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Related Experiment Videos

Topical delivery of retinyl ascorbate co-drug. 5. In vitro degradation studies.

K Abdulmajed1, C McGuigan, C M Heard

  • 1Welsh School of Pharmacy, Cardiff University, Cardiff, UK.

Skin Pharmacology and Physiology
|June 17, 2006
PubMed
Summary

Fresh skin extracts showed higher protein and esterase activity than stored extracts, with retinyl ascorbate (RA-AsA) hydrolysis slowed by antioxidants. This impacts drug stability and delivery research.

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Area of Science:

  • Biochemistry
  • Dermatology
  • Pharmacology

Background:

  • Retinyl ascorbate (RA-AsA) is a co-drug of retinoic acid (vitamin A) and ascorbic acid (vitamin C).
  • Understanding the hydrolysis of RA-AsA is crucial for its stability and efficacy in pharmaceutical applications.
  • Porcine ear skin and liver esterase are relevant models for studying drug metabolism and skin penetration.

Purpose of the Study:

  • To investigate the chemical and enzymatic hydrolysis of retinyl ascorbate (RA-AsA).
  • To compare the esterase activity and protein content in fresh versus stored porcine ear skin extracts.
  • To assess the impact of antioxidants on RA-AsA stability and hydrolysis.

Main Methods:

  • Determined protein and ester hydrolysis activity in crude cellular extracts from fresh and stored porcine ear skin using ethyl butyrate.

Related Experiment Videos

  • Assessed RA-AsA stability in crude extracts with and without added antioxidants.
  • Studied enzymatic hydrolysis of RA-AsA and retinyl-2-carboxy-2-hydroxy-ethanoate using porcine liver esterase.

    • Main Results:

    • Freshly excised porcine skin contained significantly higher amounts of active proteins (0.06 mg cm(-2)) compared to stored skin (0.01 mg cm(-2)).
    • RA-AsA underwent hydrolytic reduction, with the ascorbic acid moiety disintegrating due to free radicals, forming an intermediate cleaved by enzymes.
    • Addition of ascorbic acid as an antioxidant decelerated the hydrolysis rate of RA-AsA.

    Conclusions:

    • Fresh porcine skin exhibits higher enzymatic activity than stored skin, influencing the stability of co-drugs like RA-AsA.
    • Free radicals contribute to the disintegration of the ascorbic acid component in RA-AsA.
    • Antioxidants, such as ascorbic acid, can mitigate the hydrolysis of RA-AsA, suggesting implications for formulation and delivery strategies.