Pharmacodynamics of diclofenac from novel Eudragit entrapped microspheres.

Abstract:

:Effective clinical utilization of non-steroidal anti-inflammatory drugs such as diclofenac sodium (DS) is significantly limited by their ulcerogenic potential and poor bioavailability after oral administration, thus necessitating the need for a better carrier to minimize these obvious limitations. The objective of this study was to evaluate Eudragit® RS100/RL100 microspheres formulated by the solvent-evaporation technique for improved delivery of diclofenac. Three batches of (DF1, DF2 and DF3) microspheres were prepared using different ratios of Eudragit RS-100 and RL-100 polymers based on the solvent-evaporation method. The microspheres were characterized based on morphological properties, particle size analysis and encapsulation efficiency (EE%). In vitro release of DS was investigated in both 0.1 N HCl (pH 1.2) and phosphate-buffered saline (pH 7.4), while anti-inflammatory studies were evaluated in the rat model. Maximum EE% of 86.61 ± 0.11, 88.14 ± 0.16 and 85.50 ± 0.21 was obtained for DF1, DF2 and DF3, respectively. Discrete, smooth and brownish microspheres of size range 437 ± 0.01-479 ± 0.21 µm were obtained. Release of DS from the formulation depends on the polymer ratio. All the batches exhibited good anti-inflammatory activities. Microsphere formulations based on Eudragit® polymers would likely offer a reliable and alternative means of delivering DS orally.

journal_name

Drug Deliv

journal_title

Drug delivery

authors

Momoh MA,Kenechukwu FC,Adedokun MO,Odo CE,Attama AA

doi

10.3109/10717544.2013.843608

subject

Has Abstract

pub_date

2014-05-01 00:00:00

pages

193-203

issue

3

eissn

1071-7544

issn

1521-0464

journal_volume

21

pub_type

杂志文章
  • Floating microspheres of carvedilol as gastro retentive drug delivery system: 3(2) full factorial design and in vitro evaluation.

    abstract:CONTEXT:Designing a sustained release system for Carvedilol to increase its residence time in the stomach. OBJECTIVE:Preparation of floating microsphere by the emulsion solvent diffusion method, studying the effect of various process parameters and optimize the formulation using full factorial design. METHODS:Differe...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2013.834414

    authors: Nila MV,Sudhir MR,Cinu TA,Aleykutty NA,Jose S

    更新日期:2014-03-01 00:00:00

  • Solid lipid nanoparticles for ocular drug delivery.

    abstract::Ocular drug delivery remains challenging because of the complex nature and structure of the eye. Conventional systems, such as eye drops and ointments, are inefficient, whereas systemic administration requires high doses resulting in significant toxicity. There is a need to develop novel drug delivery carriers capable...

    journal_title:Drug delivery

    pub_type: 杂志文章,评审

    doi:10.3109/10717544.2010.483257

    authors: Seyfoddin A,Shaw J,Al-Kassas R

    更新日期:2010-09-01 00:00:00

  • Floating-bioadhesive microspheres containing acetohydroxamic acid for clearance of Helicobacter pylori.

    abstract::A new strategy based on gastric retention is proposed for the treatment of Helicobacter pylori. (H. pylori). A synergism between a floating and a bioadhesive system has been explored. Floating microspheres containing the antiurease drug acetohydroxamic acid (AHA) were prepared by a novel quasi-emulsion solvent diffusi...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717540260397837

    authors: Umamaheswari RB,Jain S,Tripathi PK,Agrawal GP,Jain NK

    更新日期:2002-10-01 00:00:00

  • Neuronal mitochondria-targeted therapy for Alzheimer's disease by systemic delivery of resveratrol using dual-modified novel biomimetic nanosystems.

