Risha Bellomo1, Matthew Brunner1, Ella Tadjally1. 1. Dr. Bellomo is with Allele Medical, in Orlando, Florida. Dr Brunner is with the Dermatology & Skin Surgery Center P.C., in Stockbridge, Georgia.
Abstract
Background: Isotretinoin is a widely used and effective drug in the treatment of severe, recalcitrant, nodular acne. However, its poor aqueous solubility limits oral bioavailability and requires administration with a high-fat, high-calorie meal (HF/HC) for optimal absorption; poor patient adherence may decrease effective dosing and treatment efficacy. Objective: This review covers the properties of the lidose isotretinoin and micronized isotretinoin formulations and their use in acne therapy. Method of Literature Search: PubMed was searched using the terms acne, isotretinoin, formulations, isotretinoin efficacy, and safety. Additional articles were searched using reference lists from the obtained results. Results: Our review discusses pathology and approved treatment options for acne; provides mechanism of action of isotretinoin; presents clinical challenges associated with isotretinoin safety; and summarizes implications in clinical practice. Newer formulations show enhanced bioavailability in both fed and fasting states. Limitations: Few published studies of real-world use of the identified formulations were available. Conclusion: Newer drug delivery technologies can simplify isotretinoin use while maximizing bioavailability and efficacy. Based on our analysis, lidose isotretinoin and micronized isotretinoin improve oral bioavailability, pharmacological bioactivity, and increase therapeutic efficacy in patients who are unwilling or unable to consistently take the medication with an HF/HC meal. Healthcare providers should consider these formulations as tools to optimize treatment based on each patient's individual needs.
Background: Isotretinoin is a widely used and effective drug in the treatment of severe, recalcitrant, nodular acne. However, its poor aqueous solubility limits oral bioavailability and requires administration with a high-fat, high-calorie meal (HF/HC) for optimal absorption; poor patient adherence may decrease effective dosing and treatment efficacy. Objective: This review covers the properties of the lidose isotretinoin and micronized isotretinoin formulations and their use in acne therapy. Method of Literature Search: PubMed was searched using the terms acne, isotretinoin, formulations, isotretinoin efficacy, and safety. Additional articles were searched using reference lists from the obtained results. Results: Our review discusses pathology and approved treatment options for acne; provides mechanism of action of isotretinoin; presents clinical challenges associated with isotretinoin safety; and summarizes implications in clinical practice. Newer formulations show enhanced bioavailability in both fed and fasting states. Limitations: Few published studies of real-world use of the identified formulations were available. Conclusion: Newer drug delivery technologies can simplify isotretinoin use while maximizing bioavailability and efficacy. Based on our analysis, lidose isotretinoin and micronized isotretinoin improve oral bioavailability, pharmacological bioactivity, and increase therapeutic efficacy in patients who are unwilling or unable to consistently take the medication with an HF/HC meal. Healthcare providers should consider these formulations as tools to optimize treatment based on each patient's individual needs.
Authors: Parinitha K Rao; Ramesh M Bhat; B Nandakishore; Sukumar Dandakeri; Jacintha Martis; Ganesh H Kamath Journal: Indian J Dermatol Date: 2014-05 Impact factor: 1.494