Abstract:OBJECTIVE To prepare the ketoprofen microemulsion-based gel in order to expand its drug loading and increase the transdermal permeability. METHODS The proportion range of oil phase/surfactant in ketoprofen microemulsion were screened by the pseudo-ternary phase diagram. Optimization of formulation for microemulsion gels was conducted by central composite design-response surface methodology with the cumulative permeation quantity across in vitro rat skin and time-lag as evaluation indexes.The transdermal performance of self prepared gel was compared with the commercially available gel. RESULTS The optimal oil phase, surfactant and cosurfactant of ketoprofen microemulsion were oleic acid, polyoxy ethylene castor oil (EL-35) and ethanol, respectively.The optimal microemulsion formulation was 1.35% oleic acid, 10.8% EL-35, and 9% ethanol by central composite design experiment. The cumulative penetration quantity in 24 h reached 562.82 μg·cm-2in vitro rat skin was 1.35 times as much as commercially available gel. CONCLUSION The ketoprofen microemulsion-based gel prepared in this study has good permeability, which lay the foundation for development of the gel.
YAKOOT M, SALEM A, YOUSEF S, et al. Clinical efficacy of spasmofen suppository in the emergency treatment of renal colic:a randomized, double -blind,double-dummy comparative trial . Drug Des Devel Ther, 2014, 8:405-410.
[2]
BALMACEDA C M. Clinical trial data in support of changing guidelines inosteoarthritis treatment . J Pain Res, 2014, 7:211-218.
[3]
GWKA F, KARAZNIEWICZ-ADA M, GRZESKOWIAK E, et al. Clinical pharmacokinetics of ketoprofen enantiomers in wild type of Cyp 2c8 and Cyp 2c9 patients with rheumatoid arthritis . Eur J Drug Metab Pharmacokinet, 2011, 36(3):167-173.
[4]
RYN J, PAIRET M. Selective COX-2 inhibitors:pharmacology, clinical effects and therapeutic potential . Exp Opin Invest Drugs,1997,6(5):609-614.
[5]
NORIAKI N, AYA I, SHION T, et al. Pharmacokinetics and antiinflammatory effect of a novel gel system containing ketoprofen solid nanoparticles . Biol Pharm Bull, 2015, 38(12):1918-1924.
[6]
SURAWEERA R K, PASANSI H G P, SAKEENA M H F. Assessing the characterizations of ketoprofen loaded and unloaded virgin coconut oil based creamy nanoemulsion . Asian J Pharm Clin Res, 2015, 8(1):275-279.
[7]
ALI F R, SHOAIB M H, YOUSUF R I, et al. Design, development, and optimization of dexibuprofen microemulsion based transdermal reservoir patches for controlled drug delivery. Biomed Res Int, 2017, 2017:1-15.
[8]
CAO M, REN L, CHEN G. Formulation optimization and ex vivo and in vivo evaluation of celecoxib microemulsion-based gel for transdermal delivery. AAPS Pharm Sci Tech, 2017, 18(16):1960-1971.
[9]
CHOURASIA K M, KANG L, CHAN S Y. Nanosized ethosomes bearing ketoprofen for improved transdermal delivery . Results Pharm Sci, 2011, 1(1):60-67. FRANCESCA M, MARIA L G R, ANTONIO M R, et al. Preparation and characterisation of liposomes encapsulating ketoprofen- cyclodextrin complexes for transdermal drug delivery . Int J Pharm, 2005, 298(1):55-67. RITIKA A, GEETA A, HARIKUMAR S L, et al. Nanoemulsion based hydrogel for enhanced transdermal delivery of ketoprofen . Adv Pharm, 2014, 2014:1-12. AMBADE K W, JADHAV S L, GAMBHIRE M N, et al. Formulation and evaluation offlurbiprofen microemulsion . Curr Drug Deliv, 2008, 5(1):32-41. BOONME P, SUKSAWAD N, SONGKRO S. Characterization and release kineties of nicotinamide microemulision-based gels . J Cosmet Sci, 2012, 63(6):397-406. YUAN Y,LI S M, WANG S L, et al. Transdermal delvery of ketoprofen microemulsion. Chin Pharm J(中国药学杂志),2006, 41(21):1647-1650. HOPPEL M, JURIC S, ETTL H, et al. Effect of monoacyl phosphatidylcholine content on the formation of microemulsions and the dermal delivery of flufenamic acid. Int J Pharm, 2015, 479(1):70-76.