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. 2021 Dec;14(12 Suppl 1):S18–S23.

TABLE 1.

Comparison of isotretinoin formulations

FORMULATION STANDARD ISOTRETINOIN LIDOSE ISOTRETINOIN MICRONIZED ISOTRETINOIN
Novel features of technology Use a conventional delivery system isotretinoin, a form of retinoid, by targeting all components involved in the development of acne30
  • Presolubilized (in a lipid matrix)

  • Encapsulated carrier with a hard gelatin capsule + active drug + lipid excipients29

  • Lipid carrier system

  • Particle reduction to micrometer (µm) size or nanostructured

  • Superior solubility and absorption31

Advantages
  • Revolutionized the treatment of acne

  • Used widely as an effective oral therapy for severe, recalcitrant nodular acne5

  • Significantly greater intestinal solubilization

  • Faster absorption

  • Greater bioavailability

  • Less food dependency8

  • Faster dissolution

  • Prolonged drug release

  • Most bioavailable without food7

  • Achieves therapeutic blood levels at a 20% lower dose 7

Limitations or challenges
  • Low solubility and bioavailability

  • Food-dependent absorption26

Complex formulation Complex formulation requiring improved nanotechnology
Bioavailability 25% (reported)40 Approximately 2 times higher in fasting state compared with standard isotretinoin8 Micronized isotretinoin 32mg is absorbed approximately twice as well as lidose isotretinoin 40mg in fasted patients7
Recommended dosing regimen 0.5–1.0 mg/kg/day, in 2 divided doses with food to a cumulative dose of 120–150 mg/kg5 0.5–1.0 mg/kg/day given in 2 divided doses without regard to meals34 0.4–0.8 mg/kg/day in 2 divided doses without regard to meals34

AE: adverse event;