Bexarotene nanocrystal—Oral and parenteral formulation development, characterization and pharmacokinetic evaluation

Chen, Lijiang; Wang, Yongjie; Zhang, Jiaozhen; Hao, Leilei; Guo, Hejian; Lou, Hongxiang; Zhang, Dianrui

doi:10.1016/j.ejpb.2013.12.005

Cited by 70 publications

(43 citation statements)

References 52 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…These studies used a very different drug formulation in their treatments, in which bexarotene was administered solubilized in DMSO (or in a cyclodextrin vehicle) rather than as the clinical formulation (TargretinTM) as micronized crystals used by Cramer et al (Cramer et al, 2012). New work has compared these preparations and shown that they yield very different pharmacodynamics and overall drug exposure (Chen et al, 2013). …”

Section: Reproducibility Of Nuclear Receptor Effects In Mouse Models mentioning

confidence: 99%

Nuclear receptors in neurodegenerative diseases

Skerrett

Malm

Landreth

2014

Neurobiology of Disease

101

View full text Add to dashboard Cite

Nuclear receptors have generated substantial interest in the past decade as potential therapeutic targets for the treatment of neurodegenerative disorders. Despite years of effort, effective treatments for progressive neurodegenerative diseases such as Alzheimer’s disease, Parkinson’s disease, Huntington’s disease and ALS remain elusive, making non-classical drug targets such as nuclear receptors an attractive alternative. A substantial literature in mouse models of disease and several clinical trials have investigated the role of nuclear receptors in various neurodegenerative disorders, most prominently AD. These studies have met with mixed results, yet the majority of studies in mouse models report positive outcomes. The mechanisms by which nuclear receptor agonists affect disease pathology remain unclear. Deciphering the complex signaling underlying nuclear receptor action in neurodegenerative diseases is essential for understanding this variability in preclinical studies, and for the successful translation of nuclear receptor agonists into clinical therapies.

show abstract

Section: Reproducibility Of Nuclear Receptor Effects In Mouse Models mentioning

confidence: 99%

Nuclear receptors in neurodegenerative diseases

Skerrett

Malm

Landreth

2014

Neurobiology of Disease

101

View full text Add to dashboard Cite

show abstract

“…The poly(methacrylic acid and methacrylate) copolymer allows release of load at a specific pH within the gastrointestinal tract. Table 6, 99, 100, 101, 102, 103, 104, 105, 106, 107, 108, 109, 110, 111, 112, 113, 114, 115, 116, 117, 118, 119, 120, 121, 122, 123, 124, 125, 126, 127, 128, 129, 130, 131, 132, 133, 134, 135, 136, 137, 138, 139, 140, 141, 142, 143, 144, 145, 146, 147 reveals a few examples of nanoparticulate systems which improve bioavailability.…”

Section: Formulation Approaches For Manipulating Solubility and Permementioning

confidence: 99%

“…Solubility and PAMPA assay in agreement with in vivo kinetic studies.103pMMA coated thiolated chitosan nanoparticleRadical polymerizationDocetaxelIITenfold increase in oral bioavailability of nanoparticle formulation may be attributed to mucoadhesion, P-gp efflux inhibition and permeability enhancement effect of thiolated chitosan.104PEG- b -PLA nanoparticleFlash nanoprecipitationDoxorubicinIIIOverexpression of P-gp in MDR cell contribute low cellular accumulation. Self-assembled PEG- b -PLA nanoparticle demonstrated higher retention in MDR cell and passive targeting to tumor cell.105NanocrystalCombination technology (antisolvent precipitation and microfluidization)BexaroteneIINanocrystal formulation optimized using L9 orthogonal array stabilized using lecithin and poloxamer 188 for oral and parenteral delivery.106NanocrystalAntisolvent precipitationCarvedilolIISDS stabilized nanosuspension demonstrated increased C max and AUC while decrease in T max when compared with coarse suspension.107NanocrystalWet media MillingFebuxostatIIHPMC and vitamin E TPGS stabilized system with 221.6% increase in relative bioavailability.108NanocrystalPrecipitation-high pressure homogenization methodNitrendipineIISurface modified chitosan nanocrystal stabilized with polyvinyl alcohol (PVA) has better stability and bioavailability compared with unmodified crystals.109NanocrystalWet-milling technologyTranilastIIHydroxy propyl cellulose-SL and SDS stabilized redispersible system exhibited improvement in the dissolution behavior under acidic conditions and enhancing the therapeutic potential of tranilast to treat liver dysfunction.110Solid nanodispersionDry media millingIngliforib, celecoxib furosemideII, IVNovel formulation approach combining two technologies, i.e .,solid dispersion and nanocrystal, and stabilized with PVP K12 and SDS.111Solid dispersionSpray drying techniqueTacrolimusIIThe formulation containing drug–Eudragit E exhibited higher drug solubility as it inhibits reprecipitation in neutral pH condition.112Solid dispersionLyophillization techniqueAtorvastatinIISolid dispersion formulation containing skimmed milk as a carrier in varying ratio has shown 33 fold increase in sol...…”

