Enhanced bioavailability of lacidipine via microemulsion based transdermal gels: Formulation optimization, ex vivo and in vivo characterization

International Journal of Pharmaceutics

Volumn 388, Issue 1-2, 2010, Pages 231-241

  Gannu, Ramesh ^a   Palem, Chinna Reddy ^a   Yamsani, Vamshi Vishnu ^a   Yamsani, Shravan Kumar ^a   Yamsani, Madhusudan Rao ^a  

^a KAKATIYA UNIVERSITY   (India)

Author keywords

Bioavailability; Box Behnken; EVIV correlation; Lacidipine; Microemulgel; Microemulsion; Optimization; Pharmacokinetics

Indexed keywords

CARBOXYMETHYLCELLULOSE; EUCALYPTUS OIL; LABRASOL; LACIDIPINE; LIQUID PARAFFIN; MYRISTIC ACID ISOPROPYL ESTER; N,N DIMETHYLFORMAMIDE; OLEIC ACID; POLYSORBATE 80; SESAME SEED OIL; WATER;

ANIMAL EXPERIMENT; ANIMAL TISSUE; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DOSAGE FORM COMPARISON; DRUG EFFICACY; DRUG FORMULATION; DRUG PENETRATION; DRUG SOLUBILITY; DRUG STABILITY; ERYTHEMA; EX VIVO STUDY; FLOW KINETICS; GEL; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HYPERTENSION; IN VIVO STUDY; MATHEMATICAL ANALYSIS; MAXIMUM PLASMA CONCENTRATION; MICROEMULSION; NONHUMAN; PRIORITY JOURNAL; RABBIT; RAT; RESPONSE SURFACE METHOD; SKIN IRRITATION; SKIN PENETRATION; TIME; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADMINISTRATION, CUTANEOUS; ANIMALS; BIOLOGICAL AVAILABILITY; CALCIUM CHANNEL BLOCKERS; CHEMISTRY, PHARMACEUTICAL; DATA INTERPRETATION, STATISTICAL; DIHYDROPYRIDINES; EMULSIONS; GELS; MYRISTATES; ORGANIC CHEMICALS; PHASE TRANSITION; POLYSORBATES; RABBITS; RATS; RATS, WISTAR; SKIN ABSORPTION; SOLUBILITY; SURFACE-ACTIVE AGENTS;

EID: 76549134681     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2009.12.050     Document Type: Article

References (30)