    abstract::Reactive oxygen species (ROS)-induced neuronal mitochondrial dysfunction is a key pathologic factor in sporadic Alzheimer's disease (AD). Neuronal mitochondria have been proposed to be a promising therapeutic target for AD, especially for the failures of phase III clinical trials on conventional amyloid-β (Aβ) targete...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2020.1745328

    authors: Han Y,Chu X,Cui L,Fu S,Gao C,Li Y,Sun B

    更新日期:2020-12-01 00:00:00

  • Modified nanoparticles with cell-penetrating peptide and amphipathic chitosan derivative for enhanced oral colon absorption of insulin: preparation and evaluation.

    abstract::Colon is an ideal absorptive site for oral protein and peptide drug (insulin), and yet it poses multiple barriers against the drug absorption, such as the barriers against the drug diffusion from colon lumen toward the absorptive mucosa and permeation across colon epithelium. In this study, modified nanoparticles (Tat...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2015.1048489

    authors: Guo F,Zhang M,Gao Y,Zhu S,Chen S,Liu W,Zhong H,Liu J

    更新日期:2016-07-01 00:00:00

  • Development of artemether and lumefantrine co-loaded nanostructured lipid carriers: physicochemical characterization and in vivo antimalarial activity.

    abstract:CONTEXT:Artemether and lumefantrine combination therapy is well-accepted for uncomplicated malaria treatment. However, the current available formulation has several pharmacokinetic mismatches such as drug degradation in gastrointestinal tract, erratic absorption, etc. Hence, need of the hour is the injectable formulati...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2014.905883

    authors: Parashar D,Aditya NP,Murthy RS

    更新日期:2016-01-01 00:00:00

  • The efficiency of a novel delivery system (PEI600-Tat) in development of potent DNA vaccine using HPV16 E7 as a model antigen.

    abstract::DNA vaccination is a promising approach for inducing both humoral and cellular immune responses. The mode of plasmid DNA delivery is critical to make progress in DNA vaccination. Using human papillomavirus type 16 E7 as a model antigen, this study evaluated the effect of peptide-polymer hybrid including PEI600-Tat con...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717540902757721

    authors: Bolhassani A,Ghasemi N,Servis C,Taghikhani M,Rafati S

    更新日期:2009-05-01 00:00:00

  • Characterization and evaluation of a self-microemulsifying drug delivery system containing tectorigenin, an isoflavone with low aqueous solubility and poor permeability.

    abstract::The purpose of this study was to characterize and evaluate tectorigenin-loaded self-microemulsifying drug delivery system (TG-SMEDDS), a previously studied preparation, and further confirm the improvement of TG in solubility and bioavailability. The appearance of TG-SMEDDS was clear and transparent, with good mobility...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2017.1284946

    authors: Zhang Y,He L,Yue S,Huang Q,Zhang Y,Yang J

    更新日期:2017-11-01 00:00:00

  • Formulation of Fe3O4/acrylate co-polymer nanocomposites as potential drug carriers.

    abstract::Magnetic nanocomposite particles were synthesized by encapsulating nanosized magnetite with an acrylate-based cationic co-polymer made of MMA, BA, and QMA and modifying with MeOPEGMA using the water replacement method. The composition of the co-polymer formulation was optimized based on zeta-potential measurements and...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717540801952597

    authors: Phanapavudhikul P,Shen S,Ng WK,Tan RB

    更新日期:2008-03-01 00:00:00

  • Formulation and evaluation of dextromethorphan hydrobromide sustained release tablets.

    abstract::Sustained release (SR) matrix tablets of dextromethorphan hydrobromide were prepared by wet granulation using hydroxypropyl methyl cellulose (HPMC-K-100 CR) as the hydrophilic rate controlling polymer. The effect of the concentration of the polymer and different fillers on the in vitro drug release rate was studied. T...

    journal_title:Drug delivery

    pub_type: 杂志文章,随机对照试验

    doi:10.1080/10717540802035301

    authors: Meyyanathan SN,Rajan S,Muralidaharan S,Siddaiah MK,Krishnaraj K,Suresh B

    更新日期:2008-09-01 00:00:00

  • Propolis organogel as a novel topical delivery system for treating wounds.

