Development of nanoparticles-in-microparticles system for improved local retention after intra-articular injection

Chen, Zhipeng; Liú, Dan; Wang, Jian; Wu, Liang; Li, Weidong; Chen, Jun; Cai, Baochang; Cheng, Haibo

doi:10.3109/10717544.2013.848495

Cited by 28 publications

(22 citation statements)

References 15 publications

(12 reference statements)

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“…In the attempt to obtain a long-lasting release of therapeutic agents in the synovial cavity through IA administration, different drug delivery systems have been extensively investigated, such as solid lipid particles, polymeric microparticles (MPs) and nanoparticles (NPs) and their combination (NPs-in-MPs), drug–polymer conjugates, hydrogels, and in situ hydrogels as such or containing conventional MPs or NPs [4,16,17,18,19,20,21,22,23]. Overall, conventional nanoscale drug delivery system-based approaches appear very promising because IA administration appears to be simple and better penetration into cartilage tissue is achieved [4].…”

Section: Introductionmentioning

confidence: 99%

Intra-Articular Formulation of GE11-PLGA Conjugate-Based NPs for Dexamethasone Selective Targeting—In Vitro Evaluation

Chiesa

Pisani

Colzani

et al. 2018

IJMS

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Selectively targeted nanoscale drug delivery systems have recently emerged as promising intravenously therapeutic option for most chronic joint diseases. Here, a newly synthetized dodecapeptide (GE11)-polylactide-co-glycolide (PLGA)-based conjugate was used to prepare smart nanoparticles (NPs) intended for intra-articular administration and for selectively targeting Epidermal Growth Factor Receptor (EGFR). GE11-PLGA conjugate-based NPs are specifically uptaken by EGFR-overexpressed fibroblast; such as synoviocytes; which are the primarily cellular component involved in the development of destructive joint inflammation. The selective uptake could help to tune drug effectiveness in joints and to decrease local and systemic side effects. Dexamethasone (DXM) is a glucorticoid drug commonly used in joint disease treatment for both systemic and local administration route. In the present research; DXM was efficiently loaded into GE11-PLGA conjugate-based NPs through an eco-friendly nanoprecipitation method set up for this purpose. DXM loaded GE11-PLGA conjugate-based NPs revealed satisfactory ex vivo cytocompatibility; with proper size (≤150 nm) and good dimensional stability in synovial fluid. Intra-articular formulation was developed embedding DXM loaded GE11-PLGA conjugate-based NPs into thermosetting chitosan-based hydrogel; forming a biocompatible composite hydrogel able to quickly turn from liquid state into gel state at physiological temperature; within 15 min. Moreover; the use of thermosetting chitosan-based hydrogel extends the local release of active agent; DXM.

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Section: Introductionmentioning

confidence: 99%

Intra-Articular Formulation of GE11-PLGA Conjugate-Based NPs for Dexamethasone Selective Targeting—In Vitro Evaluation

Chiesa

Pisani

Colzani

et al. 2018

IJMS

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“…The measurements were performed in sextuplicate. Dialysis method selected to examine the in vitro release of free QT and QT-loaded NPs (Chen et al, 2014) is also described in the Supplementary files.…”

Section: Characterization Of Qt-loaded Npsmentioning

confidence: 99%

Quercetin-loaded poly (lactic-co-glycolic acid)-d-α-tocopheryl polyethylene glycol 1000 succinate nanoparticles for the targeted treatment of liver cancer

Guan

Gao

et al. 2016

Drug Delivery

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Utilization of quercetin (QT) in clinics is limited by its instability and poor solubility. To overcome these disadvantages, we prepared QT as QT-loaded PLGA-TPGS nanoparticles (QPTN) and examined its properties and therapeutic efficacy for liver cancer. QT-loaded PLGA nanoparticles (QPN) and QT/coumarin-6-loaded PLGA-TPGS nanoparticles (QCPTN) with coumarin-6 as a fluorescent marker were also prepared to investigate the cellular uptake by HepG2 and HCa-F cells using a confocal laser scanning microscope (CLSM), and their effects on apoptosis of HepG2 cells were assessed with flow cytometry. The results measured using transmission electron microscopy, scanning electron microscopy and size analyses indicated that QPTN were stably dispersed sphere with diameter in the range of 100-200 nm. It indicated that the QT loading and encapsulation efficiency in QPTN reached 21.63% and 93.74%, respectively, and the accumulative drug release of QPTN was 85.8%, the QCPTN uptake in HCa-F and HepG2 cells were 50.87% and 61.09% using HPLC analysis, respectively. The results determined using an Annexin-PI flow cytometry indicated that QPTN could induce HepG2 cell apoptosis in a dose dependent manner. The results of histological examination and HPLC analysis confirmed that QPTN was targeted to liver cells. In vivo analysis using solid tumorbearing mouse model indicated that QPTN could suppress tumor growth by 59.07%. Moreover, all the studied properties of QPTN were more desirable than those of QT-loaded PLGA nanoparticles (QPN). In conclusion, QPTN could be used as a potential intravenous dosage form for the treatment of liver cancer owing to the enhanced pharmacological effects of QT with increased liver targeting.

