Rheological and functional characterization of new antiinflammatory delivery systems designed for buccal administration.
The aim of the present paper was to investigate the influence of different formulation parameters on the rheological and functional properties of emulgels (gelified emulsions), intended for the buccal administration of the antiinflammatory drug flurbiprofen. The influence of formulation parameters, such as (a) the amount of gelling polymeric emulsifier (Pemulen 1621 TR-1) used, (b) the oil to water ratio present in the O/W emulgel and finally (c) the pH of the formulation, was studied by a experimental design (DoE) approach. Formulations were analyzed in term of size and morphology of the internal semi-solid oil droplets as well as in term of rheological properties in the presence or in the absence of flurbiprofen by "shear stress vs. shear rate tests" and "frequency sweep tests". Emulgels were also characterized in vitro both by bioadhesion tests and release studies. In particular release studies demonstrated that flurbiprofen is released by the emulgels in a controlled manner, the drug release efficacy within the first 100min was comprised between 50 and 80% of the total amount of the drug. Finally, in vivo tests on healthy volunteers have demonstrated that emulgels were able to remain on buccal mucosa for an average period of 1h, moreover emulgels did not have bad taste and volunteers referred that were agreeable and pleasant.
Perioli
Luana
L
Dipartimento di Chimica e Tecnologia del Farmaco, Università degli Studi di Perugia, Via del Liceo 1, Perugia 06123, Italy. luanaper@unipg.it
Pagano
Cinzia
C
Mazzitelli
Stefania
S
Rossi
Carlo
C
Nastruzzi
Claudio
C
D000268:Adhesiveness; D000278:Administration, Buccal; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004655:Emulsions / Q000737:chemistry; D005079:Excipients / Q000737:chemistry*; D005480:Flurbiprofen / Q000008:administration & dosage / Q000737:chemistry*; D005782:Gels / Q000737:chemistry; D006801:Humans; D006863:Hydrogen-Ion Concentration; D009061:Mouth Mucosa / Q000378:metabolism; D009821:Oils / Q000737:chemistry; D012212:Rheology; D013552:Swine; D013649:Taste; D014867:Water / Q000737:chemistry
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D004655:Emulsions; D005079:Excipients; D005782:Gels; D009821:Oils; D014867:Water; D005480:Flurbiprofen