Parameters affecting the drug release from in situ gelling nasal inserts

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V
Ulrike Bertram, Roland Bodmeier

Abstract

The purpose of the study was to investigate the influence of physicochemical drug properties, drug loading, and composition of the release medium on the drug release from in situ gelling nasal inserts. Sponge-like nasal inserts of carrageenan and HPMC K15M with the model drugs oxymetazoline HCl, diprophyllin, and acetaminophen (APAP) were prepared by lyophilization. Drug release studies at different drug loadings were performed in various release media. Raman analysis, DSC, and SEM were conducted to analyze the physical state of the drugs in the inserts. All drugs were dissolved in the solid HPMC inserts and were released at similar rates at all investigated loadings except for the least soluble APAP. APAP concentrations in the hydrating HPMC K15M inserts in excess of its solubility limit resulted in reduced relative release rates at higher drug loadings. Drug-polymer interactions (formation of less soluble drug-polymer salts) resulted in a slower release of oxymetazoline HCl from carrageenan inserts than from HPMC K15M inserts. Changes in the composition of the release medium affected the water uptake of carrageenan but not of HPMC K15M inserts. Oxymetazoline release from carrageenan inserts increased with higher Na+-content o...Continue Reading

References

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Citations

Mar 22, 2013·AAPS PharmSciTech·Ragwa M FaridAbd El Azeem R Ebian
Nov 1, 2013·BioMed Research International·Kirandeep Kaur, Gurpreet Kaur
Jul 2, 2014·AAPS PharmSciTech·Eder André EstracanholliMarilisa Guimarães Lara
Apr 28, 2012·Drug Development and Industrial Pharmacy·Ulrike Bertram, Roland Bodmeier
Apr 12, 2008·International Journal of Pharmaceutics·A FehérE Csányi
Apr 30, 2016·Materials Science & Engineering. C, Materials for Biological Applications·Ashish G Sonje, Hitendra S Mahajan
Nov 20, 2016·Water Science and Technology : a Journal of the International Association on Water Pollution Research·William Leonardo da SilvaFernando Silveira

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