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Development and characterisation of interactive mixtures with a fine-particulate mucoadhesive carrier for nasal drug delivery
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Pharmacy.
2007 (English)In: European journal of pharmaceutics and biopharmaceutics, ISSN 0939-6411, E-ISSN 1873-3441, Vol. 67, no 2, 370-376 p.Article in journal (Refereed) Published
Abstract [en]

The aim of this study was to investigate whether mucoadhesive interactive mixtures can be created using carrier particles in a size range appropriate for nasal administration, i.e. 10–50 μm. We also used theoretical models to investigate if homogeneity measurements can be used to evaluate the formation of interactive mixtures containing carrier particles in this size range. Sodium starch glycolate (SSG) was used as carrier material and sodium salicylate (SS) as the model fine-particulate drug. The size ranges of SSG particles and amounts of SS were varied to find the smallest carrier particle size and highest amount of drug that still resulted in an interactive mixture. Visual inspection of the mixtures by scanning electron microscopy showed that interactive mixtures could be formed with carrier particles as small as 30 μm and containing up to 4% (w/w) of SS. Comparisons with theoretical models highlighted the difficulties of using homogeneity measurements to determine if interactive mixtures were formed. The measured coefficients of variation (CV) for the amount of drug in the samples were low and inferior mixtures were associated with only a slight increase. It was thus concluded that mucoadhesive interactive mixtures can be created in an appropriate size range for nasal administration, but that visual inspection of these mixtures is initially necessary to confirm the formation of an interactive mixture.

Place, publisher, year, edition, pages
2007. Vol. 67, no 2, 370-376 p.
Keyword [en]
Interactive mixtures, Ordered mixtures, Mucoadhesion, Nasal drug delivery, Sodium starch glycolate, Primojel®
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-97562DOI: 10.1016/j.ejpb.2007.03.006ISI: 000249509800008PubMedID: 17451925OAI: oai:DiVA.org:uu-97562DiVA: diva2:172557
Available from: 2008-10-03 Created: 2008-10-03 Last updated: 2017-12-14Bibliographically approved
In thesis
1. Studies on a Novel Powder Formulation for Nasal Drug Delivery
Open this publication in new window or tab >>Studies on a Novel Powder Formulation for Nasal Drug Delivery
2008 (English)Doctoral thesis, comprehensive summary (Other academic)
Abstract [en]

Nasal administration has potential for the treatment of indications requiring a fast onset of effect or for drugs with low oral bioavailability. Liquid nasal sprays are relatively common, but can be associated with suboptimal absorption from the nasal cavity; this thesis shows that nasal absorption can be significantly enhanced with a dry powder formulation.

It was shown that interactive mixtures, consisting of fine drug particles adhered to the surface of mucoadhesive carrier particles, could be created in a particle size suitable for nasal administration. Sodium starch glycolate (SSG), a common tablet excipient, was used as carrier material. In vitro evaluation of the formulation indicated that the mucoadhesion of the carrier was unlikely to be affected by the addition of a drug. The powder formulation did not improve the in vitro transfer of dihydroergotamine across porcine nasal mucosa compared with a liquid formulation; however, the results were associated with methodological shortcomings. The binding of model substances to SSG and three other excipients was evaluated. Ion exchange interactions were for example detected between SSG and cationic drugs, but these interactions were most extensive at low salt concentrations and should unlikely affect in vivo bioavailability at physiological salt concentrations. Absorption of the peptide drug desmopressin from the SSG nasal formulation, from a novel sublingual tablet formulation and from a commercial nasal liquid spray was evaluated in a clinical trial. While no improvement over the liquid spray was seen with the sublingual tablet, plasma concentrations after the nasal powder formulation were three times higher than those after the liquid spray. All formulations were well accepted by the volunteers. The use of currently available mucoadhesive carrier particles in interactive mixtures offers potential for a new method of producing nasal powder formulations that should also be applicable to large scale production.

Place, publisher, year, edition, pages
Uppsala: Acta Universitatis Upsaliensis, 2008. 70 p.
Series
Digital Comprehensive Summaries of Uppsala Dissertations from the Faculty of Pharmacy, ISSN 1651-6192 ; 81
Keyword
nasal drug delivery, nasal powder spray, interactive mixture, mucoadhesion, sodium starch glycolate, superdisintegrant, bioavailability, clinical trial
National Category
Pharmaceutical Sciences
Identifiers
urn:nbn:se:uu:diva-9292 (URN)978-91-554-7288-7 (ISBN)
Public defence
2008-10-24, B41, BMC, Husargatan 3, Uppsala, 09:15 (English)
Opponent
Supervisors
Available from: 2008-10-03 Created: 2008-10-03 Last updated: 2009-05-06Bibliographically approved

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