Section: Formulation Approaches For Manipulating Solubility and Permementioning

confidence: 99%

Understanding peroral absorption: regulatory aspects and contemporary approaches to tackling solubility and permeability hurdles

Shekhawat

Pokharkar

2017

Acta Pharmaceutica Sinica B

130

View full text Add to dashboard Cite

Oral drug absorption is a process influenced by the physicochemical and biopharmaceutical properties of the drug and its inter-relationship with the gastrointestinal tract. Drug solubility, dissolution and permeability across intestinal barrier are the key parameters controlling absorption. This review provides an overview of the factors that affect drug absorption and the classification of a drug on the basis of solubility and permeability. The biopharmaceutical classification system (BCS) was introduced in early 90׳s and is a regulatory tool used to predict bioavailability problems associated with a new entity, thereby helping in the development of a drug product. Strategies to combat solubility and permeability issues are also discussed.

show abstract

“…The enhanced dissolution and drug release of 10-HCPT nanocrystals were mainly attributed to their higher surface area, increased surface solubility, and reduced diffusion layer thickness. 26 …”

Section: In Vitro Release Studymentioning

confidence: 99%

A stabilizer-free and organic solvent-free method to prepare 10-hydroxycamptothecin nanocrystals: in vitro and in vivo evaluation

Yang¹,

Liu²,

Zhao³

et al. 2016

IJN

View full text Add to dashboard Cite

10-Hydroxycamptothecin (10-HCPT) is a promising anticancer drug with a wide spectrum of antitumor activities. Due to its poor solubility, the carboxylate form that shows high water solubility but minimal anticancer activity and pharmacokinetic defects is used in the marketed 10-HCPT injections, resulting in its limited clinical application. To develop a simple, safe, and highly effective drug delivery system, a modified acid–base microprecipitation combined with a high-pressure homogenization technique was adopted to prepare 10-HCPT nanocrystals. Neither organic solvents nor stabilizers were employed throughout the preparation process. The in vitro and in vivo performances of the resulting10-HCPT nanocrystals were investigated systematically. The nanocrystals were spherical with a small size of ~130 nm, and the actual drug-loading content was as high as 75%. The nanocrystals displayed a sustained release pattern and were proven to have a higher cell uptake and antiproliferative activity than the 10-HCPT injections. The 10-HCPT nanocrystals also showed enhanced drug accumulation in tumors and better anticancer efficacy in 4T1-bearing mice. In summary, the 10-HCPT nanocrystals prepared in this study seem to be a promising delivery system for a new form of 10-HCPT dosages.

show abstract

Bexarotene nanocrystal—Oral and parenteral formulation development, characterization and pharmacokinetic evaluation

Cited by 70 publications

References 52 publications

Nuclear receptors in neurodegenerative diseases

Nuclear receptors in neurodegenerative diseases

Understanding peroral absorption: regulatory aspects and contemporary approaches to tackling solubility and permeability hurdles

A stabilizer-free and organic solvent-free method to prepare 10-hydroxycamptothecin nanocrystals: in vitro and in vivo evaluation

Contact Info

Product

Resources

About