Back
 PP  Vol.2 No.3 , July 2011
Design, Formulation and Evaluation of Transdermal Drug Delivery System of Budesonide
Abstract: Budesonide is a highly potent synthetic, nonhalogenated corticosteroid. The mechanism of action of corticosteroids in allergic rhinitis remains unknown, but may involve reductions in number of various mediator cells such as basophils, eosinophils, T-helper cells, mast cells, and neutrophils. In the nasal mucosa, nasal reactivity to allergens, and release of inflammatory mediators and proteolytic enzymes. Budesonide is very effective and quikly acting as it is rapidly and almost completely absorbed after oral administration, but has poor systemic availability (about 10%) due to extensive first-pass metabolism in the liver, mainly by the cytochrome P450 isoenzyme CYP3A4.. The major metabolites, 6-β- hydroxybudesonide and 16-α-hydroxyprednisolone have less than 1% of the glucocorticoid activity of unchanged drug with a terminal half-life of about 2 - 4 hours. Polymeric films containing Eudragit RL 100: Eudragit RS: drug (7:3:1, 7: 2:1) and Ethyl cellulose: PVP: drug (7:3:1, 7:2:1) were selected for transdermal administration based on evaluation studies. These polymeric films were prepared by mercury substrate method employing PEG-400 as plasticizer. Two different penetration enhancers Urea and Dimethyl sulphoxide (DMSO) were employed in the study. The patches in each group were uniform in drug content, thickness. In Vitro drug permeation, moisture absorption and WVTR studies were carried out on these test patches. It was found that at all humidity condition the absorption increases which were linear to the moisture absorbed. In PVA and EUDRAGIT RL 100 patches the water vapor transmission rate was found to be higher at 75% RH, RT conditions. Therefore at both % RH, RT condition the PVA and EUDRAGIT RL 100 patches provides the best resistance to water vapor. Therefore, when applied to animals (in further studies) these patches may provide more occlusion to water vapor loss from skin thus making atmosphere beneath the skin more humid that aid in drug permeation.
Cite this paper: nullU. Lade, Y. Amgaonkar, R. Chikhale, D. Biyani and M. Umekar, "Design, Formulation and Evaluation of Transdermal Drug Delivery System of Budesonide," Pharmacology & Pharmacy, Vol. 2 No. 3, 2011, pp. 199-211. doi: 10.4236/pp.2011.23029.
References

[1]   B. J. Unde, “Pharmacotherapy of asthma,” In: L. L. Brunton, J. S. Lazo, K. L. Parker, Eds., Goodman & Gil- man’s, The pharmacological basis of therapeutics., Mc- graw-Hill medical publishing division, New York, 2006, pp. 897-934.

[2]   C. M. Spencer, D. McTavish, “Budesonide: a review of its pharmacological properties and therapeutic efficacy in inflammatory bowel disease,” Drugs, Vol. 50, 1995, pp. 854-72.

[3]   R. N. Brogden, D. McTavish, “Budesonide: an updated review of its pharmacological properties, and therapeutic efficacy in asthma and rhinitis,” Drugs, Vol. 44, 1998, pp. 375-407,

[4]   G. Jeffrey, et al., “Have done budesonide enema for the treatment of active, distal ulcerative colitis and proctitis: A dose ranging study,” Current Therapy, Vol. 22, 2005, 23-27.

[5]   N. Mygind, T. J. H. Clark, “Topical steroid treatment for asthma and rhinitis” In: B. Tindall, Inc., London, 1980, pp. 89, 91,152,159,172.

[6]   K. Masuyama, et al., “Glucocorticosteroid (fluticasone propionate) inhibits cells expressing cytokine mRNA for interleukin-4 in the nasal mucosa in allergen-induced rhinitis,” Immunology, Vol. 82, 1994, pp. 192-99.

[7]   N. S. Chandrashekar, R. H. Shobha Rani, “Design, fabri- cation and calibration of modified Franz diffusion cell for transdermal diffusion studies,” International Journal of Pharmaceutical excipients. October-November 2005, pp. 104-106.

[8]   J. Eliassaf, “Detection of small quantity of Poly(vinyl alcohol) in poly(vinyl chloride) resins,” Polym. Lett., Vol.16, 1972, pp. 225-235.

[9]   S. P. Gupta, S. K. Jain, “Development of matrix-mem- brane transdermal drug delivery system for atenolol,” Drug Delivery, Vol. 11, 2004, pp. 281-286.

[10]   P. R. P. Verma, S. S. Iyer, “Transdermal Delivery of propranolol using mixed grades of Eudragit: Design and in vitro and in vivo evaluation,” Drug dev. Ind. Pharm., Vol. 26, No. 4, 2000, pp. 471-476.

[11]   R. Krishna, J. K. Pandit, “Transdermal delivery of pro- pranolol,” Ind. Pharm., Vol. 20, No. 15, 1994, pp. 2459- 2465.

[12]   P. Arora, B. Mukherjee, “Design, Development, Phys- icochemical and in vitro and in vivo Evaluation of Transdermal Patches containing Diclofenac diethylam- monium salt,” J. Pharm. Sci., Vol. 91, 2002, pp. 2076- 2089.

[13]   United States Pharmacopoeia, “Physical tests <711> Dissolution,” Vol. 24, 2000, pp. 1941.

[14]   M. Siewert, J. Dressman, C. K. Brown, V. P. Shah, “FIP/ AAPS Guidelines to Dissolution / in vitro release testing of novel / special dosage forms,” AAP Spharmscitech, Vol. 4, No. 1, Article 7. 2003, pp. 1-10.

[15]   C. Valenta, B. G. Auner, “The use of polymers for dermal and transdermal delivery,” European Journal of Pharma- ceutical Sciences. Vol. 58, 2004, pp. 279-289.

[16]   P. Costa, “Modeling and comparison of dissolution pro- files,” Eur. J. Pharm. Sci. Vol. 13, 2001, pp. 123-133.

[17]   J. Singh, H. I. Maibach, “Irritancy of Topical Chemicals and Transdermal Delivery Systems,” Drug Pharm. Sci. Vol. 1, 2001, pp. 281-296.

[18]   A. C. Calpena, E. Escribano, H. San Martin, “Influence of formulation on the in vitro transdermal penetration of sodium Diclofenac,” Arzneimittle Forschung Drug Research, Vol. 49, No. 11, 1999, pp. 1012-1017.

 
 
Top