    abstract:CONTEXT:Propolis has traditionally been used in curing infections and healing wounds and burns. OBJECTIVE:The aim of this study is to formulate pluronic lecithin organogel of propolis to improve its availability and antimicrobial activity. MATERIALS AND METHODS:Different organogels were prepared by using soybean leci...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2013.847032

    authors: Balata G,El Nahas HM,Radwan S

    更新日期:2014-02-01 00:00:00

  • Preparation, characterization, and antitumor activities of folate-decorated docetaxel-loaded human serum albumin nanoparticles.

    abstract:CONTEXT:Docetaxel is now a major antitumor drug in clinical use for the treatment of a variety of tumors. The ethanol/Tween 80 solvent required in the formulation to increase the docetaxel solubility is at least partly responsible for the hypersensitivity reaction, decreased uptake by tumor tissue, and increased exposu...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2013.879964

    authors: Jiang S,Gong X,Zhao X,Zu Y

    更新日期:2015-02-01 00:00:00

  • Sustained ocular drug delivery from a temperature and pH triggered novel in situ gel system.

    abstract::Various ocular diseases like glaucoma, conjunctivitis, and dry eye syndrome require frequent drug administration. Poor ocular bioavailability of drugs (< 1%) from conventional eye drops is due mainly to the precorneal loss factors that include rapid tear turnover, nonproductive absorption, transient residence time in ...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717540701606426

    authors: Gupta H,Jain S,Mathur R,Mishra P,Mishra AK,Velpandian T

    更新日期:2007-11-01 00:00:00

  • Targeted nano-delivery strategies for facilitating thrombolysis treatment in ischemic stroke.

    abstract::Ischemic stroke is one of the major causes of severe disability and death worldwide. It is mainly caused by a sudden reduction in cerebral blood flow due to obstruction of the supplying vessel by thrombi and subsequent initiation of a complex cascade of pathophysiological changes, which ultimately lead to brain ischem...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2021.1879315

    authors: Ma H,Jiang Z,Xu J,Liu J,Guo ZN

    更新日期:2021-12-01 00:00:00

  • Lung cancer combination therapy: co-delivery of paclitaxel and doxorubicin by nanostructured lipid carriers for synergistic effect.

    abstract:CONTEXT:Paclitaxel (PTX) and doxorubicin (DOX) are widely used for the combined chemotherapy of solid tumors. However, free drug combination has lower antitumor efficiency. It is necessary to design a drug delivery system to carry both of them. OBJECTIVE:This study aimed to engineer a nano-drug delivery system for co-...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2015.1055619

    authors: Wang Y,Zhang H,Hao J,Li B,Li M,Xiuwen W

    更新日期:2016-05-01 00:00:00

  • Assessment of the efficacy of drug transdermal delivery by electro-phonophoresis in treating tuberculous lymphadenitis.

    abstract::Electro-phonophoresis (EP) has been used in various clinical fields. The objective of present study is to evaluate the skin permeability of isoniazid (INH) and rifampicin (RIF) in patients with tuberculous lymphadenitis with the aid of EP to validate the clinical applications of this transdermal delivery system for th...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2015.1124474

    authors: Chen S,Qin M,Han Y,Zhao L,Fu Y,Shang Y,Liu Z,Huang H

    更新日期:2016-06-01 00:00:00

  • The optimized drug delivery systems of treating cancer bone metastatic osteolysis with nanomaterials.

    abstract::Some cancers such as human breast cancer, prostate cancer, and lung cancer easily metastasize to bone, leading to osteolysis and bone destruction accompanied by a complicated microenvironment. Systemic administration of bisphosphonates (BP) or denosumab is the routine therapy for osteolysis but with non-negligible sid...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2020.1856225

    authors: Cheng X,Wei J,Ge Q,Xing D,Zhou X,Qian Y,Jiang G

    更新日期:2021-12-01 00:00:00

  • Β-Cyclodextrin-graft-poly(amidoamine) dendrons as the nitric oxide deliver system for the chronic rhinosinusitis therapy.

