Enhanced transdermal delivery of pranoprofen from the bioadhesive gels.
Percutaneous delivery of NSAIDs has advantages of avoiding hepatic first pass effect and delivering the drug for extended period of time at a sustained, concentrated level at the inflammation site that mainly acts at the joint and the related regions. To develop the new topical formulations of pranoprofen that have suitable bioadhesion, the gel was formulated using hydroxypropyl methylcellulose (HPMC) and poloxamer 407. The effects of temperature on drug release was performed at 32 degrees C, 37 degrees C and 42 degrees C according to drug concentration of 0.04%, 0.08%, 0.12%, 0.16%, and 0.2% (w/w) using synthetic cellulose membrane at 37+/-0.5 degrees C. The increase of temperature showed the increased drug release. The activation energy (Ea), which were calculated from the slope of lop P versus 1000/T plots was 11.22 kcal/ mol for 0.04%, 10.79 kcal/mol for 0.08%, 10.41 kcal/mol for 0.12% and 8.88 kcal/mol for 0.16% loading dose from the pranoprofen gel. To increase the drug permeation, some kinds of penetration enhancers such as the ethylene glycols, the propylene glycols, the glycerides, the non-ionic surfactants and the fatty acids were incorporated in the gel formulation. Among the various enhancers used, propylene glycol mono laurate showed the highest enhancing effects with the enhancement factor of 2.74. The results of this study suggest that development of topical gel formulation of pranoprofen containing an enhancer is feasible.
Shin
Sang-Chul
SC
College of Pharmacy, Chonnam National University, Gwangju 500-757, Korea.
Cho
Cheong-Weon
CW
D000269:Adhesives / Q000737:chemistry; D000279:Administration, Cutaneous; D000465:Algorithms; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics; D001578:Benzopyrans / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D001692:Biological Transport; D001831:Body Temperature; D004058:Diffusion; D005782:Gels / Q000737:chemistry*; D065347:Hypromellose Derivatives; D007848:Laurates / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D010539:Permeability; D020442:Poloxamer / Q000737:chemistry; D011422:Propionates / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D011409:Propylene Glycols / Q000737:chemistry / Q000493:pharmacokinetics; D051381:Rats; D017207:Rats, Sprague-Dawley; D015203:Reproducibility of Results; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption; D012995:Solubility; D013500:Surface Tension; D013678:Technology, Pharmaceutical / Q000379:methods; D013696:Temperature; D014783:Viscosity
D000269:Adhesives; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001578:Benzopyrans; D005782:Gels; D007848:Laurates; D011422:Propionates; D011409:Propylene Glycols; D020442:Poloxamer; C098387:propyleneglycol monolaurate; C043940:pyranoprofen; D065347:Hypromellose Derivatives; D008747:Methylcellulose