Development, characterization and in vivo localization study of topical 5-fluorouracil gels: A comparative study with conventional formulation

Current Drug Delivery

Volumn 11, Issue 3, 2014, Pages 401-414

  Jain, Subheet Kumar ^a   Puri, Richa ^b  

^a GURU NANAK DEV UNIVERSITY   (India)

^b PUNJABI UNIVERSITY   (India)

Author keywords

5 FU; Bioadhesive strength; Conventional cream; Localization index; Skin targeting

Indexed keywords

CARBOMER; CARBOPOL 934; FLUOROURACIL; METHYLCELLULOSE; POLOXAMER; ACRYLIC ACID DERIVATIVE; ACRYLIC ACID RESIN; ANTINEOPLASTIC AGENT; DRUG CARRIER; GEL;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; COMPARATIVE STUDY; CONTROLLED STUDY; DRUG FORMULATION; DRUG SCREENING; DRUG SOLUBILITY; ERYTHEMA; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IN VIVO STUDY; NONHUMAN; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; RAT; SKIN IRRITATION; SUSTAINED DRUG RELEASE; VISCOMETRY; VISCOSITY; ADHESION; ANIMAL; CHEMISTRY; GEL; MEDICINAL CHEMISTRY; METABOLISM; SKIN; SKIN ABSORPTION; SOLUBILITY;

ACRYLATES; ACRYLIC RESINS; ADHESIVENESS; ANIMALS; ANTINEOPLASTIC AGENTS; CHEMISTRY, PHARMACEUTICAL; DRUG CARRIERS; FLUOROURACIL; GELS; METHYLCELLULOSE; POLOXAMER; RATS; SKIN; SKIN ABSORPTION; SOLUBILITY; VISCOSITY;

EID: 84906559820     PISSN: 15672018     EISSN: 18755704     Source Type: Journal    
DOI: 10.2174/1567201810666131210112150     Document Type: Article

References (36)