1. Baboota S., Al-Azaki A., Kohli K., Ali J., Dixit N., and Shakeel F. Development and evaluation of a microemulsion formulation for transdermal delivery of terbinafine PDA. J. Pharm. Sci. Technol. 61 (2007) 276-285
2. Baroli B., Lopez-Quintela M.A., Delgado-Charro M.B., Fadda A.M., and Blanco-Mendez J. Microemulsions for topical delivery of 8-methoxsalen. J. Control Release 69 (2000) 209-218
3. Bonacucina G., Martelli S., and Palmieri G.F. Rheological, mucoadhesive and release properties of Carbopol gels in hydrophilic cosolvents. Int. J. Pharm. 282 (2004) 115-130
4. Box G.E.P., and Behnken D.W. Some new three level designs for the study of quantitative variables. Technometrics 2 (1960) 455-475
5. Chen H., Mou D., Du D., Chang X., Zhu D., Liu J., Xu H., and Yang X. Hydrogel thickened microemulsion for topical administration of drug molecule at an extremely low concentration. Int. J. Pharm. 341 (2007) 78-84
6. Chen H.B., Chang X.L., Du D.R., Li J., Xu H.B., and Yang X.L. Microemulsion based hydrogel formulation of ibuprofen for topical delivery. Int. J. Pharm. 315 (2006) 52-58
7. Chopra S., Pati G.V., and Motwani S.K. Release modulating hydrophilic matrix systems of losartan potassium: optimisation of formulation using statistical experimental design. Eur. J. Pharm. Biopharm. 66 (2007) 73-82
8. Clarke. Clarke's Analysis of Drugs and Poisons (2007). www.medicinescomlete.com
9. Emami J. In vitro-in vivo correlations: from theory to applications. J. Pharm. Pharm. Sci. 9 (2006) 31-51
10. Gallarate M., Gasco M.R., and Rua G. In vitro release of azelaic acid from oil-in-water microemulsions. Acta Pharm. Yugoslv. 40 (1990) 541-545
11. Gannu R., Yamsani V.V., Palem C.R., Yamsani S.K., and Yamsani M.R. Development of high performance liquid chromatography method for Lacidipine in rabbit serum: application to pharmacokinetic study. Anal. Chim. Acta 632 (2009) 278-283
12. Gasco M.R., Gallarate M., and Pattarino F. In vitro permeation of azelaic acid from viscosized microemulsions. Int. J. Pharm. 69 (1991) 193-196
13. Goldberg-Cettina M., Liu P., Nightingale L., and Kurihara-Bergstrom T. Enhanced transdermal delivery of estradiol in vitro using binary vehicles of isopropyl myristate and short-chain alkanols. Int. J. Pharm. 114 (1995) 237-245
14. Govender S., Pillay V., Chetty D.J., Essack S.Y., Dangor C.M., and Govender T. Optimisation and characterisation of bioadhesive controlled release tetracycline microspheres. Int. J. Pharm. 306 (2005) 24-40
15. Hayton W.L., and Chen T. Correction of perfusate concentration for sample removal. J. Pharm. Sci. 71 (1982) 820-821
16. Ho H.O., Hsiao C.C., and Sheu M.T. Preparation of microemulsions using polyglycerol fatty acid esters as surfactant for the delivery of protein drugs. J. Pharm. Sci. 85 (1996) 138-143
17. Kamal M.A., Iimura N., Nabekura T., and Kitagawa S. Enhanced skin permeation of diclofenac by ion-pair formation and further enhancement by microemulsion. Chem. Pharm. Bull. 55 (2007) 368-371
18. Kreilgaard M. Influence of microemulsions on cutaneous drug delivery. Adv. Drug Deliv. Rev. 54 (2002) 77-98
19. Kreilgaard M., Pedersen E.J., and Jaroszewski J.W. NMR characterisation and transdermal drug delivery potential of microemulsion systems. J. Control Release 69 (2000) 421-433
20. Lawrence M.J., and Rees G.D. Microemulsion-basedmedia as novel drug delivery systems. Adv. Drug Deliv. Rev. 45 (2000) 89-121
21. Lee C.R., and Bryson H.M. Lacidipine: a review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in the treatment of hypertension. Drugs 48 (1994) 274-296
22. Levang A.K., Zhao K., and Singh J. Effect of ethanol/propylene glycol on the in vitro percutaneous absorption of aspirin, biophysical changes and macroscopic barrier properties of the skin. Int. J. Pharm. 181 (1999) 255-263
23. Mc Cormack P.L., and Wagstaff A.J. Lacidipine a review of its use in the management of hypertension. Drugs 63 (2003) 2327-2356
24. Mohammed C., and Manoj V. Aerosol-OT microemulsions as transdermal carriers of tatracaine hydrochloride. Drug Dev. Ind. Pharm. 26 (2000) 507-512
25. Peltola S., Saarinen-Savolainen P., Kiesvaara J., Suhonen T.M., and Urtti A. Microemulsions for topical delivery of estradiol. Int. J. Pharm. 254 (2003) 99-107
26. Rhee Y.S., Choi J.G., Park E.S., and Chi S.C. Transdermal delivery of ketoprofen using microemulsions. Int. J. Pharm. 228 (2001) 161-170
27. Sintov A.C., and Shapiro L. New microemulsion vehicle facilitates percutaneous penetration in vitro and cutaneous drug bioavailability in vivo. J. Control. Release 95 (2004) 173-183
28. Trotta M., Gallarate M., Pattarino F., and Carlotti M.E. Investigation of the phase behaviour of systems containing lecithin and 2-acyl lysolecithin derivatives. Int. J. Pharm. 190 (1999) 83-89
29. Wu H., Ramachandran C., Weiner N.D., and Roessler B.J. Topical transport of hydrophilic compounds using water-in-oil nano emulsions. Int. J. Pharm. 220 (2001) 63-75
30. Zhao X., Liu J.P., Zhang X., and Li Y. Enhancement of transdermal delivery of theophylline using microemulsion vehicle. Int. J. Pharm. 327 (2006) 58-64