Dataset Information

Sunscreen-Based Photocages for Topical Drugs: A Photophysical and Photochemical Study of A Diclofenac-Avobenzone Dyad.

ABSTRACT: Photosensitization by drugs is a problem of increasing importance in modern life. This phenomenon occurs when a chemical substance in the skin is exposed to sunlight. Photosensitizing drugs are reported to cause severe skin dermatitis, and indeed, it is generally advised to avoid sunbathing and to apply sunscreen. In this context, the nonsteroidal anti-inflammatory drug (NSAID) diclofenac is a photosensitive drug, especially when administered in topical form. In this work, efforts have been made to design and study an innovative pro-drug/pro-filter system containing diclofenac and the UVA filter avobenzone in order to develop a safer use of this topical drug. The design is based on the presence of a well-established photoremovable phenacyl group in the avobenzone structure. Steady-state photolysis of the dyad in hydrogen-donor solvents, monitored by UV-Vis spectrophotometry and HPLC, confirms the simultaneous photorelease of diclofenac and avobenzone. Laser flash photolysis and phosphorescence emission experiments allow us to gain insight into the photoactive triplet excited-state properties of the dyad. Finally, it is shown that avobenzone provides partial photoprotection to diclofenac from photocyclization to carbazole derivatives.

SUBMITTER: Aparici-Espert I

PROVIDER: S-EPMC6017856 | biostudies-other | 2018 Mar

REPOSITORIES: biostudies-other

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Sunscreen-Based Photocages for Topical Drugs: A Photophysical and Photochemical Study of A Diclofenac-Avobenzone Dyad.

Aparici-Espert Isabel I Miranda Miguel A MA Lhiaubet-Vallet Virginie V

Molecules (Basel, Switzerland) 20180316 3

Photosensitization by drugs is a problem of increasing importance in modern life. This phenomenon occurs when a chemical substance in the skin is exposed to sunlight. Photosensitizing drugs are reported to cause severe skin dermatitis, and indeed, it is generally advised to avoid sunbathing and to apply sunscreen. In this context, the nonsteroidal anti-inflammatory drug (NSAID) diclofenac is a photosensitive drug, especially when administered in topical form. In this work, efforts have been made ...[more]

PMID: 29547525

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Project description:ObjectivesTo determine if a topically applied non-steroidal anti-inflammatory drug (diclofenac) can provide short-term pain relief for chronic Achilles tendinopathy (CAT), in order to inform the development of a new rehabilitation protocol.Design and settingPilot double-blind, cross-over randomised controlled trial providing participants with tertiary care. The study was conducted at a single research centre in Vancouver, BC.ParticipantsSixteen adults with unilateral CAT and three adults with bilateral CAT participated.InterventionsParticipants received two successive treatments (10% diclofenac gel or placebo gel) in random order over a 3-day period. There was a 1-week washout period between the treatments. Allocation was by simple randomisation, and the participants as well as the assessing/treating researcher were blinded to treatment allocation.Outcome measuresThe primary outcome measure was pain level (0-10) during tendon loading (hopping). Secondary outcome measures included pain at rest, pressure pain threshold of the Achilles tendon and symptom improvement.ResultsNineteen adults participated in the study, and all were included in the analysis. Diclofenac gel significantly reduced the average pain during tendon loading (p<0.001) and at rest (p=0.031). The average baseline hopping pain was 4.8/10 (95% CI 3.92?to 5.68) and was reduced to 3.1/10 (2.35-3.85) by diclofenac. Pain at rest was decreased and pressure pain threshold increased with diclofenac treatment, but not with placebo gel. There were no observed or reported side effects of either treatment.ConclusionsIn this small, short-term study, diclofenac was able to improve symptoms and reduce pain during tendon loading in participants with CAT, whereas placebo gel was not. A future study of diclofenac as a supplement to rehabilitation, with longer follow-up and powered to detect a difference between diclofenac and placebo, is indicated.Trial registrationISRCTN60151284, http://www.isrctn.com/ISRCTN60151284 ETHICS: UBC Clinical Research Ethics Board approval was obtained for this research. The certificate number of the ethics certificate of approval to conduct research is H15-00999.

Dataset Information

Sunscreen-Based Photocages for Topical Drugs: A Photophysical and Photochemical Study of A Diclofenac-Avobenzone Dyad.

Publications

Sunscreen-Based Photocages for Topical Drugs: A Photophysical and Photochemical Study of A Diclofenac-Avobenzone Dyad.

Similar Datasets

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