lornoxicam and glyceryl-behenate

Solid lipid nanoparticles (SLN), nanostructured lipid carriers (NLC) and nanoemulsion (NE) of lornoxicam (LRX) were prepared for the treatment of painful and inflammatory conditions of the skin. Compritol® 888 ATO, Lanette® O and oleic acid were used as solid and liquid lipids. SLN, NLC and NE were found physically stable at various temperatures for 6 months. Case I diffusional drug release was detected as the dominant mechanism indicating Fickian drug diffusion from nanoparticles and nanoemulsion. The highest rate of drug penetration through rat skin was obtained with NE followed by NLC, SLN and a gel formulation. Nanoformulations significantly increased drug penetration through rat skin compared to the gel (p<0.05). Thus, SLN, NLC and NE of LRX can be suggested for relieving painful and inflammatory conditions of the skin.

Topics: Administration, Cutaneous; Animals; Anti-Inflammatory Agents, Non-Steroidal; Drug Carriers; Drug Liberation; Drug Stability; Drug Storage; Emulsions; Fatty Acids; Fatty Alcohols; Inflammation; Lipids; Male; Nanoparticles; Oleic Acid; Pain; Piroxicam; Rats; Rats, Wistar; Skin Absorption; Skin Diseases; Temperature; Time Factors

The objective of this study was to modify the release characteristics of lornoxicam, a highly potent nonsteroidal anti-inflammatory drug, by preparing compression-coated tablets (CCTs) that provide complete drug release that starts in the stomach to rapidly alleviate the painful symptoms and continues in the intestine to maintain prolonged analgesic effect as well as meets the reported sustained release specifications.. Each of the prepared CCTs was composed of a sustained release tablet core and an immediate release coat layer. Amorphous, well-characterized, freeze-dried solid dispersion of lornoxicam with polyvinylpyrrolidone K-30 was employed in the coat layer to attain an initial rapid dissolution of lornoxicam in the stomach, assuring rapid onset of analgesic effect. Compritol ATO 888, a lipophilic matrix-forming material, was included in the core tablets to sustain lornoxicam release. Lactose was also incorporated into these core tablets to ensure complete release of lornoxicam in a time period comparable to the gastrointestinal residence time.. All the prepared CCTs showed acceptable physical properties that complied with compendial requirements. On the basis of in vitro drug release studies, performed in simulated gastric and intestinal fluids in sequence to mimic the gastrointestinal transit, CCTs belonging to formulations F3 CCTs and F4 CCTs were able to show the desired release profile.. This study demonstrated the possibility of modulating lornoxicam release using CCTs to meet the reported sustained release specifications.

Topics: Anti-Inflammatory Agents, Non-Steroidal; Calorimetry, Differential Scanning; Chemical Phenomena; Chemistry, Pharmaceutical; Delayed-Action Preparations; Drug Compounding; Excipients; Fatty Acids; Gastrointestinal Transit; Humans; Hydrogen-Ion Concentration; Lactose; Piroxicam; Povidone; Solubility; Spectroscopy, Fourier Transform Infrared; Surface Properties; Suspensions; Tablets; Time Factors; X-Ray Diffraction