    abstract::Chronic rhinosinusitis (CRS) is a rather prevalent condition with a chronic inflammatory process, which is hard to cure. Herein, a new antibacterial drug, nitric oxide (NO), was used for the attempt on CRS therapy. To achieve this, a star copolymer (β-CD-PAMAM) consisting of the β-cyclodextrin (β-CD) core and seven PA...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2021.1876183

    authors: Liu T,Li G,Wu X,Chen S,Zhang S,Han H,Zhang H,Luo X,Cai X,Ma D

    更新日期:2021-12-01 00:00:00

  • PLA/PEG-PPG-PEG/dexamethasone implant prepared by hot-melt extrusion for controlled release of immunosuppressive drug to implantable medical devices, Part 2: in vivo evaluation.

    abstract::Hot-melt extrusion (HME) plays an important role in preparing implants as local drug delivery systems in pharmaceutical fields. Here, a new PLA/PEG-PPG-PEG/Dexamethasone (PLA/F68/Dex) implant prepared by HME has been developed. Importantly, the implant was successfully achieved to control release of immunosuppressive ...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2013.801049

    authors: Li D,Guo G,Deng X,Fan R,Guo Q,Fan M,Liang J,Luo F,Qian Z

    更新日期:2013-04-01 00:00:00

  • Carboplatin-Loaded PLGA Microspheres for Intracerebral Implantation: In Vivo Characterization.

    abstract::Carboplatin is a potent anticancer agent that has shown efficacy in clinical trials against malignant glioma, one of the most deadly cancers in humans. However, a high systemic dose is required to achieve an effective concentration in the brain because of the presence of the blood-brain barrier (BBB). Such a high dose...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717549709052017

    authors: Chen W,He J,Olson JJ,Lu DR

    更新日期:1997-01-01 00:00:00

  • Sodium alginate microspheres of metoprolol tartrate for intranasal systemic delivery: development and evaluation.

    abstract::Bioadhesive sodium alginate microspheres of Metoprolol tartrate (MT) for intranasal systemic delivery were prepared to avoid the first-pass effect, as an alternative therapy to injection, and to obtain improved therapeutic efficacy in the treatment of hypertension and angina pectoris. The microspheres (Ms) were prepar...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/713840323

    authors: Rajinikanth PS,Sankar C,Mishra B

    更新日期:2003-01-01 00:00:00

  • Transdermal delivery of isoniazid and rifampin in guinea pigs by electro-phonophoresis.

    abstract::Electro-phonophoresis (EP) has been used as a drug delivery approach in clinical fields. The objective of the present study is to evaluate the skin permeability of isoniazid and rifampin in guinea pigs by EP to provide reference basis for clinical applications of such transdermal delivery system in the treatment of pa...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2016.1267275

    authors: Chen S,Han Y,Yu D,Huo F,Wang F,Li Y,Dong L,Liu Z,Huang H

    更新日期:2017-11-01 00:00:00

  • Pharmacokinetics and anti-hypertensive effect of metoprolol tartrate rectal delivery system.

    abstract::The main aim of this work was to develop rectal suppositories for better delivery of metoprolol tartrate (MT). The various bases used were fatty, water soluble and emulsion bases. The physical properties of the prepared suppositories were characterized such as weight variation, hardness, disintegration time, melting r...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2014.904021

    authors: Abou el Ela Ael S,Allam AA,Ibrahim EH

    更新日期:2016-01-01 00:00:00

  • Drug delivery devices based on mesoporous silicate.

    abstract::A mesoporous material based on aluminosilicate mixture was studied to investigate its ability to include drugs and then release them. Nonsteroidal anti-inflammatory agents such as diflunisal, naproxen, ibuprofen and its sodium salt have been used in this study. The preparation of the mesoporous material and its charac...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717540490265252

    authors: Cavallaro G,Pierro P,Palumbo FS,Testa F,Pasqua L,Aiello R

    更新日期:2004-01-01 00:00:00

  • Laser-assisted delivery enhances topical uptake of the anticancer agent cisplatin.

