Dissolving polymer microneedle patches for rapid and efficient transdermal delivery of insulin to diabetic rats

作者：Ling Ming Hung; Chen Mei Chin^*

来源：Acta Biomaterialia, 2013, 9(11): 8952-8961.

DOI：10.1016/j.actbio.2013.06.029

• Bioavailability
• Bolus release
• Hypoglycemic effect
• Polysaccharide
• Protein delivery

This study presents a dissolving microneedle patch, composed of starch and gelatin, for the rapid and efficient transdermal delivery of insulin. The microneedles completely dissolve after insertion into the skin for 5 min, quickly releasing their encapsulated payload into the skin. A histological examination shows that the microneedles have sufficient mechanical strength to be inserted in vitro into porcine skin to a depth of approximately 200 mu m and in vivo into rat skin to 200-250 mu m depth. This penetration depth does not induce notable skin irritation or pain sensation. To evaluate the feasibility of using these dissolving microneedles for diabetes treatment insulin-loaded microneedles were administered to diabetic rats using a homemade applicator. Pharmacodynamic and pharmacokinetic results show a similar hypoglycemic effect in rats receiving insulin-loaded microneedles and a subcutaneous injection of insulin. The relative pharmacological availability and relative bioavailability of insulin were both approximately 92%, demonstrating that insulin retains its pharmacological activity after encapsulation and release from the microneedles. Storage stability analysis confirms that more than 90% of the insulin remained in the microneedles even after storage at 25 or 37 degrees C for 1 month. These results confirm that the proposed starch/gelatin microneedles enable stable encapsulation of bioactive molecules and have great potential for transdermal delivery of protein drugs in a relatively painless, rapid, and convenient manner.

• 出版日期2013-11