EFFECT OF CHEMICAL ENHANCERS ON THE RELEASE OF GLIPIZIDE IN A MATRIX DISPERSION TRANSDERMAL SYSTEM
Glipizide is one of the most commonly prescribed drugs for treatment of type 2 diabetes.Â Â Oral therapy with Glipizide comprises problems of bioavailability fluctuations and may be associated with severe hypoglycaemia and gastric disturbances. As a potential for convenient, safe and effective antidiabetic therapy, the rationale of this study is to develop a transdermal delivery system for Glipizide in order to improve its therapeutic efficacy. Â In the preparation of films, chitosan was used as polymer. Inclusion complex of glipizide with Î²-Cyclodextrin was formed. The role of different permeation enhancers in the formulation was also studied. The films were characterized for thickness, tensile strength, drug content, moisture uptake, moisture content, and drug release. In vivo and skin irritation studies were performed for the optimized film.
Formulation F12 containing Chitosan (1.5percent w/v) and combination of permeation enhancers (Oleic acid: ethanol 1:1.5) showed the highest drug content 99.95percent and the drug release was 99.39percent in a period of 24 hours. The release data fitted into kinetic equations, yielded Higuchi plot and diffusion mechanism of drug release. The physical evaluation indicated the formation of smooth, flexible and translucent films. No skin irritation occurred on rat skin and the infrared studies showed the compatibility of the drug with the formulation excipients. The ex vivo study revealed a constant permeation of drug for long periods. The best permeation enhancer was F12 (Oleic acid: ethanol 1:1.5). The obtained results indicated the feasibility for transdermal delivery of Glipizide using Chitosan.
Glipizide, Diabetes, Transdermal Drug Delivery, Î²-cyclodextrin, Chitosan, in vitro permeation
2. Diagnosis and Classification of Diabetes Mellitus. American Diabetes Association. Diabetes Care 2012; s64-s71.
3. Tripathi KD. Essentials of medical pharmacology. Jaypee Brothers Medical Publishers; 2010.p. 254-55, 62-63, 70-72.
4. Standards of medical care in Diabetes- 2012. American Diabetes Association. Diabetes Care 2012; s11-s63.
5. Shankar S.J, Varalakshmi C, Patel R, Manoj K. Development of a membrane controlled transdermal therapeutic system containing Glipizide. IJPRD 2011; 3(4): 131 â€“ 138.
6. Ramchandani U, Balakrishnan S. Development and evaluation of transdermal drug delivery system of ketoprofen drug with chitosan for treatment of Arthritis. EJAS 2012; 4(2):72-77.
7. Brunton LL, Chabner BA, Knollmann BC. Endocrine Pancreas and Pharmacotherapy of Diabetes Mellitus and Hypoglycemia. The pharmacological basis of therapeutics. 12th ed. New York: McGraw-Hill; 2010. Ch. 43.
8. Mutalik S, Udupa N, Kumar S, Agarwal S. Glipizide matrix transdermal systems for diabetes mellitus: preparation, in vitro and preclinical studies. Life Sci 2006; 79:1568-77.
9. Abdul Ahad H, Sreeramulu J, Hima Bindu V, Chitta Suresh Kumar, Kumar K, Reddy B, et al. A designing and in- vitro permeation studies of glipizide-ficus carica fruit mucilage and povidone transdermal patches. J Pharm Res 2010; 3(7):1583-86.
10. Vaseeha Banu TS, Som S, Khaleel M, Nirmal, Havannavar T. An approach to the formulation of transdermal film of Oxybutynin. Res J Pharm Bio Chem Sci 2010; 412-21.
11. Bhosale AV, Hardikar S, Jagtap RS, Patil NB, Sushant S, Dhawale SS. Formulation of Î²-Cyclodextrin complexed controlled release matrix tablet of Glipizide and its in vitro evaluation. Int J Pharm Res 2009; 1(3):773-8.
12. Ammar HO, Salama, Ghorab M, Nahas E, Elmotase. H. A transdermal delivery system for Glipizide. Curr Drug Del 2006; 3:333-41.
13. Bangale GS, Rathinaraj S, Rajesh KS, Gajanan V, Shinde, Deepak G. Design and evaluation of transdermal films of Atenolol. J Chem Pharm Res 2010; 2(3):593-604.
14. Ammar HO, Salama, Ghorab M, Nahas E, Elmotase H. Design and evaluation of chitosan films for transdermal delivery of Glimepiride. Curr Drug Del 2008; 5(4):290-98.
15. Nayak BS, Ellaiah P, Pattanayak D, Das S. Formuation design preparation and in vitro characterization of nebivolol transdermal patches. Asian J Pharm 2011; 5:175-182.
16. Jayachandran DL, Krishnamoorthy M, Jeganath S, Ashlin V, Sheeja Devi K. Formulation and characterization of transdermal films of Torasemide. IAJPR 2011;1(4):289-304.
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