Sustained release of the candidate antiretroviral peptides T-1249 and JNJ54310516-AFP from a rod insert vaginal ring

Drug Delivery and Translational Research
Diarmaid J MurphyR Karl Malcolm

Abstract

Administration of biomacromolecular drugs in effective quantities from conventional vaginal rings is hampered by poor drug permeability in the polymers from which rings are commonly constructed. Here, we report the formulation development and testing of rod insert rings for sustained release of the candidate antiretroviral peptides T-1249 and JNJ54310516-AFP (JNJ peptide), both of which have potential as HIV microbicides. Rod inserts were prepared comprising antiviral peptides T-1249 or JNJ peptide in combination with a hydrophilic excipient (sodium chloride, sodium glutamate, lactose or zinc acetate) dispersed at different loadings within a medical grade silicone elastomer. The inserts were tested for weight change and swelling when immersed in simulated vaginal fluid (SVF). Dye migration into the inserts was also assessed visually over 28 days. In vitro release of T-1249 and JNJ peptide from rings containing various insert types was tested. Weight change and degree of swelling of rods immersed in SVF was dependent on the type and concentration of excipient present. The rods displayed the following rank order in terms of weight change: sodium glutamate > zinc acetate ≈ sodium chloride > lactose. The weight change and degree of...Continue Reading

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Citations

Jul 31, 2016·International Journal of Pharmaceutics·Peter BoydR Karl Malcolm
Aug 9, 2017·Antimicrobial Agents and Chemotherapy·John W McBrideR Karl Malcolm
Oct 1, 2018·Advanced Therapeutics·Burcin YavuzDavid L Kaplan
Jun 30, 2021·Advanced Drug Delivery Reviews·Sai Archana KroviAriane van der Straten
Jul 20, 2021·Advanced Drug Delivery Reviews·José das NevesBruno Sarmento

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