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      Controlled delivery of the antiprotozoal agent (tinidazole) from intravaginal polymer matrices for treatment of the sexually transmitted infection, trichomoniasis.

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          Abstract

          Microporous polymeric matrices prepared from poly(ɛ-caprolactone) [PCL] were evaluated for controlled vaginal delivery of the antiprotozoal agent (tinidazole) in the treatment of the sexually transmitted infection, trichomoniasis. The matrices were produced by rapidly cooling co-solutions of PCL and tinidazole in acetone to -80 °C to induce crystallisation and hardening of the polymer. Tinidazole incorporation in the matrices increased from 1.4 to 3.9% (w/w), when the drug concentration in the starting PCL solution was raised from 10 to 20% (w/w), giving rise to drug loading efficiencies up to 20%. Rapid 'burst release' of 30% of the tinidazole content was recorded over 24 h when the PCL matrices were immersed in simulated vaginal fluid. Gradual drug release occurred over the next 6 days resulting in delivery of around 50% of the tinidazole load by day 7 with the released drug retaining antiprotozoal activity at levels almost 50% that of the 'non-formulated' drug in solution form. Basic modelling predicted that the concentration of tinidazole released into vaginal fluid in vivo from a PCL matrix in the form of an intravaginal ring would exceed the minimum inhibitory concentration against Trichomonas vaginalis. These findings recommend further investigation of PCL matrices as intravaginal devices for controlled delivery of antiprotozoal agents in the treatment and prevention of sexually transmitted infections.

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          Author and article information

          Journal
          Pharm Dev Technol
          Pharmaceutical development and technology
          Informa UK Limited
          1097-9867
          1083-7450
          Mar 2019
          : 24
          : 3
          Affiliations
          [1 ] a School of Medicine, The International Medical University , Kuala Lumpur , Malaysia.
          [2 ] b Dermatology Research Centre, School of Medicine , The University of Queensland, Translational Research Institute , Brisbane , Australia.
          [3 ] c School of Pharmacy , Monash University , Selangor , Malaysia.
          [4 ] d Department of Parasitology, Faculty of Medical Sciences , University of Sri Jayewardenepura , Nugegoda , Sri Lanka.
          [5 ] e ULTI Pharmaceuticals , Hamilton , New Zealand.
          Article
          10.1080/10837450.2018.1481430
          29799300
          1ad66254-2ac7-49e6-8274-727c6d423c55
          History

          sexually transmitted infection,Polycaprolactone,trichomoniasis,insert,intravaginal delivery,tinidazole

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