Abstract
A key challenge of HIV treatment with multiple antiretroviral drugs is patient adherence. Thus, there is an urgent need for long-acting depot systems for delivering drugs over an extended duration. Although the parenteral route is preferred for depot systems, it is associated with obvious drawbacks, such as painful injections, potentially-contaminated sharps waste, and the necessity of trained healthcare personnel for administration. Amongst a small number of alternatives in development microneedles are versatile delivery systems enabling systemic drug delivery and potentially improving patient adherence due to their capacity for self-administration. We have developed dissolving microneedle (DMNs) embedded with etravirine nanosuspension (ETR NS) as a long-acting HIV therapy to improve patient adherence. The ETR NS prepared by sonoprecipitation yielded particle sizes of 764 ± 96.2 nm, polydispersity indices of of 0.23 ± 0.02, and zeta potentials of −19.75 ± 0.55 mV. The DMNs loaded with ETR NS demonstrated 12.84 ± 1.33% ETR deposition in ex-vivo neonatal porcine skin after 6 h application. In in vivo rat pharmacokinetic studies, the Cmax exhibited by DMNs loaded with ETR powder and ETR NS were 158 ± 10 ng/mL and 177 ± 30 ng/mL, respectively. DMN groups revealed a higher t1/2, Tmax, and mean residence time compared to intravenous ETR solutions, suggesting the long-acting potential of etravirine delivered intradermally using DMNs.
Highlights
Over 40 million people are infected with human ımmuno deficiency virus (HIV)
The parenteral route is preferred for depot systems, it is associated with obvious drawbacks, such as painful injections, potentiallycontaminated sharps waste, and the necessity of trained healthcare personnel for administration
We have developed dissolving microneedle (DMNs) embedded with etravirine nanosuspension (ETR Etravirine long-acting nanosuspension (NS)) as a long-acting HIV therapy to improve patient adherence
Summary
Over 40 million people are infected with human ımmuno deficiency virus (HIV). Etravirine (ETR) is the first second-generation non-nucleoside reverse transcriptase inhibitors (NNRTIs) marketed to treat NNRTI-resistant HIV-1 infection and has been approved for treat ment since 2008 [8]. It is active against the first generation NNRTI-resistant HIV-1. ETR is generally prescribed to a patient who shows evidence of active viral replication and harbors multidrug-resistant HIV-1 strains and who is already on other HIV medications, such as nevirapine, delavirdine, efavirenz that did not work well enough to control their HIV [8]. ETR has numerous disadvantages over the other anti-HIV drugs related to drug delivery, despite its use in the clinical
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callMore From: European Journal of Pharmaceutics and Biopharmaceutics
Disclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
