Bioavailability enhancement of a COX-2 inhibitor, BMS-347070, from a nanocrystalline dispersion prepared by spray-drying

Yin, Shawn; Franchini, Miriam; Chen, Jinling; Hsieh, Alice; Jen, Sandy; Lee, Tu; Hussain, Munir; Smith, Ronald L.

doi:10.1002/jps.20366

Cited by 60 publications

(39 citation statements)

References 27 publications

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“…Sonication was required for effective reconstitution of the primary particles. Yin et al (12) described spray drying of poorly soluble drugs, wherein the drug was in a dissolved form prior to spray drying, but formed nanocrystalline domains after spray drying. In this study, Poloxamers were used during spray drying, to form a matrix to encapsulate the nanocrystalline drug domains.…”

Section: Introductionmentioning

confidence: 99%

Conversion of Nanosuspensions into Dry Powders by Spray Drying: A Case Study

2008

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Purpose. Drying of nanosuspensions can cause destabilization of the particles, leading to irreversible aggregation. In order to prepare an effective solid dosage form for a nanosuspension, it is imperative that the spray-dried nanoparticles should go back to their original particle size when reconstituted in an aqueous system. This case study examines impact of various formulation and processing parameters on redispersibility of the spray dried nanoparticles. Methods. Nanosuspensions were prepared using the microprecipitation-homogenization process. Spray drying of nanosuspensions was achieved using a lab-scale Buchi spray dryer.Results. Formulation components appeared to have the most significant impact on redispersibility of spray dried particles. Absence of surface charge led to particles that could not be redispersed. On the other hand, charged particles stabilized with an appropriate sugar led to spray dried powders that were flowable and easily redispersible. Dissolution testing showed the presence of two phases-a lag phase that represented dispersion of the loose aggregates, and dissolution of the dispersed nanoparticles. Conclusions. Nanosuspensions of a poorly soluble drug could be spray dried to obtain flowable powders that could be easily redispersed. These optimized powders also showed significantly improved dissolution rates as compared to the micronized drug, or unoptimized nanosuspensions.

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Section: Introductionmentioning

confidence: 99%

Conversion of Nanosuspensions into Dry Powders by Spray Drying: A Case Study

2008

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“…This increased bioavailability (Kondo et al 1993a, b;Liversidge and Conzentino 1995;Liversidge and Cundy 1995;Yin et al 2005;Kesisoglou et al 2007) occurs primarily due to increased dissolution velocity (Vergote et al 2001;Hu et al 2002;Rasenack and Muller 2002;Kayser et al 2003;Hecq et al 2005Hecq et al , 2006Jinno et al 2006;Kocbek et al 2006;Zhang et al 2007), but can also be a result of increased permeability (Jia et al 2002) and enhanced particulate uptake (Desai et al 1996). For example, nanocrystalline cilostazol, a BCS Class II drug with an aqueous solubility of 3 mg/mL at 25°C and a median particle size of 220 nm, dissolved immediately in water.…”

Section: Biopharmaceutical Benefits Of Nanosuspensionsmentioning

confidence: 96%

“…Usually the particle size obtained by spray drying lies in the micrometer range. However, Yin et al (2005) reported the preparation of nanocrystalline dispersions of a research compound BMS-347070 with Pluronic F-127. On the basis of the broadening of peaks in powder X-Ray diffraction, the particle size of the spray dried material was determined to be in the range of 40-60 nm.…”

Section: Spray Dryingmentioning

confidence: 97%

“…In addition, nanosuspensions can be administered via all major routes, such as oral (Liversidge and Conzentino 1995;Liversidge and Cundy 1995;Vergote et al 2001;Kayser et al 2003;White et al 2003;Yin et al 2005), intramuscular, intravenous (Scholer et al 2001;Moschwitzer et al 2004), intraocular, and pulmonary .…”

Section: Applicationsmentioning

confidence: 99%

“…A direct consequence of the increase in saturation solubility and fast dissolution rates of pharmaceutical nanoparticles is their improved pharmacokinetics in terms of: increased rate and extent of absorption; rapid onset of action (Yin et al 2005;Jinno et al 2006); reduced variations in fed and fasted state (Wu et al 2004); reduced gastric irritancy (Liversidge and Conzentino 1995); and better clinical efficacy (Kayser et al 2003).…”

Section: Superior Clinical Performancementioning

confidence: 99%

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Solid Nanosuspensions: The Emerging Technology and Pharmaceutical Applications as Nanomedicine

Verma

Burgess

2009

Pharmaceutical Suspensions

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One of the foremost reasons for such a widespread interest in nanosuspensions as drug delivery systems is their ability to provide formulations of poorly soluble drugs with increased saturation solubility and higher dissolution rates. Nanosuspensions manifest these properties because of their small size and high surface area. The unique properties of the nanosuspensions along with their fast development times, low production costs, ease of manufacture and scale-up as well as their ability to extend the lifecycle of off-patent drugs have resulted in rapid commercialization. Nanosuspensions provide us with a useful tool for formulating an ever-increasing number of poorly water soluble drugs in pharmaceutical development programs.

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Combinatorial Screening

2009

Two‐Dimensional X‐Ray Diffraction

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Bioavailability enhancement of a COX-2 inhibitor, BMS-347070, from a nanocrystalline dispersion prepared by spray-drying

Cited by 60 publications

References 27 publications

Conversion of Nanosuspensions into Dry Powders by Spray Drying: A Case Study

Conversion of Nanosuspensions into Dry Powders by Spray Drying: A Case Study

Solid Nanosuspensions: The Emerging Technology and Pharmaceutical Applications as Nanomedicine

Combinatorial Screening

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