Delivery of Itraconazole from Extruded HPC Films

Trey, Stacy; Wicks, Douglas A.; Mididoddi, Praveen K.; Repka, Michael A.

doi:10.1080/03639040701199225

Cited by 33 publications

(11 citation statements)

References 8 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…The structure of the HpC film may be effective in slowing the release. The release of water-insoluble drugs from HpC films was examined by different study groups and the release profile was shown to be completed within approximately 10 h [71–73]. In another study regarding the release of paclitaxel (which is another member of taxane class, such as docetaxel, released from nanocomposite film) the initial release was observed within 7 h due to the rapid release of drugs from surface of the film [74].…”

Section: Resultsmentioning

confidence: 99%

Cationic PEGylated polycaprolactone nanoparticles carrying post-operation docetaxel for glioma treatment

Varan¹,

Bilensoy²

2017

Beilstein J. Nanotechnol.

View full text Add to dashboard Cite

Background: Brain tumors are the most common tumors among adolescents. Although some chemotherapeutics are known to be effective against brain tumors based on cell culture studies, the same effect is not observed in clinical trials. For this reason, the development of drug delivery systems is important to treat brain tumors and prevent tumor recurrence. The aim of this study was to develop core–shell polymeric nanoparticles with positive charge by employing a chitosan coating. Additionally, an implantable formulation for the chemotherapeutic nanoparticles was developed as a bioadhesive film to be applied at the tumor site following surgical operation for brain glioma treatment. To obtain positively charged, implantable nanoparticles, the effects of preparation technique, chitosan coating concentration and presence of surfactants were evaluated to obtain optimal nanoparticles with a diameter of less than 100 nm and a net positive surface charge to facilitate cellular internalization of drug-loaded nanoparticles. Hydroxypropyl cellulose films were prepared to incorporate these nanoparticle dispersions to complete the implantable drug delivery system. Results: The diameter of core–shell nanoparticles were in the range of 70–270 nm, depending on the preparation technique, polymer type and coating. Moreover, the chitosan coating significantly altered the surface charge of the nanoparticles to net positive values of +30 to +50 mV. The model drug docetaxel was successfully loaded into all particles, and the drug release rate from the nanoparticles was slowed down to 48 h by dispersing the nanoparticles in a hydroxypropyl cellulose film. Cell culture studies revealed that docetaxel-loaded nanoparticles cause higher cytotoxicity compared to the free docetaxel solution in DMSO. Conclusion: Docetaxel-loaded nanoparticles dispersed in a bioadhesive film were shown to be suitable for application of chemotherapeutics directly to the action site during surgical operation. The system was found to release chemotherapeutics for several days at the tumor site and neighboring tissue. This can be suggested to result in a more effective brain tumor treatment when compared to chemotherapeutics administered as an intravenous bolus infusion.

show abstract

Section: Resultsmentioning

confidence: 99%

Cationic PEGylated polycaprolactone nanoparticles carrying post-operation docetaxel for glioma treatment

Varan¹,

Bilensoy²

2017

Beilstein J. Nanotechnol.

View full text Add to dashboard Cite

show abstract

“…It is hypothesized that the pH-independent solubility along with tunable density of functional groups of PVAL would be ideal in the creation of solid dispersions especially for weakly basic drugs. While other groups have shown stability with semicrystalline polymers, PVAL will also need to be investigated to establish that the polymer crystalline structure does not create nucleation sites for drug recrystallization during processing and storage (49). As a first step in investigating that PVAL will function as a solubility-enhancing polymer, ITZ was selected as the model drug to be formulated in various grades.…”

Section: Introductionmentioning

confidence: 99%

Use of Polyvinyl Alcohol as a Solubility-Enhancing Polymer for Poorly Water Soluble Drug Delivery (Part 1)

Brough

Miller²,

Keen³

et al. 2015

AAPS PharmSciTech

View full text Add to dashboard Cite

Abstract. Polyvinyl alcohol (PVAL) has not been investigated in a binary formulation as a concentrationenhancing polymer owing to its high melting point/high viscosity and poor organic solubility. Due to the unique attributes of the KinetiSol® dispersing (KSD) technology, PVAL has been enabled for this application and it is the aim of this paper to investigate various grades for improvement of the solubility and bioavailability of poorly water soluble active pharmaceutical ingredients. Solid amorphous dispersions were created with the model drug, itraconazole (ITZ), at a selected drug loading of 20%. Polymer grades were chosen with variation in molecular weight and degree of hydroxylation to determine the effects on performance. Differential scanning calorimetry, powder X-ray diffraction, polarized light microscopy, size exclusion chromatography, and dissolution testing were used to characterize the amorphous dispersions. An in vivo pharmacokinetic study in rats was also conducted to compare the selected formulation to current market formulations of ITZ. The 4-88 grade of PVAL was determined to be effective at enhancing solubility and bioavailability of itraconazole.

show abstract

“…These molds yield the classic tablet, capsule shapes, or custom-designed shapes to suit various applications such as denture adhesives, vaginal rings, ear inserts, or pediatric friendly (enhance the esthetic appeal of the product) designs. Some of the dosage forms (made with melt extruded material) that have been previously characterized are films (Repka and McGinity 2001;Trey et al 2007), pellets, spherical pellets (Young et al 2002), punched tablets (Fukuda et al 2006), injection-molded tablets (Quinten et al 2009), rods, and granules (Robinson and Mcginity 2000) .…”

Section: Melting and Mixingmentioning

confidence: 99%

Melt Extrusion in Drug Delivery: Three Decades of Progress

Shah

Repka

2013

AAPS Advances in the Pharmaceutical Sciences Series

Self Cite

View full text Add to dashboard Cite

This chapter appraises the role of melt extrusion as a solubilization and bioavailability enhancement technique. The introductory chapter highlights major aspects of hot melt extrusion (HME) technology as applied in the pharmaceutical industry, particularly processing techniques, material considerations, recent innovative applications of melt extrusion in drug delivery system design, and a review of current HME-based formulations (marketed or under commercial development). The chapter also focuses on key development aspects of HME processes, such as material sparing screening approaches, process formulation relationships, and stability evaluation of prototype formulations, which emphasize the clinical and biological significance of this technique. In addition, it displays the journey and evolution of this important processing technology into an established pharmaceutical manufacturing platform. The chapter describes several case studies wherein melt extrusion has been utilized to develop commercial drug products.Early-stage development in melt extrusion encompasses various critically interdependent areas involving process considerations, stability assessment of prototype formulations, and performance evaluation (with respect to intended applications) of prototype formulations. Processing ConsiderationsProcessing considerations is a rather broad terminology covering material properties, instrument considerations, and process-formulation interplay. Systematic research over the last couple of decades has revealed that critical product quality attributes are directly dependent on both "formulation" and the "process" employed. It is important to note that the interplay between these determines the finished product attributes. Material PropertiesAll of the materials used in melt extrusion (drugs, carriers, processing aids, release modifiers, etc.) should meet certain minimal pharmaceutical criteria, which

show abstract

Delivery of Itraconazole from Extruded HPC Films

Cited by 33 publications

References 8 publications

Cationic PEGylated polycaprolactone nanoparticles carrying post-operation docetaxel for glioma treatment

Cationic PEGylated polycaprolactone nanoparticles carrying post-operation docetaxel for glioma treatment

Use of Polyvinyl Alcohol as a Solubility-Enhancing Polymer for Poorly Water Soluble Drug Delivery (Part 1)

Melt Extrusion in Drug Delivery: Three Decades of Progress

Contact Info

Product

Resources

About