Physical carboxymethylscleroglucan/calcium ion hydrogels as modified drug delivery systems in topical formulations.
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 CaCl(2). 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.
Corrente
Federica
F
Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Piazzale Aldo Moro 5, 00185, Rome, Italy.
Matricardi
Pietro
P
Paolicelli
Patrizia
P
Tita
Beatrice
B
Vitali
Federica
F
Casadei
Maria Antonietta
MA
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000494:pharmacology; D002118:Calcium / Q000737:chemistry*; D004008:Diclofenac / Q000008:administration & dosage / Q000494:pharmacology; D016503:Drug Delivery Systems / Q000379:methods*; D005936:Glucans / Q000008:administration & dosage / Q000138:chemical synthesis* / Q000737:chemistry; D020100:Hydrogels / Q000008:administration & dosage* / Q000138:chemical synthesis* / Q000737:chemistry; D011817:Rabbits; D012867:Skin / Q000187:drug effects
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005936:Glucans; D020100:Hydrogels; C526264:carboxymethylscleroglucan; D004008:Diclofenac; D002118:Calcium
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