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Question: Describe in detail the five main strategies for microneedle-enhanced transdermal drug delivery: Poke and patch, coat and poke, dissolving microneedles, hollow microneedles and hydrogel-forming microneedles.

10 Oct 2022,9:11 PM

 

  • VIADUR® was previously marketed as a sterile, nonbiodegradable, single-use, titanium implant designed to continuously deliver leuprolide acetate (a gonadotropin releasing hormone drug) at a constant rate over one year for the treatment of advanced prostate cancer. The design of the VIADUR® implant device is shown in Figure A.

 

 

The in vivo performance of the implant was evaluated in rats. After different periods of implantation (3, 6, 9, and 12 months), the implants were removed from the rats and the residual drug content measured using high-performance liquid chromatography.

 

In vitro release from the implants was evaluated by placing individual implants in test tubes containing phosphate buffered saline with 2% sodium azide as preservative. Test tubes were maintained in a water bath at 37 °C, and samples of the release medium were sampled periodically.

 

In vitro cumulative release data was then plotted against in vivo cumulative data; the data is presented in Figure B.

 

Figure B. Cumulative in vitro release of leuprolide acetate from VIADUR® implants versus cumulative in vivo release (in rats) for four different timepoints (3, 6, 9, and 12 months).

 

  1. What level of in vitro-in vivo correlation (IVIVC) does the data is Figure B represent?

[10%]

 

  1. Based on the data presented in Figure B, determine the cumulative amount of leuprolide acetate released in vivo after 6 months implantation in rats.

[10%]

 

  • Based on your answer to Part B (or otherwise), determine the daily release rate of the VIADUR® implant. You must show your working.

[10%]

 

  1. In 2016, Kimball et al. reported a matrix-type vaginal ring device for sustained vaginal administration of leuprolide acetate. How might the release of leuprolide acetate from the ring device compare with the VIADUR® implant?

[20%]

 

 

 

  • Describe in detail the five main strategies for microneedle-enhanced transdermal drug delivery: Poke and patch, coat and poke, dissolving microneedles, hollow microneedles and hydrogel-forming microneedles.

[50%]

Expert answer

 

There are five main strategies for microneedle-enhanced transdermal drug delivery:

 

1. Poke and patch: This strategy involves using a sharp object, such as a needle, to puncture the skin and create a small opening. The patch is then applied over the top of the opening to deliver the medication.

 

2. Coat and poke: This strategy involves coating the microneedles with the medication before piercing the skin. Once the microneedles are in place, they release the medication into the body.

 

3. Dissolving microneedles: These microneedles are made of materials that dissolve once they come into contact with body fluids. As they dissolve, they release the medication into the body.

 

4. Hollow microneedles: These microneedles have a hollow center that can be filled with medication. Once the microneedles are in place, the medication is released into the body.

 

5. Hydrogel-forming microneedles: These microneedles are made of materials that form a gel once they come into contact with body fluids. The gel helps to hold the medication in place and release it over time.

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