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“…17,18,19 Briefly, 5 mg DS containing different nanoparticle formulations were suspended in 1 mL of pH 7.4 phosphate buffer then placed in dialysis bag. For hydrogel formulations, 5 mg of non-encapsulated DS containing hydrogel or 14 mg of F6 coded nanoparticle bearing (contains 5 mg DS) 1 mL hydrogel were put in dialysis bag directly without any dilution.…”

Section: In Vitro Releasementioning

confidence: 99%

<i>In Situ</i> Hydrogel Formulation for Intra-Articular Application of Diclofenac Sodium-Loaded Polymeric Nanoparticles

Küçüktürkmen

Öz

Bozkır

2017

tjps

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Objectives: The world's population is getting older and the number of people suffering from arthritis is a major problem according to World Health Organization's data. In this respect, the need for more efficient treatment for arthritis becomes an urgent issue. In this research, nanoparticle bearing in situ gelling hydrogel formulation was developed for prolonged local delivery of diclofenac sodium (DS). Materials and Methods: Emulsion-solvent evaporation technique was used for the preparation of nanoparticles. Particle size, encapsulation efficiency, morphology, and drug release profile of DS loaded biodegradable nanoparticles as well as gel viscosity and gelation time of in situ gelling hydrogel formulations were optimized to increase the time interval between each dose application for enhanced patience compliance. Results:The spherical nanoparticles with a mean particle diameter of 168 nm was obtained and confirmed by both transmission electron microscope and atomic force microscope. Different types of surfactants were tested in the first emulsification step of nanoparticle production process and Arlacel ® -C significantly increased the encapsulation efficiency to 89.7%. Thirty days prolonged in vitro release of DS was achieved by using the combined formulation of polymeric nanoparticles and in situ hydrogel prepared by using poloxomer 407 and chitosan. Conclusion: Local administration of DS with this novel delivery system could be considered of having potential to minimize side effects associated with decreased amount of drug in dosage form compared to conventional oral dose. Key words: Diclofenac sodium, drug delivery, PLGA, Poly(ε-caprolactone), thermosensitive hydrogel, poloxamers ABSTRACT ÖZ Amaç: Dünya Sağlık Örgütü'nün verilerine göre dünya çapında insanların yaş ortalaması ve bağlantılı olarak artrit hastalığından mağdur olan insan sayısı da artmaktadır. Bu açıdan bakıldığında, artrit tedavisi için daha etkili tedavilerin gerekliliği önemli hale gelmiştir. Bu araştırmada, diklofenak sodyumun (DS) uzatılmış lokal taşınımı için nanopartikül içeren in situ hidrojel formülasyonları geliştirilmiştir. Gereç ve Yöntemler: Nanopartiküllerin hazırlanmasında emülsiyon-çözücü buharlaştırma yöntemi kullanılmıştır. DS yüklü nanopartiküllerin partikül büyüklüğü, enkapsülasyon etkinliği, morfolojisi ve ilaç salım profilleri ile in situ hidrojelin jel viskozitesi ve jelleşme süresi, hasta uyuncunu artırmak için her bir dozun uygulanması arasındaki zamanı artırmak amacıyla optimize edilmiştir. Bulgular: Ortalama partikül büyüklüğü 168 nm olan küresel nanopartiküller elde edilmiş ve geçirimli elektron mikroskobu ve atomik kuvvet mikroskobu ile desteklenmiştir. Nanopartikül üretim sürecinin ilk emülsifikasyon adımında farklı sürfaktanlar denenmiş ve Arlacel ® -C diklofenak sodyumun enkapsülasyon etkinliğini %89.7'ye yükseltmiştir. DS'nin 30 güne uzatılmış in vitro salımı, nanopartiküllerin ve poloksamer 407/kitozan ile hazırlanmış in situ hidrojelin kombine kullanılmasıyla başarılmıştır. Sonuç: DS'nin bu yenilikçi taşıy...

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Development of nanoparticles-in-microparticles system for improved local retention after intra-articular injection

Cited by 28 publications

References 15 publications

Intra-Articular Formulation of GE11-PLGA Conjugate-Based NPs for Dexamethasone Selective Targeting—In Vitro Evaluation

Intra-Articular Formulation of GE11-PLGA Conjugate-Based NPs for Dexamethasone Selective Targeting—In Vitro Evaluation

Quercetin-loaded poly (lactic-co-glycolic acid)-d-α-tocopheryl polyethylene glycol 1000 succinate nanoparticles for the targeted treatment of liver cancer

<i>In Situ</i> Hydrogel Formulation for Intra-Articular Application of Diclofenac Sodium-Loaded Polymeric Nanoparticles

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