COMPLEXATION OF NAPROXEN WITH BETA-CYCLODEXTRIN WITH AND WITHOUT POLOXAMER 407 TO ENHANCE DRUG DISSOLUTION
Amal A. Elkordy1*, Amin Ashoore1 and Ebtessam A. Essa2,3
1. University of Sunderland, Department of Pharmacy, Health and Well-being, Sunderland, SR1 3SD, UK 2. Faculty of Pharmacy, Tanta University, Tanta, Egypt 3. Faculty of Pharmacy, Am El-Qura University, Saudi Arabia
Keywords: Dissolution enhancement, Naproxen, freeze drying, cyclodextrins, poloxamer-407
Abstract

Non steroidal anti-inflammatory drugs (NSAID) have adverse effects on stomach. The histological appearance of affected mucosal cells ranging from mild to sever inflammation. Accordingly, the purpose of this study was to investigate the effects of: (i) ß-cyclodextrin (ß-CD), Poloxamer-407 (PLX) and sorbitol (Sorb) as carriers and (ii) freeze drying and physical mixing as techniques on solubility and dissolution of a model poorly water soluble NSAID drug, Naproxen (Nap) for the ultimate aim to avoid gastric discomfort via enhancement drug release. Therefore, two binary drug/carrier (1:1 and 1:4 w/w Nap/carrier ratios) combinations were prepared. The effect of multicomponent carrier systems, using ternary physical mixtures of Nap with ß-CD and PLX on the drug solubility and dissolution were also studied. All formulations were characterized using solubility, content uniformity, dissolution studies, Fourier transform infra-red (FT-IR) spectroscopy, and differential scanning calorimetry (DSC). All tested Nap/ combinations showed enhancement in drug release compared to pure drug, except Sorb that show a slight improvement only at high sugar concentration. Ternary Nap combinations showed the highest improvement of drug dissolution, compared to binary ones. Freeze dried formulations showed a marked enhancement in drug release especially in the first few minutes, compared to physical mixtures. Thermal studies indicated a reduction in drug crystallinity with freeze dried samples giving a higher amorphous yield obtained compared to binary physical mixtures.

Article Information

Identifiers and Pagination:
Year:2012
Volume:4
First Page:178
Last Page:191
Publisher Id:JAppPharm (2012 ). 4. 178-191
Article History:
Received:April 7, 2012
Accepted:June 20, 2012
Collection year:2012
First Published:July 1, 2012


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Prof. Dr. Cornelia M. Keck (Philipps-Universität Marburg)
Marburg, Germany

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Welcome to the research group of Prof. Dr. Cornelia M. Keck in Marburg. Cornelia M. Keck is a pharmacist and obtained her PhD in 2006 from the Freie Universität (FU) in Berlin. In 2009 she was appointed as Adjunct Professor for Pharmaceutical and Nutritional Nanotechnology at the University Putra Malaysia (UPM) and in 2011 she obtained her Venia legendi (Habilitation) at the Freie Universität Berlin and was appointed as a Professor for Pharmacology and Pharmaceutics at the University of Applied Sciences Kaiserslautern. Since 2016 she is Professor of Pharmaceutics and Biopharmaceutics at the Philipps-Universität Marburg. Her field of research is the development and characterization of innovative nanocarriers for improved delivery of poorly soluble actives for healthcare and cosmetics. Prof. Keck is executive board member of the German Association of Nanotechnology (Deutscher Verband Nanotechnologie), Vize-chairman of the unit „Dermocosmetics“ at the German Society of Dermopharmacy, active member in many pharmaceutical societies and member of the BfR Committee for Cosmetics at the Federal Institute for Risk Assessment (BfR).

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