Gastroresistant microcapsules: new approaches for site-specific delivery of ketoprofen.
Ketoprofen is a potent non-steroidal anti-inflammatory drug (NSAID) that has been widely used in the treatment of rheumatoid arthritis and other related conditions. However, it carries the risk of undesirable systemic side effects and gastrointestinal irritation at the usual dose of oral administration. The aim of this study was to prepare and evaluate gastroresistant microcapsules containing ketoprofen. Microcapsules were obtained by a spray-drying process starting from an O/A emulsion in the presence of different pH-dependent materials (Eudragit L100, Eudragit S100, and stearic acid) dissolved in the external phase. The influence of formulation factors (oily phase employed for drug solubilization, type of coating) on the morphology, particle size distribution, drug loading capacity, in-vitro release, and ex-vivo permeation characteristics were investigated. Drug loading capacity was very high for all the microcapsules prepared. Formulation factors did not significatively influence the mean particle size, but modified microcapsule in-vitro and ex-vivo behavior.
Luppi
Barbara
B
Department of Pharmaceutical Sciences, Bologna University, Bologna, Italy. barbara.luppi@unibo.it
Bigucci
Federica
F
Zecchi
Vittorio
V
Cerchiara
Teresa
T
D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D002214:Capsules; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007408:Intestinal Absorption; D007660:Ketoprofen / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D008297:Male; D008863:Microspheres; D010316:Particle Size; D011109:Polymethacrylic Acids / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D013229:Stearic Acids / Q000737:chemistry
D000894:Anti-Inflammatory Agents, Non-Steroidal; D002214:Capsules; D005079:Excipients; D011109:Polymethacrylic Acids; D013229:Stearic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; C031183:stearic acid; D007660:Ketoprofen