What is a Suitable Dissolution Method for Drug Nanoparticles?

Heng, Desmond; Cutler, David J.; Chan, Hak‐Kim; Yun, Jimmy; Raper, Judy A

doi:10.1007/s11095-008-9560-0

Cited by 105 publications

(86 citation statements)

References 37 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…This dissolution technique has been proven to be reproducible and robust, which is an important characteristic for dissolution testing (27)(28)(29). The increased sensitivity of the flow-through cell dissolution method related to particle size of a poorly soluble drug powder has also been reported recently (30,31). In the work by Heng et al (31), the paddle, rotating basket, and flow-through cell from the USP, and a dialysis method, were used to measure the dissolution rates of cefuroxime axetil as a model for drug nanoparticles.…”

Section: Introductionmentioning

confidence: 94%

“…Although the use of the USP 1, USP 2 and USP 4 for conventional solid dosage forms have been presented before (19)(20)(21)(22)(23)(24)(25)(26), there is usually a lack of standard regulatory tests for new solid dosage forms, which represents a major obstacle in their development (31). One of these new solid dosage forms, pharmaceutical strip-film products, has received much attention because of several advantages including rapid disintegration and dissolution in the oral cavity and increased bioavailability (32)(33)(34)(35).…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Using USP I and USP IV for Discriminating Dissolution Rates of Nano- and Microparticle-Loaded Pharmaceutical Strip-Films

et al. 2012

View full text Add to dashboard Cite

Abstract. Recent interest in the development of drug particle-laden strip-films suggests the need for establishing standard regulatory tests for their dissolution. In this work, we consider the dissolution testing of griseofulvin (GF) particles, a poorly water-soluble compound, incorporated into a strip-film dosage form. The basket apparatus (USP I) and the flow-through cell dissolution apparatus (USP IV) were employed using 0.54% sodium dodecyl sulfate as the dissolution medium as per USP standard. Different rotational speeds and dissolution volumes were tested for the basket method while different cell patterns/ strip-film position and dissolution media flow rate were tested using the flow-through cell dissolution method. The USP I was not able to discriminate dissolution of GF particles with respect to particle size. On the other hand, in the USP IV, GF nanoparticles incorporated in strip-films exhibited enhancement in dissolution rates and dissolution extent compared with GF microparticles incorporated in strip-films. Within the range of patterns and flow rates used, the optimal discrimination behavior was obtained when the strip-film was layered between glass beads and a flow rate of 16 ml/min was used. These results demonstrate the superior discriminatory power of the USP IV and suggest that it could be employed as a testing device in the development of strip-films containing drug nanoparticles.

show abstract

Section: Introductionmentioning

confidence: 94%

Section: Introductionmentioning

confidence: 99%

Using USP I and USP IV for Discriminating Dissolution Rates of Nano- and Microparticle-Loaded Pharmaceutical Strip-Films

et al. 2012

View full text Add to dashboard Cite

show abstract

“…At present, there is a tendency to use such apparatuses more frequently. For example, when conducting the test "Dissolution" in flow-through devices with nanopowders of the relatively insoluble medicines, the issues of worsening in wettability and adhesion of nanoparticles are removed [6].…”

Section: Literature Review and Problem Statementmentioning

confidence: 99%

Development of a bootstrap-model for determining the release of medicinal preparations in the human organism

Chorny¹,

Savyak²,

Kondratov

2017

EEJET

View full text Add to dashboard Cite

“…16 In drug delivery, nanoparticulated systems are preferred over micro-sized particles, owing to their smaller size and larger surface area, which improve dissolution rate, absorption, and bioavailability. 17 Pharmaceutical nanoparticulated systems can be developed using a variety of techniques, such as solvent evaporation, emulsification, spray drying, phase inversion, self-assembly, and solvent displacement. 18,19 Spray drying is one of the most frequently employed techniques in the preparation of a dry powder from a liquid phase, 20 because of the simple operation, good yield, and the fact that it is easy to scale up.…”

Section: Introductionmentioning

confidence: 99%

Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation

Yousaf¹,

Kim²,

Oh³

et al. 2015

IJN

View full text Add to dashboard Cite

Background The intention of this research was to prepare and compare various solubility-enhancing nanoparticulated systems in order to select a nanoparticulated formulation with the most improved oral bioavailability of poorly water-soluble fenofibrate. Methods The most appropriate excipients for different nanoparticulated preparations were selected by determining the drug solubility in 1% (w/v) aqueous solutions of each carrier. The polyvinylpyrrolidone (PVP) nanospheres, hydroxypropyl-β-cyclodextrin (HP-β-CD) nanocorpuscles, and gelatin nanocapsules were formulated as fenofibrate/PVP/sodium lauryl sulfate (SLS), fenofibrate/HP-β-CD, and fenofibrate/gelatin at the optimized weight ratios of 2.5:4.5:1, 1:4, and 1:8, respectively. The three solid-state products were achieved using the solvent-evaporation method through the spray-drying technique. The physicochemical characterization of these nanoparticles was accomplished by powder X-ray diffraction, differential scanning calorimetry, scanning electron microscopy, and Fourier-transform infrared spectroscopy. Their physicochemical properties, aqueous solubility, dissolution rate, and pharmacokinetics in rats were investigated in comparison with the drug powder. Results Among the tested carriers, PVP, HP-β-CD, gelatin, and SLS showed better solubility and were selected as the most appropriate constituents for various nanoparticulated systems. All of the formulations significantly improved the aqueous solubility, dissolution rate, and oral bioavailability of fenofibrate compared to the drug powder. The drug was present in the amorphous form in HP-β-CD nanocorpuscles; however, in other formulations, it existed in the crystalline state with a reduced intensity. The aqueous solubility and dissolution rates of the nanoparticles (after 30 minutes) were not significantly different from one another. Among the nanoparticulated systems tested in this study, the initial dissolution rates (up to 10 minutes) were higher with the PVP nanospheres and HP-β-CD nanocorpuscles; however, neither of them resulted in the highest oral bioavailability. Irrespective of relatively retarded dissolution rate, gelatin nanocapsules showed the highest apparent aqueous solubility and furnished the most improved oral bioavailability of the drug (~5.5-fold), owing to better wetting and diminution in crystallinity. Conclusion Fenofibrate-loaded gelatin nanocapsules prepared using the solvent-evaporation method through the spray-drying technique could be a potential oral pharmaceutical product for administering the poorly water-soluble fenofibrate with an enhanced bioavailability.

show abstract

What is a Suitable Dissolution Method for Drug Nanoparticles?

Cited by 105 publications

References 37 publications

Using USP I and USP IV for Discriminating Dissolution Rates of Nano- and Microparticle-Loaded Pharmaceutical Strip-Films

Using USP I and USP IV for Discriminating Dissolution Rates of Nano- and Microparticle-Loaded Pharmaceutical Strip-Films

Development of a bootstrap-model for determining the release of medicinal preparations in the human organism

Enhanced oral bioavailability of fenofibrate using polymeric nanoparticulated systems: physicochemical characterization and in vivo investigation

Contact Info

Product

Resources

About