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Skin and Mucosal Delivery (Focus Group – SMD)

Long-Acting Microneedle Delivery of a Novel Rilpivirine Coamorphous Phase

Ryan Donnelly – Professor, Queen's University Belfast; Maria Galleri – PhD Candidate, Queen's University Belfast; Qonita Anjani – Post Doctoral Researcher, Queen's University Belfast; Octavio Fandiño – Post Doctoral Researcher, Queen's University Belfast
Introduction:

The poor aqueous solubilities (Sw) of new chemical entities is a major drawback in the drug development pipeline [1]. Rilpivirine (RPV) like other antiretroviral agents, possesses a poor Sw [2]. In the context of microneedle (MN) drug delivery, a poor Sw is a major hinderance to the drug delivery efficiency. Herein, coamorphous systems have been employed to combat this barrier to enable the efficient delivery of RPV into the skin, whereby the temporary solubility enhancement effects are halted via disproportionation of RPV and coformer, to enable a long-acting delivery, due to a depot effect.

Learning Objectives:

  • Understand the rationale for using coamorphous systems to enhance the Sw of drugs for microneedle delivery
  • Explain the process of coformer selection, and mechanical/dermatokinetic evaluation used to develop microneedles
  • Evaluate how coamorphous systems and disproportionation allow enhanced delivery efficiency and dermal deposition