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Molecules 2009, 14(8), 2684-2698; doi:10.3390/molecules14082684

Physical Carboxymethylscleroglucan/Calcium Ion Hydrogels as Modified Drug Delivery Systems in Topical Formulations

1
Dipartimento di Chimica e Tecnologie del Farmaco, “Sapienza” Università di Roma, Piazzale Aldo Moro 5, 00185, Rome, Italy
2
Dipartimento di Fisiologia e Farmacologia, “Sapienza” Università di Roma, Piazzale Aldo Moro 5, 00185, Rome, Italy
*
Author to whom correspondence should be addressed.
Received: 29 June 2009 / Revised: 16 July 2009 / Accepted: 21 July 2009 / Published: 24 July 2009
(This article belongs to the Special Issue Macromolecules Applied to Pharmaceutics)
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Abstract

A carboxymethyl derivative of scleroglucan (Scl-CM) with a 65±5% carboxylic group degree of derivatization (DD) was recently synthesized and characterized. Aqueous solutions of the polymer underwent to a sharp transition toward a gel like behaviour in the presence of divalent ions such as Ca+2. Physical hydrogels with different Scl-CM/Ca+2 ratios were prepared and characterized for their rheological behaviour. Their potential as drug delivery systems was also evaluated. To this end three non steroidal anti-inflammatory drugs (NSAIDs) were loaded into the hydrogels obtained with 2% w/v solution of Scl-CM and 0.05 and 0.1 M CaCl2. The release rate of the drugs was critically related to the salt concentration. By an appropriate combination of the hydrogels prepared using different amounts of salt, it was possible to obtain a system able to release diclofenac with zero-order kinetics. Primary skin irritation tests showed a good biocompatibility of the new polymer, as well as of its hydrogels. These results suggest a potential of the new hydrogels for the development of modified delivery systems in topical formulations.
Keywords: carboxymethyl scleroglucan; physical hydrogels; controlled release; rheology; mucoadhesiveness; primary skin irritation carboxymethyl scleroglucan; physical hydrogels; controlled release; rheology; mucoadhesiveness; primary skin irritation
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Corrente, F.; Matricardi, P.; Paolicelli, P.; Tita, B.; Vitali, F.; Casadei, M.A. Physical Carboxymethylscleroglucan/Calcium Ion Hydrogels as Modified Drug Delivery Systems in Topical Formulations. Molecules 2009, 14, 2684-2698.

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