title: Physical carboxymethylscleroglucan/calcium ion hydrogels as modified drug delivery systems in topical formulations.
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 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.
authors.affiliation: Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Piazzale Aldo Moro 5, 00185, Rome, Italy.
authors.forename: Federica
authors.initials: F
authors.lastname: Corrente
authors.forename: Pietro
authors.initials: P
authors.lastname: Matricardi
authors.forename: Patrizia
authors.initials: P
authors.lastname: Paolicelli
authors.forename: Beatrice
authors.initials: B
authors.lastname: Tita
authors.forename: Federica
authors.initials: F
authors.lastname: Vitali
authors.forename: Maria Antonietta
authors.initials: MA
authors.lastname: Casadei
mesh_terms: 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
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D005936:Glucans; D020100:Hydrogels; C526264:carboxymethylscleroglucan; D004008:Diclofenac; D002118:Calcium
references.citation: Adv Drug Deliv Rev. 2002 Jan 17;54(1):3-12
references.pmid: 11755703
references.citation: Eur J Pharm Biopharm. 2000 Jul;50(1):27-46
references.pmid: 10840191
references.citation: Molecules. 2005 Jan 31;10(1):6-33
references.pmid: 18007275
references.citation: Carbohydr Res. 2000 Feb 11;324(2):116-26
references.pmid: 10702878
references.citation: Carbohydr Res. 1994 May 20;258:307-11
references.pmid: 8039185
references.citation: Eur J Pharm Sci. 2000;10(4):251-7
references.pmid: 10838014
references.citation: Fundam Clin Pharmacol. 2003 Aug;17(4):393-403
references.pmid: 12914541
references.citation: Biomaterials. 2001 Jul;22(13):1899-909
references.pmid: 11396896
references.citation: Pharm Res. 2002 Feb;19(2):182-8
references.pmid: 11885560
references.citation: Eur J Pharm Biopharm. 2007 Nov;67(3):682-9
references.pmid: 17537623
references.citation: J Control Release. 2007 May 14;119(1):5-24
references.pmid: 17382422
references.citation: J Mater Sci Mater Med. 2009 May;20(5):1081-7
references.pmid: 19132513