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. Author manuscript; available in PMC: 2020 Aug 7.
Published in final edited form as: Adv Ther (Weinh). 2018 Jul 29;1(6):1800054. doi: 10.1002/adtp.201800054

Table 6.

Delivery formats for anti-HIV microbicides.[209]

Delivery format Advantages Limitations
Gels (semi-solid), rectal and vaginal
  • Greater ease of formulation and manufacture, lower cost of production

  • Ease of administration by the user

  • Rapid dispersal of the active compound, conferring protection shortly after placement

  • High localized drug concentrations can be attained

  • Additional functionality as a lubricant for sexual intercourse

  • Timing of device application is coitally dependent

  • Limited duration of retention at the site of application, requiring more frequent dosing

  • Leakage and potential user discomfort

  • Vulnerability of active compounds to extremes of temperatures and humidity

Vaginal tablets and films
  • Rapid release of the active compound, providing protection shortly after placement

  • Precise, consistent dosing

  • Lower manufacturing costs

  • Ease of application by the user

  • Improved stability of active compounds to extreme temperatures and humidity

  • Timing of device application is coitally dependent

  • Shorter retention time of active compounds in the site of application, requiring more frequent dosing

  • For films, their low overall mass limits the amount of active compound that can be incorporated into a single dose

Vaginal rings (VRs)
  • Sustained release of the microbicide over weeks or months, requiring less frequent user intervention

  • Timing of device application is coitally independent

  • Increased complexity of manufacture and production costs

  • User discomfort with device insertion/removal

  • Only useful for the vaginal (and not rectal) compartment

Nanoparticles (NPs)
  • Protection and stabilization of active compounds against degradation

  • Enhanced solubilization of incorporated active compounds

  • Permeation through cervicovaginal mucus to better reach HIV susceptible sites in the epithelium

  • Increased complexity of manufacture and production costs

  • Clinical safety and efficacy studies are still needed

Electrospun fibers (EFs)
  • Dry, solid dosage form that can stabilize drugs that may be less stable in a liquid format

  • Base polymers used are often mucoadhesive, potentially increasing

  • residence time of the microbicide at the site of application

  • Increased complexity of manufacture, low manufacturing production capacity at present, thus higher cost per dose

  • Clinical safety and efficacy studies are still needed

Live microbicides (commensals)
  • Sustained release of the microbicide

  • over weeks, months, or longer, requiring less frequent user intervention

  • Timing of device application is coitally independent

  • Lactobacilli themselves may positively impact the vaginal mucosal environment

  • Long-term clinical data are still needed to demonstrate safety and efficacy

  • Limited to delivery of biologic microbicides that can be stably

  • expressed in bacteria

  • User concern about GMOs

GMOs, genetically modified organisms.