1. Zackheim, H.S.; Farber, E.M. Topical Antimetabolites. Ann. Rev. Med.,1970, 21, 59-66.
2. Gross, K.; Kircik, L.; Kricorian, G. 5% 5-Fluorouracil cream for the treatment of small superficial basal cell carcinoma: efficacy, tolerability, cosmetic outcome, and patient satisfaction. Dermatol. Surgery, 2007, 33, 433-439.
3. Shin, S.C.; Cho, C.W. Enhanced transdermal delivery of pranoprofen from the bioadhesive gels. Arch. Pharm. Res., 2006, 29, 928-933.
4. Cho, C.W.; Choi, J.S.; Shin, S.C. Enhanced local anesthetic action of mepivacaine from the bioadhesive gels. Pak. J. Pharm. Sci., 2011, 24(1), 87-93.
5. Dhawan, S.; Medhi, B.; Chopra, S. Formulation and Evaluation of Diltiazem Hydrochloride Gels for the Treatment of Anal Fissures. Sci. Pharm., 2009, 77, 465-482.
6. Khullar, R.; Kumar, D.; Seth, N.; Saini, S. Formulation and evaluation of mefenamic acid emulgel for topical delivery. Saudi. Pharm. J., 2012, 20, 63-67.
7. Varshosaz, J.; Jaffari, F.; Karimzadeh, S. Development of bioadhesive chitosan gels for topical delivery of lidocaine. Sci. Pharm., 2006, 74, 209-223.
8. Dhiman, M.; Yedurkar, P.; Sawant, K.K. Formulation, characterization, and in vitro evaluation of bioadhesive gels containing 5- Fluorouracil. Pharm. Develop. Tech., 2008, 13, 15-25.
9. Sudhakar, Y.; Koutsu, K.; Bandyopadhyay, A.K. Buccal bioadhesive drug delivery - A promising option for orally less efficient drugs. J. Control. Release., 2006, 114, 15-40.
10. Jukanti, R.; Mateti, A.; Bandari, S.; Veerareddy, P.R. Transdermal Delivery of Acyclovir Sodium Via Carbopol Gels: Role of Chemical Permeation Enhancers. Lett. Drug Design Discov., 2011, 8, 381-389
11. Puri, R.; Jain, S. Ethogel topical formulation for increasing the local bioavailability of 5-Fluorouracil: A mechanistic study. Anti- Cancer Drugs, 2012, 23,9 923-934.
12. Jain, S.; Jain, N.; Bhadra, D.; Tiwary, A.K.; Jain, N.K. Transdermal delivery of an Analgesic agent using Elastic liposomes: Preparation, characterization and performance evaluation. Curr. Drug Deliv., 2005, 2(3), 223-233.
13. Nassim, M.A.; Shirazi, F.H.; Cripps, C.M.; Veerasinghan, S.; Molepo, M.J.; Obrocea, M.; Redmond, D.; Bates, S.; Fry, D.; Stewart, D.J.; Goel, R. An HPLC method for the measurement of 5-fluorouracil in human plasma with a low detection limit and a high extraction yield. Int. J. Mol. Med., 2002, 10(4), 513-6.
14. Draize, J.; Woodard, G.; Calvery, H. Methods for the study of irritation and toxicity of substance applied to the skin and mucous membranes. J. Pharmacol. Exp. Ther., 1944, 82, 377-390.
15. United State Pharmacopoeia NF. 5-Fluorouracil. 2007, p 2163.
16. Patel, J.; Patel, B.; Banwai, H.; Parma, K.; Patel, M. Formulation and evaluation of topical aceclofenac gel using different gelling agent. Int. J. Drug. Dev. Res., 2011, 3(1), 156-164.
17. Abd El- Hady, S.S.; Mortada, N.; Awad, G.A.S.; Zaki, N.M.; Taha, R.A. Development of in-situ gelling and mucoadhesive mebeverine hydrochloride solution for rectal administration. Saudi. Pharm. J., 2003, 11(4), 159-171.
18. Amal, E.K.; Mona, E.K. Thermally reversible in situ gelling carbamazepine liquid suppository. Drug Deliv., 2006, 13, 143-148.
19. GRAS Notification for Hydroxypropyl Methylcellulose. www.accessdata.fda.gov/scripts/fcn/gras_notices/grn000190.pdf (Assessed on April 10, 2012).
20. Islam, M.T.; Hornedo, N.R.; Ciotti, S.; Ackermann, C. Rheological Characterization of topical Carbomer gels neutralized to different pH. Pharm. Res., 2004, 21, 1192-1199.
21. Lee, J.W.; Park, J.H.; Robinson, J.R. Bioadhesive-based dosage forms: the next generation. J. Pharm. Sci., 2000, 89, 850-866.
22. Schmolka, I., Artificial skin, preparation and properties of Pluronic F-127 gels for the treatment of the burns. J. Biomed. Mater. Res., 1972, 6, 571-82.
23. Mitkari, B.V.; Korde, S.A.; Mahadik, K.R.; Kokare, C.R. Formulation and evaluation of topical liposomal gel for Fluconazole. Indian. J. Pharm. Educ. Res., 2010, 44(4), 324-329.
24. Arias, J.L. Novel Strategies to Improve the Anticancer Action of 5- Fluorouracil by Using Drug Delivery Systems. Molecules, 2008, 13, 2340-2369.
25. Ahuja, A.; Khar, R.K.; Ali, J. Mucoadhesive drug delivery systems. Drug Dev. Ind. Pharm., 1997, 23, 489-515.
26. Levang, A.K.; Zhao, K.; 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., 1999, 181, 255-263.
27. Mak, VH.; Potts, R.O.; Guy, R.H. Percutaneous penetration enhancement in vivo measured by attenuated total reflectance infrared spectroscopy. Pharm. Res., 1990, 7(8), 835-41.
28. Babita, K.; Kumar, V.; Rana, V.; Jain, S.; Tiwary, A. K. Thermotropic and Spectroscopic behavior of skin: Relationship with percutaneous permeation enhancement. Curr. Drug Deliv., 2006, 3(1), 95-113.
29. Obata, Y.; Utsumi, S.; Watanabe, H.; Suda, M.; Tokudome, Y.; Otsuka, M.; Takayama, K. Infrared spectroscopic study of lipid interaction in stratum corneum treated with transdermal absorption enhancers. Int. J. Pharm., 2010, 389, 18-23.
30. Jain, S.; Jain, N.; Bhadra, D.; Tiwary, A.K.; Jain, N.K. Sustained and targeted delivery of an ant-HIV agent using elastic liposomal formulation: Mechanism of action. Curr. Drug Deliv., 2006, 3(2), 157-166.
31. Apikian, M.; Goodman, G., Intralesional 5-Fluorouracil in the treatment of keloid scars. Australas. J. Dermatol., 2004, 45(2), 140-143.
32. Johnson, M.R.; Hageboutros, A.; Wank, K.; High, L.; Smith, J.B.; Diasio, R.B. Life-threatening toxicity in a dihydropyrimidine dehydrogenase- deficient patient after treatment with topical 5-Fluorouracil. Clin. Cancer Res., 1999, 5, 2006-2011.
33. Han, R.; Yang, Y.M.; Dietrich, J.; Luebke, A.; Mayer-Pröschel, M.; Noble, M. Systemic 5-Fluorouracil treatment causes a syndrome of delayed myelin destruction in the central nervous system. J. Biol., 2008, 7, 12.1-12.22.
34. Erlanger, M.; Martz, G.; Ott, F.; Storck, H.; Rieder, J.; Kessler, S. Cutaneous absorption and urinary excretion of 6- 14C-5- Fluorouracil ointment applicated in an ointment to healthy and diseased human skin. Dermatologica, 1970, 140(1), 7-14.
35. Jirova, D.; Liebsch, M.; Basketter, D.; Spiller, E.; Kejlova, K.; Bendova, H. Comparison of human skin irritation and photoirritation patch test data with cellular in vitro assays and animal in vivo data. In: Proc. 6th World Congress on Alternatives & Animal Use in the Life Sciences August 21-25, Japan Special Issue. Tokyo, 2007; pp. 359-365.
36. Levy, S.; Furst, K.; Chern, W. A comparison of the skin permeation of three topical 0.5% Fluorouracil formulations with that of a 5% formulation. Clin. Therap., 2001, 23(6), 901-907.