Solubilizing Excipients in Oral and Injectable Formulations

Strickley, Robert G.

doi:10.1023/b:pham.0000016235.32639.23

Cited by 1,238 publications

(722 citation statements)

References 32 publications

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“…Over the years, different strategies have been developed to overcome poor solubility issues. This includes micronization and nanonization, particle engineering, amorphisation, solid dispersion, salts formation, the use of surfactant "micellization", cyclodextrins and polymeric complexations (Cavallari et al, 2005;Chen et al, 2011;Del Valle, 2004;Junghanns and Müller, 2008;Owen, 2013;Strickley, 2004). Nevertheless, these strategies are not always able to satisfactorily improve the drug solubility and the combination of more than one strategy may be required.…”

Section: Introductionmentioning

confidence: 99%

Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin

Khoder

Abdelkader

ElShaer

et al. 2016

International Journal of Pharmaceutics

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Please cite this article as: Khoder, Mouhamad, Abdelkader, Hamdy, ElShaer, Amr, Karam, Ayman, Najlah, Mohammad, Alany, Raid G., Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin.International Journal of Pharmaceutics http://dx.doi.org/10. 1016/j.ijpharm.2016.11.019 This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.

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Section: Introductionmentioning

confidence: 99%

Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin

Khoder

Abdelkader

ElShaer

et al. 2016

International Journal of Pharmaceutics

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“…Likewise, each of the emulsifiers represents different classes of structures. However, all components listed in Table 1 are already used in commercially available oral or injectable pharmaceutical products 7 , 8 , Table 2. defines the composition of each emulsion manufactured along with physical properties.…”

Section: Resultsmentioning

confidence: 99%

Adjuvanted pandemic influenza vaccine: variation of emulsion components affects stability, antigen structure, and vaccine efficacy

Fox¹,

Barnes²,

Evers³

et al. 2012

Influenza Resp Viruses

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Please cite this paper as: Fox et al. (2012) Adjuvanted pandemic influenza vaccine: variation of emulsion components affects stability, antigen structure, and vaccine efficacy. Influenza and Other Respiratory Viruses DOI: 10.1111/irv.12031. Abstract Background Adjuvant formulations are critical components of modern vaccines based on recombinant proteins, which are often poorly immunogenic without additional immune stimulants. Oil‐in‐water emulsions comprise an advanced class of vaccine adjuvants that are components of approved seasonal and pandemic influenza vaccines. However, few reports have been published that systematically evaluate the in vitro stability and in vivo adjuvant effects of different emulsion components. Objectives To evaluate distinct classes of surfactants, oils, and excipients, for their effects on emulsion particle size stability, antigen structural interactions, and in vivo activity when formulated with a recombinant H5N1 antigen. Methods Emulsions were manufactured by high pressure homogenization and characterized alone or in the presence of vaccine antigen by dynamic light scattering, zeta potential, viscosity, pH, hemolytic activity, electron microscopy, fluorescence spectroscopy, and SDS‐PAGE. In vivo vaccine activity in the murine model was characterized by measuring antibody titers, antibody‐secreting plasma cells, hemagglutination inhibition titers, and cytokine production. Results We demonstrate that surfactant class and presence of additional excipients are not critical for biological activity, whereas oil structure is crucial. Moreover, we report that simplified two‐component emulsions appear more stable by particle size than more complex formulations.Finally, differences in antigen structural interactions with the various emulsions do not appear to correlate with in vivo activity. Conclusions Oil‐in‐water emulsions can significantly enhance antibody and cellular immune responses to a pandemic influenza antigen. The dramatic differences in adjuvant activity between squalene‐based emulsion and medium chain triglyceride‐based emulsion are due principally to the biological activity of the oil composition rather than physical interactions of the antigen with the emulsion.

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“…They are defined by The International Pharmaceutical Excipients Council as "substances, other than the active drug substance of finished dosage form, which have been appropriately evaluated for safety and are included in a drug delivery system to either aid the processing of the drug delivery system during its manufacture; protect; support; enhance stability, bioavailability, or patient acceptability; assist in product identification; or enhance any other attributes of the overall safety and effectiveness of the drug delivery system during storage or use" (Apte and Ugwu 2003). Lists of pharmaceuticals with their associated excipients and inclusion levels are detailed by Apte and Ugwu 2003, Sougata et al 2004and Strickley 2004. Excipients may be present at low levels, e.g.…”

Section: Excipientsmentioning

confidence: 99%

“…As APIs of the same family will employ very similar carrier fluids and excipients (Strickley 2004), the behaviour of the drop formation event will therefore be correlated to the API chemistry and structure. It is anticipated from this review that proof of concept systems for pharmaceutical printability should focus on developing a series of model systems to enable easy transfer to other similar products.…”

Section: ) Gesim A010-201mentioning

confidence: 99%

Inkjet printing for pharmaceutics – A review of research and manufacturing

Daly

Harrington

Martin

et al. 2015

International Journal of Pharmaceutics

274

185

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Abstract:Global regulatory, manufacturing and consumer trends are driving a need for change in current pharmaceutical sector business models, with a specific focus on the inherently expensive research costs, high-risk capital-intensive scale-up and the traditional centralised batch manufacturing paradigm. New technologies, such as inkjet printing, are being explored to radically transform pharmaceutical production processing and the end-to-end supply chain. This review provides a brief summary of inkjet printing technologies and their current applications in manufacturing before examining the business context driving the exploration of inkjet printing in the pharmaceutical sector. We then examine the trends reported in the literature for pharmaceutical printing, followed by the scientific considerations and challenges facing the adoption of this technology. We demonstrate that research activities are highly diverse, targeting a broad range of pharmaceutical types and printing systems. To mitigate this complexity we show that by categorising findings in terms of targeted business models and Active Pharmaceutical Ingredient (API) chemistry we have a more coherent approach to comparing research findings and can drive efficient translation of a chosen drug to inkjet manufacturing.

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Solubilizing Excipients in Oral and Injectable Formulations

Cited by 1,238 publications

References 32 publications

Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin

Efficient approach to enhance drug solubility by particle engineering of bovine serum albumin

Adjuvanted pandemic influenza vaccine: variation of emulsion components affects stability, antigen structure, and vaccine efficacy

Inkjet printing for pharmaceutics – A review of research and manufacturing

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