Design, Formulation, and Evaluation of Novel Dissolving Microarray Patches Containing Rilpivirine for Intravaginal Delivery

Design, Formulation, and Evaluation of Novel Dissolving Microarray Patches Containing Rilpivirine for Intravaginal Delivery

Antiretroviral (ARV) drugs have, for many years, been studied and administered in the prevention and treatment of human immunodeficiency virus (HIV). Intramuscular (IM) injection of long acting (LA) ARVs are in clinical development, but injectable formulations require regular access to healthcare fa...

Full description

Saved in:
Bibliographic Details
Published in:Advanced healthcare materials Vol. 8; no. 9; pp. e1801510 - n/a
Main Authors: Mc Crudden, Maelíosa T. C., Larrañeta, Eneko, Clark, Annie, Jarrahian, Courtney, Rein‐Weston, Annie, Creelman, Benjamin, Moyo, Yolanda, Lachau‐Durand, Sophie, Niemeijer, Nico, Williams, Peter, McCarthy, Helen O., Zehrung, Darin, Donnelly, Ryan F.
Format: Journal Article
Language:English
Published: Germany Wiley Subscription Services, Inc 01-05-2019
Subjects:
Animals
Antiretroviral agents
Antiretroviral drugs
Cattle
Drug Compounding
Drug delivery
Drug delivery systems
Epithelium
Evaluation
Female
Formulations
Health care
Health care facilities
HIV
HIV Infections - blood
HIV Infections - metabolism
Human immunodeficiency virus
In Vitro Techniques
In vivo methods and tests
Lymph Nodes - metabolism
Mechanical properties
Medical personnel
microarray patches
pre‐exposure prophylaxis
Rats
Rats, Sprague-Dawley
rilpivirine
Rilpivirine - administration & dosage
Rilpivirine - blood
Rilpivirine - pharmacokinetics
Skin
Tissues
Vagina
Vagina - metabolism
vaginal delivery
Viruses
Workers
pre-exposure prophylaxis
HIV
vaginal delivery
microarray patches
rilpivirine
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Antiretroviral (ARV) drugs have, for many years, been studied and administered in the prevention and treatment of human immunodeficiency virus (HIV). Intramuscular (IM) injection of long acting (LA) ARVs are in clinical development, but injectable formulations require regular access to healthcare facilities and disposal facilities for sharps. The development of a discrete, self‐administered, and self‐disabling vehicle to deliver ARVs could obviate these issues. This study describes the formulation, mechanical characterization, and in vivo evaluation of dissolving microarray patches (MAPs) containing a LA nanosuspension of the ARV, rilpivirine (RPV, RPV LA), for vaginal delivery. This is the first study to apply MAPs into vaginal tissue. The RPV LA MAPs penetrate ex vivo skin and a synthetic vaginal skin model and withstand the effects of potential dragging motion across synthetic vaginal epithelium. In in vivo studies, the mean plasma concentration of RPV in rats at the 56 day endpoint (116.5 ng mL−1) is comparable to that achieved in the IM control cohort (118.9 ng mL−1). RPV is detected systemically, in lymph and vaginal tissue, indicating the potential to deliver RPV LA to primary sites of viral challenge and replication. This innovative research has future potential for patients and healthcare workers, particularly in low‐resource settings. A study describing the design, formulation and characterisation of novel dissolving microarray patches (MAP) for vaginal delivery of a long acting nanosuspension of the antiretroviral (ARV) drug, rilpivirine (RPV). In an in vivo model, RPV is detected systemically, in lymph and vaginal tissue. This innovative delivery system could have wide ranging benefits for patients and healthcare workers in the future.
Bibliography:The copyright line for this article was changed on 2 April 2019 after original online publication.
ISSN:2192-2640
2192-2659
DOI:10.1002/adhm.201801510