targeted efficiency of budesonide loaded PLGA nanoparticles for the treatment of inflammatory bowel disease (IBD). METHODS: The nanoparticles were prepared by an oil/water (O/W) emulsion evaporation technique. The nanoparticles were characterized for their size, shape and in vitro drug release profile. Solid state characterization was carried out by differential scanning calorimetry (DSC) and X-ray Power diffraction (XPRD). In order to evaluate the targeted efficiency of nanoparticles, a particle localization study in the healthy and in the inflamed colon was determined in vivo. These data were complemented by cryo-sections. RESULTS: Nanoparticles were 200 ± 05 nm in size with a smooth and spherical shape. The encapsulation efficiency was around 85 ± 3.5%, which was find-out by both, direct and indirect methods. Release of budesonide from the nanoparticles showed a biphasic release profile with an initial burst followed by sustained release. XPRD data revealed that the drug in the polymer matrix existed in crystalline state. Nanoparticles accumulation in inflamed tissues was evaluated by in-vivo imaging system and it was found that particles are accumulated in abundance at the site of inflammation when compared to the healthy group. CONCLUSION: The study demonstrates that the budesonide loaded PLGA nanoparticles are an efficient delivery system for targeted drug delivery to the inflamed intestinal mucosa.
PURPOSE: The purpose of this study was to evaluate the specifically targeted efficiency of budesonide loaded PLGA nanoparticles for the treatment of inflammatory bowel disease (IBD). METHODS: The nanoparticles were prepared by an oil/water (O/W) emulsion evaporation technique. The nanoparticles were characterized for their size, shape and in vitro drug release profile. Solid state characterization was carried out by differential scanning calorimetry (DSC) and X-ray Power diffraction (XPRD). In order to evaluate the targeted efficiency of nanoparticles, a particle localization study in the healthy and in the inflamed colon was determined in vivo. These data were complemented by cryo-sections. RESULTS: Nanoparticles were 200 ± 05 nm in size with a smooth and spherical shape. The encapsulation efficiency was around 85 ± 3.5%, which was find-out by both, direct and indirect methods. Release of budesonide from the nanoparticles showed a biphasic release profile with an initial burst followed by sustained release. XPRD data revealed that the drug in the polymer matrix existed in crystalline state. Nanoparticles accumulation in inflamed tissues was evaluated by in-vivo imaging system and it was found that particles are accumulated in abundance at the site of inflammation when compared to the healthy group. CONCLUSION: The study demonstrates that the budesonide loaded PLGA nanoparticles are an efficient delivery system for targeted drug delivery to the inflamed intestinal mucosa.
Entities:
Keywords:
DSC; XRD; budesonide; colitis; nanoparticles; oxazolone; sustained drug release
Authors: R Löfberg; P Rutgeerts; H Malchow; C Lamers; A Danielsson; G Olaison; D Jewell; O Ostergaard Thomsen; H Lorenz-Meyer; H Goebell; H Hodgson; T Persson; C Seidegård Journal: Gut Date: 1996-07 Impact factor: 23.059
Authors: A Lamprecht; N Ubrich; H Yamamoto; U Schäfer; H Takeuchi; C M Lehr; P Maincent; Y Kawashima Journal: J Control Release Date: 2001-04-28 Impact factor: 9.776
Authors: Beatriz Pelaz; Christoph Alexiou; Ramon A Alvarez-Puebla; Frauke Alves; Anne M Andrews; Sumaira Ashraf; Lajos P Balogh; Laura Ballerini; Alessandra Bestetti; Cornelia Brendel; Susanna Bosi; Monica Carril; Warren C W Chan; Chunying Chen; Xiaodong Chen; Xiaoyuan Chen; Zhen Cheng; Daxiang Cui; Jianzhong Du; Christian Dullin; Alberto Escudero; Neus Feliu; Mingyuan Gao; Michael George; Yury Gogotsi; Arnold Grünweller; Zhongwei Gu; Naomi J Halas; Norbert Hampp; Roland K Hartmann; Mark C Hersam; Patrick Hunziker; Ji Jian; Xingyu Jiang; Philipp Jungebluth; Pranav Kadhiresan; Kazunori Kataoka; Ali Khademhosseini; Jindřich Kopeček; Nicholas A Kotov; Harald F Krug; Dong Soo Lee; Claus-Michael Lehr; Kam W Leong; Xing-Jie Liang; Mei Ling Lim; Luis M Liz-Marzán; Xiaowei Ma; Paolo Macchiarini; Huan Meng; Helmuth Möhwald; Paul Mulvaney; Andre E Nel; Shuming Nie; Peter Nordlander; Teruo Okano; Jose Oliveira; Tai Hyun Park; Reginald M Penner; Maurizio Prato; Victor Puntes; Vincent M Rotello; Amila Samarakoon; Raymond E Schaak; Youqing Shen; Sebastian Sjöqvist; Andre G Skirtach; Mahmoud G Soliman; Molly M Stevens; Hsing-Wen Sung; Ben Zhong Tang; Rainer Tietze; Buddhisha N Udugama; J Scott VanEpps; Tanja Weil; Paul S Weiss; Itamar Willner; Yuzhou Wu; Lily Yang; Zhao Yue; Qian Zhang; Qiang Zhang; Xian-En Zhang; Yuliang Zhao; Xin Zhou; Wolfgang J Parak Journal: ACS Nano Date: 2017-03-14 Impact factor: 15.881
Authors: Zahra Davoudi; Nathan Peroutka-Bigus; Bryan Bellaire; Michael Wannemuehler; Terrence A Barrett; Balaji Narasimhan; Qun Wang Journal: J Biomed Mater Res A Date: 2017-12-21 Impact factor: 4.396