Mucoadhesive buccal patches of lornoxicam: II- in-vivo evaluation and clinical efficacy

Lornoxicam is a NSAID of the oxicam class and it has the same side effects of this group when taken orally. In attempts to avoid the systemic side effects of lornoxicam [e.g. gastric irritation] and to achieve sustained release of the drug, several buccal patch formulations containing lornoxicam were prepared using different polymers and were evaluated for in-vitro characteristics in part I of this study. In the current study, the selected formulations [based on the previous in-vitro data] are evaluated for in-vivo performance using experimental animals and clinical efficacy on human volunteers. Pharmacokinetic parameters were assessed following application of the selected patches in rabbits. A comparative clinical study was conducted on patients with post-operative pain and edema following maxillofacial operations. The results of the in-vivo animal experiment showed that lornoxicam formulated in different buccal patches was successfully delivered to the systemic circulation and showed high absolute bioavailability of lornoxicam. The clinical study results revealed that sodium carboxy methyl cellulose [NaCMC, 3%] formulation applied to the buccal mucosa was slightly better or equally effective to the orally administered commercial oxicam product [Feldene Flash tablets] in reducing pain level, swelling and tenderness within a period of 4 days with no observed side effects. These findings suggest that lornoxicam administered in this buccal patch may present a potential therapeutic use as a strong anti-inflammatory and analgesic agent

Mucoadhesive buccal patches of lornoxicam: 1-development and in-vitro characterization

Lornoxicam as a non-steroidal anti-inflammatory drug [NSAID] has the same side effects of this group if taken orally [GIT, renal, and hepatic disorders]. Lornoxicam and its metabolites bind extensively to plasma albumin [99%], beside that, it has a relatively short half-life [3 to 5 hrs]. The drug was formulated in mucoadhesive buccal patches using different polymers including, hydroxyethyl cellulose [HEC], hydroxypropyl cellulose [HPC], hydroxypropylmethyl cellulose [HPMC], chitosan, polyvinyl alcohol [PVA,], gelatin, sodium alginate and sodium carboxymethyl cellulose [Na CMC]. The physical characteristics of the formulated patches as mass uniformity, patch thickness, surface pH, folding endurance, swelling, residence time as well as mucoadhesion [in-vitro and ex-vivo mucoadhesion force] were evaluated. The in-vitro release of the drug from the formulated patches was studied using the USP dissolution apparatus, and the results indicated that HEC, HPC and chitosan showed the lowest drug release [70%, 76%, and 81%, respectively] while gelatin] sodium alginate and Na CMC gave the highest release [nearly 100%]. Permeation of larnoxicam formulated in different patches through rabbit buccal mucosa was also studied and the results showed that gelatin and chitosan patches resulted in the highest drug permeation. Kinetics of drug release from the different patches was found to follow zero order or diffusion kinetics

Formulation of ketorolac tromethamine in semi-solid dosage forms

Ketorolac tromethamine [KT] is one of NSAIDs that has GIT, renal and hepatic disorder if taken orally. The study aimed at avoiding the adverse effects of KT by formulating it in different topical dosage form such as gel [Sodium aignate, NaCMC, HPMC, Carbopol 934 and Pluronic F127], emulgel [O/W], microemulsion and cream [O/Wand W/O]. The interactions between KT, polymers and other ingredients used were studied using differential scanning calorimeter [DSC] and Infra red [JR] spectroscopy. The physical properties of these formulations appearance, homogeneity, pH and viscosity were studied The in-vitro release of KT from these formulations through cellophane membrane was carried out. The kinetic study of KT release from these formulations was also studied In-vitro study of KT permeation in diffusion cell using rat skin from the selected formulations was carried out. Physical investigation of KT and polymers indicated that no interaction between KT and polymers. Among the polymers used in gel formulations, HPMC and NaCMC gave the highest release rate of KT in-vitro, while pluronic F127 gave promising sustained release, In case of emulgel formulations, O/W emulgel base gave higher release than microemulsion base, Also in case of emulsion ointment base formulations, the release of KT from 0/W base was higher than W/0 type which gave the lowest release. In-vitro study of KT through the diffusion cell using rat skin as biological membrane, higher permeation was obtained in case of carbopol 934 gel and O/W emulgel comparison with pluronic F127 gel which gave the lowest permeation of KT