Ciprofloxacin and ciprofloxacin-lidocaine sustained release hydrogels for topical administration

BREDA SA; MANZO RH; OLIVERA ME

Tandil-Buenos Aires, Argentina

Otro; 40 Reunion Anual de la Sociedad Argentina de Farmacología Experimental (SAFE). 40a Reunión Anual de SAFE; 2008

<!-- /* Style Definitions */ p.MsoNormal, li.MsoNormal, div.MsoNormal {mso-style-parent:""; margin:0cm; margin-bottom:.0001pt; mso-pagination:widow-orphan; font-size:12.0pt; font-family:"Times New Roman"; mso-fareast-font-family:"Times New Roman";} @page Section1 {size:612.0pt 792.0pt; margin:70.85pt 3.0cm 70.85pt 3.0cm; mso-header-margin:36.0pt; mso-footer-margin:36.0pt; mso-paper-source:0;} div.Section1 {page:Section1;} --> st1:*{behavior:url(#ieooui) } <!-- /* Font Definitions */ @font-face {font-family:Calibri; panose-1:2 15 5 2 2 2 4 3 2 4; mso-font-charset:0; mso-generic-font-family:swiss; mso-font-pitch:variable; mso-font-signature:-1610611985 1073750139 0 0 159 0;} /* Style Definitions */ p.MsoNormal, li.MsoNormal, div.MsoNormal {mso-style-parent:""; margin-top:0cm; margin-right:0cm; margin-bottom:10.0pt; margin-left:0cm; line-height:115%; mso-pagination:widow-orphan; font-size:11.0pt; font-family:Calibri; mso-fareast-font-family:Calibri; mso-bidi-font-family:"Times New Roman"; mso-fareast-language:EN-US;} @page Section1 {size:612.0pt 792.0pt; margin:70.85pt 3.0cm 70.85pt 3.0cm; mso-header-margin:36.0pt; mso-footer-margin:36.0pt; mso-paper-source:0;} div.Section1 {page:Section1;} --> The objective was to design hydrogels for the controlled release of Ciprofloxacin, (CIP, antibiotic) alone or in combination with Lidocaine, LIDO (analgesic). A set of hydrogels were prepared from partial neutralization of an acidic polyelectrolyte carrier with the basic groups of CIP and LIDO, to achieve the doses commonly indicated for their topical administration. Stability after one sterilization cycle (autoclave) was determined. The irritation potential was evaluated through Dreize test in rabbit skin. Release (0.9% NaCl solution) and reology (32, 35 and 37¨¬C) were assayed. The systems allow adjusting doses in the hydrogels with final pHs between 6-7. They are physically and chemically stable after sterilization. The products were regarded as non-irritant with non-tixotropic plastic flow. They behave as intelligent systems since both drugs are released upon contact with biological fluids. Delivery is sustained and at time ¡Ã 30 min CIP concentration is above 3 x CIM (determined for main strains responsible of skin infections). The formulations could be useful to improve available pharmacotherapy for the topical treatment and prophylaxis of infections caused by CIP-sensitive isolates such as endometriosis, bloody wounds and/or varicose ulcers. Also, the systems can be valid for other fluoroquinolones having the free basic group.