Research Article

Drug Delivery and Translational Research

, Volume 2, Issue 2, pp 106-111

First online:

Evaluation of a perforated drug delivery system in mice for prolonged and constant release of a hydrophilic drug

  • Ashish RastogiAffiliated withUS Army Institute of Surgical ResearchDivision of Pharmaceutics, College of Pharmacy, The University of Texas at Austin
  • , Phillip D. BowmanAffiliated withUS Army Institute of Surgical ResearchUS Army Institute of Surgical Research Email author 
  • , Salomon StavchanskyAffiliated withDivision of Pharmaceutics, College of Pharmacy, The University of Texas at Austin Email author 

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Abstract

A drug delivery system (DDS) consisting of a perforated microtube (polyimide, inside diameter = 1.8 mm, tube length = 20 mm, hole size = 0.15 mm) was characterized in vitro and in vivo for its usefulness for long-term release of hydrophilic drugs at a constant rate. Sodium fluorescein mixed with stearic acid was used as the model drug. The DDS was packed with sodium fluorescein and stearic acid in ratios of 50:50, 40:60, and 25:75, respectively, and in vitro drug release studies were performed in saline. Linear release rates with R 2 > 0.9700 were obtained for all groups. Release rates of 1,077.3 ± 264.6, 342.6 ± 146.4, and 14.4 ± 7.0 μg/day for sodium fluorescein were obtained from the three groups, respectively. After monitoring the in vitro release of fluorescein for 11 days, 7 tubes from the 40:60 group were implanted subcutaneously in each individual mice to study the in vivo release of fluorescein from the tubes by measuring the fluorescein in the urine for 84 days. An initial rapid release during the first 4 days was followed by a near zero order fluorescence from the tubes (R 2 = 0.9870). Following completion of the study, the DDSs were retrieved for histology. Morphological analysis indicated no clinical adverse reaction at the site of device implantation specific to the device. The DDS was found to be biocompatible and capable of long-term constant release of a hydrophilic drug such as sodium fluorescein.

Keywords

Drug delivery system Microholes Stearic acid Sodium fluorescein Controlled release