New Approach of Sucrose Myristate as a Promising Penetration Enhancer in Dermal Preparations

Boglárka Balázs; Eszter Csizmazia; Szilvia Berkó; Mária Budai-Szűcs; Piroska Szabó-Révész; Erzsébet Csányi

doi:10.3139/113.110388

Published by De Gruyter September 15, 2015

New Approach of Sucrose Myristate as a Promising Penetration Enhancer in Dermal Preparations

Saccharosemyristinsäureester als ein vielversprechender Penetrationsverstärker in dermalen Zubereitungen – Ein neuer Ansatz

Boglárka Balázs , Eszter Csizmazia , Szilvia Berkó , Mária Budai-Szűcs , Piroska Szabó-Révész and Erzsébet Csányi

From the journal Tenside Surfactants Detergents

https://doi.org/10.3139/113.110388

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Abstract

The aim of this work was to compare the penetration enhancer effect of newly developed sucrose myristate with the generally used sucrose laurate. Hydrogel formulations containing sucrose esters (SEs) were prepared and the model drug was Ibuprofen (IBU), which has oral side effects, so applying it in a transdermal system could be useful. We evaluated the effect of SE hydrogel formulations on the skin by the noninvasive in vivo test and examined their concentration dependent influence on the penetration of IBU through a synthetic membrane (in vitro) by the Franz cell method. The results indicated that sucrose myristate incorporated into hydrogel moistures the skin well and lastingly and showed a better drug penetration enhancing effect at a much lower concentration compared to sucrose laurate. Our results revealed that sucrose myristate could be a promising and effective penetration enhancer in the pharmaceutical field.

Kurzfassung

Ziel dieser Arbeit ist, den penetrationsverstärkenden Effekt eines kürzlich entwickelten Saccharosemyristinsäureesters mit dem des üblicherweise eingesetzten Saccharoselaurinsäuresters zu vergleichen. Hydrogelfomulierungen mit den Saccharoseestern (SEs) wurden präpariert. Ibuprofen (IBU) wurde als Modellwirkstoff eingesetzt. Wegen seiner oralen Nebenwirkungen könnte sein Einsatz in transdermalen Systemen sinnvoll sein. Wir bestimmten den Einfluss von SE-haltigen Hydrogelen auf die Haut mittels nichtinvasiven in-vivo-Tests und untersuchten ihren konzentrationsabhängigen Einfluss auf die Penetration von IBU durch eine synthetische Membrane mittels der Franz-Zellen-Methode. Die Ergebnisse zeigten, dass der in den Hydrogelen befindliche Saccharosemyristinsäureester die Haut gut und langanhaltend befeuchtet und eine bessere Wirkstoff-penetration bei deutlich geringerer Konzentration im Vergleich zum Saccharoselaurinsäurester hat. Unsere Resultate machten deutlich, dass der Saccharosemyristinsäureester ein vielversprechender und effektiver Penetrationsverstärker auf dem pharmazeutischen Gebiet sein kann.

Key words: Sucrose esters; penetration enhancers; dermal dosage form; skin hydration; in vitro drug diffusion

Stichwörter: Saccharoseester; Penetrationsverstärker; dermale Verabreichungsform; Hautfeuchtigkeit; in-vitro-Wirkstoffdiffusion

*Correspondence address, Mrs. Dr. Erzsébet Csányi, Department of Pharmaceutical Technology, University of Szeged, Eötvös str. 6, H-6720 Szeged, Hungary, Tel.: +36 62 54 55 73, Fax: +36 62 54 55 71, E-Mail: csanyi@pharm.u-szeged.hu

Boglárka Balázs was born in September 1988. She has graduated as pharmacist at University of Szeged, Faculty of Pharmacy in 2012. She is 3^rd year Ph. D. student at University of Szeged, Doctoral School of Pharmaceutical Sciences. Her research fields are investigation of skin diseases with spectroscopy methods (ATR-FTIR, NIR and RAMAN), development of dermal and transdermal systems and electrically-assisted transdermal delivery.

Dr. Eszter Csizmazia was born in September 1984. She completed her post graduation at University of Szeged, Faculty of Pharmacy in 2008. She obtained her Ph. D. in 2011 at University of Szeged. At present she is working as Developer at Gedeon Richter Plc. Her research activities are investigation of the drug permeation through various biological membranes and development of dermal and transdermal systems.

Dr. Szilvia Berkó was born in September 1973, studied for her pharmacist diploma at Medical University of Szeged. She did her Ph. D. in 2003, from University of Szeged, Doctoral School of Pharmaceutical Sciences. At present she is working as Assistant Lecturer at Department of Pharmaceutical Technology, University of Szeged. Her research activities are formulation rectal dosage forms, development of semisolid dosage forms and modification of skin penetration of different drugs.

Dr. Mária Budai-Szűcs was born in June 1981. She completed her post graduation in 2005 from University of Szeged, Faculty of Pharmacy. She did her Ph. D. in 2008, from University of Szeged, Doctoral School of Pharmaceutical Sciences. At present she is working as Assistant Lecturer at Department of Pharmaceutical Technology, University of Szeged. Her research focuses on stimuli responsive polymer drug deliveries, and focal drug deliveries.

Dr. Piroska Szabó-Révész was born in August 1951. She completed her post graduation at Medical University of Szeged in 1975. After obtaining her University Doctorate, she worked for as Assistant Lecturer at Department of Pharmaceutical Technology, Medical University of Szeged. Since 2005 she is working as Professor & Head of the Department of Pharmaceutical Technology. She obtained her D.Sc. in 2006. Her research activities are preparation, optimization and characterization of nanoparticular (e. g. nanocrystalline) systems with the aim of improvement of dissolution rate and permeability of water insoluble active pharmaceutical ingredients.

Dr. Erzsébet Csányi was born in February 1957. She studied for her pharmacist diploma at Medical University of Szeged. After she obtained her post graduation in 1980 she joined Medical University of Szeged as Teaching Assistant in the Department of Pharmaceutical Technology. She obtained her University Doctorate in 1982 and did her Ph. D. in 2005. Since 2005 she is working as Associate Professor at Department of Pharmaceutical Technology, University of Szeged. Her research fields are development of dermal and transdermal systems, their rheological and biopharmaceutical investigation, enhancement of the solubility of poorly soluble drugs with solubilization, with the use of microemulsion and lyotropic liquid crystalline systems and in vitro and ex vivo drug penetration examination.

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Received: 2015-03-30

Accepted: 2015-06-22

Published Online: 2015-09-15

Published in Print: 2015-09-15

New Approach of Sucrose Myristate as a Promising Penetration Enhancer in Dermal Preparations

Abstract

Kurzfassung

References

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