ReportDrug Delivery

A once-a-month oral contraceptive

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Science Translational Medicine  04 Dec 2019:
Vol. 11, Issue 521, eaay2602
DOI: 10.1126/scitranslmed.aay2602
  • Fig. 1 Concept and in vitro characterization of an oral, long-acting contraceptive.

    (A) Schematic design of the oral gastric resident dosage form. The dosage form can be loaded with levonorgestrel (LNG) and folded into a capsule for ingestion; the dosage form recoils upon dissolution of the capsule in the stomach. (B) Various designs for the arms. The V-shaped arm was used to load drug matrices made of poly(sebacic anhydride). Poly(dimethylsiloxane) (PDMS)–based matrices were loaded in the caged arm. The “slotted arm” design was used because of the higher surface area. The slotted arm design showed higher fracture force than V-shaped arms (n = 6; *P < 0.05, Student’s t test). (C) Flexural strength of the Sorona 3015G NC010 arms when incubated in simulated gastric fluid (SGF) for 4 weeks, evaluated using a three-point bending test. Circles represent individual measurements. *P < 0.05, one-way analysis of variance (ANOVA) and post hoc Bonferroni. (D) The interface between Sorona 3015G NC010 (arms) and Elastollan 1185A10 (elastomeric core) polymers was evaluated using a cyclic cantilever test. The number of samples remaining intact after 500 cycles is shown. Three samples were evaluated at each time point. (E) Stability of levonorgestrel in SGF at 37°C evaluated using high-performance liquid chromatography. Circles represent individual measurements (n = 5). Release of levonorgestrel from matrices made of (F) poly(sebacic anhydride) and (G) PDMS in SGF over 4 weeks. Drug loading ranged from 12.5 to 50%. Circles represent individual measurements, and the line indicates average drug release (n = 5 to 6).

  • Fig. 2 Oral pharmacokinetics of levonorgestrel tablet and gastric resident dosage form in pigs.

    The serum concentrations of levonorgestrel when administered as (A) tablet (n = 5), (B) long-acting formulation–1 (n = 3), and (C) long-acting formulation–2 (n = 3). Dark lines indicate average serum concentrations, and dotted lines show serum concentrations for individual animals. (D) X-ray images showing gastric resident dosage forms containing long-acting formulation–2 loaded with metallic beads as x-ray contrast agent.

Supplementary Materials

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    • Materials and Methods
    • Fig. S1. Image of gastric resident dosage form.
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