Skin Permeation of Rosiglitazone from Transdermal Matrix Patches - Pharmaceutical Technology

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Skin Permeation of Rosiglitazone from Transdermal Matrix Patches
The authors demonstrate that sustained-release delivery can help avoid the risk of sudden higher-blood concentration of a drug to avoid toxicity.


Pharmaceutical Technology
Volume 34, Issue 5, pp. 56-72


Figure 9
Drug release from the experimental patches and subsequent penetration through the skin reached a drug concentration in human plasma of 106.45 ng/mL after 2 h, 258.36 ng/mL after 4 h, 460.08 ng/mL after 8 h, 232.63 ng/mL after 24 h, and 143.24 ng/mL after 48 h. The maximum concentration of the drug (C max) in plasma was 460.08 ng/mL, and this level was reached in 8 h (T max) (see Figure 9). An important limitation of the present study is that it was conducted only at a few predetermined time points, as permitted by the Institutional Ethics Committee, and based on those time points the C max and T max data were calculated. However, values might have varied if more time points had been considered. Thus, these results depict only the trend of drug skin-permeation patterns in humans, and the C max and T max of the formulations might not be accurate. The variation in drug concentration in the plasma among the volunteers may result from various factors such as variation in skin type and absorption characteristics. The study reveals that rosiglitazone can permeate through human skin and reach the blood circulation for at least 48 h from formulated patches.

Moreover, currently available antidiabetic agents such as sulfonylureas, meglitinides, and D-phenylalanine derivatives increase β-cell insulin secretion. Biguanides reduce hepatic-glucose production, and glucosidase inhibitors decrease the intestinal absorption of carbohydrates and insulin (25). None of the currently available antidiabetic agents increases insulin sensitivity. Thus, a patient can use any of the above mentioned antidiabetic agents along with a transdermal patch of rosiglitazone to combat the glucose level in Type 2 diabetes mellitus effectively.

Conclusion

Rosiglitazone maleate can be formulated into transdermal matrix patches suitably using Duro-Tak 387-2516 and Duro-Tak 87-2852 pressure-sensitive adhesive polymers without using any gelling agent. Furthermore, sustained-release delivery can avoid the risk of sudden high blood concentration of drug to avoid toxicity, and a prolonged blood level of the drug is suitable for the treatment of Type 2 diabetic patients.

Acknowledgment

This work was funded by the All Indian Council of Technical Education, New Delhi, India, under the Quality Improvement Program for doctoral degrees.

N. Damodharan is a senior research fellow, Gopa Roy is a senior research fellow, Soma Ghosh is a research associate, and Biswajit Mukherjee* is a reader, all in the department of pharmaceutical technology at Jadavpur University, Kolkata -700 032, West Bengal, India, tel: +91 33 24146677, fax +91 33 24146677,
.

*To whom all correspondence should be addressed.

Submitted: Feb. 24, 2009. Accepted: Apr. 29, 2009.


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