    abstract::Systemic chemotherapy with the anticancer agent cisplatin is approved for advanced non-melanoma skin cancer (NMSC), but topical treatment is limited by insufficient cutaneous penetration. We studied the impact of ablative fractional laser (AFL) exposure on topical cisplatin's pharmacokinetics and biodistribution in sk...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2018.1534896

    authors: Wenande E,Olesen UH,Boesen MR,Persson DP,Lerche CM,Stürup S,Gammelgaard B,Husted S,Anderson RR,Haedersdal M

    更新日期:2018-11-01 00:00:00

  • Extension of nasal anti-Staphylococcus aureus efficacy of lysostaphin by its incorporation into a chitosan-o/w cream.

    abstract::Nasal colonization of Staphylococcus aureus (S.aureus) is known as a significant risk factor for nosocomial infections, and clearance of its nasal colonization greatly reduces the risk. In the present study the preparation and characterizations of the chitosan-o/w cream incorporated with lysostaphin (CCL) were describ...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717544.2010.509360

    authors: Cui F,Li G,Huang J,Zhang J,Lu M,Lu W,Huang Q

    更新日期:2010-11-01 00:00:00

  • Anti-tumor effect of local injectable hydrogel-loaded endostatin alone and in combination with radiotherapy for lung cancer.

    abstract::Endostatin (ES) can effectively inhibit neovascularization in most solid tumors and has the potential to make oxygen delivery more efficient and increase the efficacy of radiotherapy (RT). With a short half-life, ES is mainly administered systemically, which leads to low intake in tumor tissue and often toxic systemic...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2020.1869864

    authors: Wang N,Gao Q,Tang J,Jiang Y,Yang L,Shi X,Chen Y,Zhang Y,Fu S,Lin S

    更新日期:2021-12-01 00:00:00

  • Etoposide-loaded biodegradable amphiphilic methoxy (poly ethylene glycol) and poly (epsilon caprolactone) copolymeric micelles as drug delivery vehicle for cancer therapy.

    abstract::Amphiphilic diblock copolymers composed of methoxy poly ethylene glycol (MePEG) and poly epsilon caprolactone (PCL) were synthesized for the formation of micelles by ring opening mechanism using stannous octoate as a catalyst. The effects of the molecular weight of MePEG and the copolymer ratio on the properties of mi...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.3109/10717541003720688

    authors: Mohanty AK,Dilnawaz F,Mohanty C,Sahoo SK

    更新日期:2010-07-01 00:00:00

  • Cetuximab-modified silica nanoparticle loaded with ICG for tumor-targeted combinational therapy of breast cancer.

    abstract::Combinational therapy is usually considered as a preferable approach for effective cancer therapy. Especially, combinational chemo and photothermal therapy is of particular interest due to its high flexibility as well as efficiency. In this article, we the silica nanoparticles (SLN) were surface conjugated with Cetuxi...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717544.2018.1564403

    authors: Zhang X,Li Y,Wei M,Liu C,Yu T,Yang J

    更新日期:2019-12-01 00:00:00

  • Gentamicin release from photopolymerized PEG diacrylate and pHEMA hydrogel discs and their in vitro antimicrobial activities.

    abstract::Hydrogels based on poly(ethylene glycol)-diacrylate (PEG-DA) and 2-hydroxyethyl methacrylate (HEMA) were polymerized with cross-linking agent ethylene glycol diacrylate (EGDMA) under mild photoinitiating conditions. PEG-DA and HEMA concentrations of disks with 1 +/- 0.3 mm thickness were 30% and 50% w/w and 40% and 60...

    journal_title:Drug delivery

    pub_type: 杂志文章

    doi:10.1080/10717540701202911

    authors: Ayhan F,Ozkan S

    更新日期:2007-10-01 00:00:00