Particle size reduction for improvement of oral bioavailability of hydrophobic drugs: I. Absolute oral bioavailability of nanocrystalline danazol in beagle dogs

Liversidge, Gary G.; Cundy, Kenneth C.

doi:10.1016/0378-5173(95)00122-y

Cited by 644 publications

(330 citation statements)

References 7 publications

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“…To overcome this limitation, these compounds have to be further processed, and in most cases their particle size is reduced (3)(4)(5)(6)(7). As per the Noyes-Whitey equation, formation of finer drug particles leads to an increase in dissolution rate, which can be related to an increase in the drug bioavailability (8).…”

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

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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.

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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

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“…Nanoparticles have to date been extensively used for various applications including drug delivery (Liversidge and Cundy, 1995;Duncan, 2005), tissue engineering (Langer, 2000) and imaging (Bruchez, 2005). Their physiochemical properties including their small size and large surface area have led to these advances.…”

Section: Introductionmentioning

confidence: 99%

In vivo uptake and acute immune response to orally administered chitosan and PEG coated PLGA nanoparticles

Semete

Booysen

Kalombo

et al. 2010

Toxicology and Applied Pharmacology

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a b s t r a c t a r t i c l e i n f oNanoparticulate drug delivery systems offer great promise in addressing challenges of drug toxicity, poor bioavailability and non-specificity for a number of drugs. Much progress has been reported for nano drug delivery systems for intravenous administration, however very little is known about the effects of orally administered nanoparticles. Furthermore, the development of nanoparticulate systems necessitates a thorough understanding of the biological response post exposure. This study aimed to elucidate the in vivo uptake of chitosan and polyethylene glycol (PEG) coated Poly, DL, lactic-co-glycolic Acid (PLGA) nanoparticles and the immunological response within 24 h of oral and peritoneal administration. These PLGA nanoparticles were administered orally and peritoneally to female Balb/C mice, they were taken up by macrophages of the peritoneum. When these particles were fluorescently labelled, intracellular localisation was observed. The expression of pro-inflammatory cytokines IL-2, IL-6, IL-12p70 and TNF-α in plasma and peritoneal lavage was found to remain at low concentration in PLGA nanoparticles treated mice as well as ZnO nanoparticles during the 24 hour period. However, these were significantly increased in lipopolysaccharide (LPS) treated mice. Of these pro-inflammatory cytokines, IL-6 and IL-12p70 were produced at the highest concentration in the positive control group. The anti-inflammatory cytokines IL-10 and chemokines INF-γ, IL-4, IL-5 remained at normal levels in PLGA treated mice. IL-10 and INF-γ were significantly increased in LPS treated mice. MCP-1 was found to be significantly produced in all groups in the first hours, except the saline treated mice. These results provide the first report to detail the induction of cytokine production by PLGA nanoparticles engineered for oral applications.

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“…The value, utility and commercial viability of this approach for compounds with a low aqueous solubility has been demonstrated in recent years (Liversidge et al, 1995;Muller, 2001;Merisko-Liversidge et al, 2003;Pathak et al, 2005;Keck, Muller, 2006;Overhoff et al 2007;Pu et al, 2009;Timpe, 2010). In addition, this approach has received significant attention, as reflected in the number of publications and reviews that have appeared recently (Hauss, 2007;Tang et al, 2008).…”

Section: Introductionmentioning

confidence: 99%

Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs

Wadhwa¹,

Nair²,

Kumria³

2011

Braz. J. Pharm. Sci.

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Self-emulsifying therapeutic system (SETs) provide an effective and intelligent solution to the various issues related to the formulation of hydrophobic drugs with limited solubility in gastrointestinal fluid. Although the potential utility of SETs is well known, only in recent years has a mechanistic understanding of the impact of these systems on drug disposition emerged. These in situ emulsion-forming systems have a high stability when incorporated in various dosage forms. SETs are being looked upon as systems which can overcome the problems associated with delivery of poorly water soluble drugs. An in-depth knowledge about lipids and surfactants that can contribute to these systems, criterion for their selection and the proportion in which they can be used, represent some crucial factors determining the in vivo performance of these systems. This article presents a comprehensive account of various types of self-emulsifying formulations with emphasis on their composition and examples of currently marketed preparations.Uniterms: Lipid based formulations. Self-emulsifying therapeutic system. Self-emulsification.O sistema terapêutico auto-emulsionante (SETs) fornece solução eficaz e inteligente para os vários problemas relativos à formulação de fármacos hidrofóbicos com solubilidade limitada no fluido gastrintestinal. Embora a utilidade potencial dos SETs seja bem conhecida, só recentemente se compreendeu, mecanisticamente,o impacto desses sistemas na disposição de fármacos. Estes sistemas de formação de emulsão in situ têm alta estabilidade, quando incorporados em várias formas de dosagem. Os SETs têm sido considerados como sistemas que podem resolver problemas associados à liberação de fármacos pouco solúveis em água. O conhecimento profundo dos lipídios e tensoativos que podem ser utilizados para estes sistemas e o critério para a sua seleção e proporção na qual eles são utilizados são alguns dos fatores cruciais que determinam o desempenho do sistema in vivo. Este artigo apresenta o relato abrangente de vários tipos de formulações auto-emulsificantes, com ênfase em sua composição e exemplos das preparações que são correntemente comercializadas.Unitermos: Formulações baseadas em lipídio. Sistema terapêutico auto-emulsificante. Autoemulsificação.

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Particle size reduction for improvement of oral bioavailability of hydrophobic drugs: I. Absolute oral bioavailability of nanocrystalline danazol in beagle dogs

Cited by 644 publications

References 7 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

In vivo uptake and acute immune response to orally administered chitosan and PEG coated PLGA nanoparticles

Self-emulsifying therapeutic system: a potential approach for delivery of lipophilic drugs

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