Transdermal anti-inflammatory activity of bilayer film containing olive compound hydroxytyrosol

physical assessment, in vivo dermal safety and efficacy study in Freund’s adjuvant-induced arthritic rat model

Shiow Fern Ng, Leong Seng Tan, Fhataheya Buang

Research output: Contribution to journalArticle

10 Citations (Scopus)

Abstract

Previous studies have shown that hydroxytyrosol (HT) can be a potential alternative therapeutic agent for the treatment of rheumatoid arthritis (RA). However, HT is extensively metabolized following oral administration, which leads to formulating HT in a topical vehicle to prolong drug action as well as to provide a localized effect. Hidrox-6 is a freeze-dried powder derived from fresh olives and contains a high amount of HT (∼3%) and other polyphenols. Alginate bilayer films containing 5% and 10% Hidrox-6 were formulated. The films were characterized with respect to their physical, morphology, rheological properties; drug content uniformity; and in vitro drug release. Acute dermal irritancy tests and a skin sensitization study were carried out in rats. An efficacy study of the bilayer films for RA was conducted using Freund’s adjuvant-induced polyarthritis rats. Animal data showed that the bilayer film formulations did not cause skin irritancy. The efficacy in vivo results showed that the Hidrox-6 bilayer films lowered the arthritic scores, paw and ankle circumference, serum IL-6 level and cumulative histological scores compared with those measured for controls. The topical Hidrox-6 bilayer films improve synovitis and inflammatory symptoms in RA and can be a potential alternative to oral RA therapy.

Original languageEnglish
Pages (from-to)1-12
Number of pages12
JournalDrug Development and Industrial Pharmacy
DOIs
Publication statusAccepted/In press - 2 Sep 2016

Fingerprint

Experimental Arthritis
Freund's Adjuvant
Olea
Rats
Rheumatoid Arthritis
Anti-Inflammatory Agents
Safety
Skin
Skin Irritancy Tests
Arthritis
Synovitis
Polyphenols
Ankle
Pharmaceutical Preparations
Powders
Oral Administration
Interleukin-6
Therapeutics
3,4-dihydroxyphenylethanol
Animals

Keywords

  • alginate
  • bilayer film
  • Freund’s adjuvant-induced rats
  • Hidrox
  • Hydroxytyrosol
  • rheumatoid arthritis

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Cite this

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title = "Transdermal anti-inflammatory activity of bilayer film containing olive compound hydroxytyrosol: physical assessment, in vivo dermal safety and efficacy study in Freund’s adjuvant-induced arthritic rat model",
abstract = "Previous studies have shown that hydroxytyrosol (HT) can be a potential alternative therapeutic agent for the treatment of rheumatoid arthritis (RA). However, HT is extensively metabolized following oral administration, which leads to formulating HT in a topical vehicle to prolong drug action as well as to provide a localized effect. Hidrox-6 is a freeze-dried powder derived from fresh olives and contains a high amount of HT (∼3{\%}) and other polyphenols. Alginate bilayer films containing 5{\%} and 10{\%} Hidrox-6 were formulated. The films were characterized with respect to their physical, morphology, rheological properties; drug content uniformity; and in vitro drug release. Acute dermal irritancy tests and a skin sensitization study were carried out in rats. An efficacy study of the bilayer films for RA was conducted using Freund’s adjuvant-induced polyarthritis rats. Animal data showed that the bilayer film formulations did not cause skin irritancy. The efficacy in vivo results showed that the Hidrox-6 bilayer films lowered the arthritic scores, paw and ankle circumference, serum IL-6 level and cumulative histological scores compared with those measured for controls. The topical Hidrox-6 bilayer films improve synovitis and inflammatory symptoms in RA and can be a potential alternative to oral RA therapy.",
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