Topically used corticosteroids: What is the big picture of drug product degradation?

Heugten, A.J.P. van; Boer, Wiebe de; Vries, Wouter S. de; Pieters, Roland J.; Vromans, Herman

doi:10.1016/j.ejps.2018.02.001

Cited by 2 publications

(2 citation statements)

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“…With regard to the literature, the main degradation pathways of glucocorticoids in the presence of water and oxygen containing a C-17 dihydroxacetone side chain such as HC and DEX are proposed to be via the oxidative and hydrolytic reactions of the C-17 side chain, with oxidative degradation being strongly catalyzed by trace metal ions such as copper or iron [ 82 , 83 , 84 ]. The complexation of these trace metal ions by chelating agents such as EDTA is a well-described means to inhibit the degradation of these glucocorticoids, which ties well with the observed results [ 82 , 85 , 86 ].…”

Section: Resultsmentioning

confidence: 99%

“…In conclusion, the generally good stability of HC and DEX can be increased by controlled storage at lower temperatures or the addition of metal complexing agents such as EDTA. Although we hypothesize that a combination of controlled, low-temperature storage with EDTA leads to long-term drug stability which is beneficial for a stable and effective product, future studies should evaluate the chemical stability for periods longer than 90 days, the influence of possible degradation products on the biocompatibility and toxicity [ 82 , 83 , 84 ] of the formulations and the effects of excipients on drug permeation and wound healing.…”

Section: Resultsmentioning

confidence: 99%

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Exploring Microemulsion Systems for the Incorporation of Glucocorticoids into Bacterial Cellulose: A Novel Approach for Anti-Inflammatory Wound Dressings

Zahel,

Bruggink,

Hülsmann

et al. 2024

Pharmaceutics

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The effective pharmacological treatment of inflamed wounds such as pyoderma gangraenosum remains challenging, as the systemic application of suitable drugs such as glucocorticoids is compromised by severe side effects and the inherent difficulties of wounds as drug targets. Furthermore, conventional semi-solid formulations are not suitable for direct application to open wounds. Thus, the treatment of inflamed wounds could considerably benefit from the development of active wound dressings for the topical administration of anti-inflammatory drugs. Although bacterial cellulose appears to be an ideal candidate for this purpose due to its known suitability for advanced wound care and as a drug delivery system, the incorporation of poorly water-soluble compounds into the hydrophilic material still poses a problem. The use of microemulsions could solve that open issue. The present study therefore explores their use as a novel approach to incorporate poorly water-soluble glucocorticoids into bacterial cellulose. Five microemulsion formulations were loaded with hydrocortisone or dexamethasone and characterized in detail, demonstrating their regular microstructure, biocompatibility and shelf-life stability. Bacterial cellulose was successfully loaded with the formulations as confirmed by transmission electron microscopy and surprisingly showed homogenous incorporation, even of w/o type microemulsions. High and controllable drug permeation through Strat-M® membranes was observed, and the anti-inflammatory activity for permeated glucocorticoids was confirmed in vitro. This study presents a novel approach for the development of anti-inflammatory wound dressings using bacterial cellulose in combination with microemulsions.

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