Continuous drug release by sea anemone Nematostella vectensis stinging microcapsules

Transdermal delivery is an attractive option for drug delivery. Nevertheless, the skin is a tough barrier and only a limited number of drugs can be delivered through it. The most difficult to deliver are hydrophilic drugs. The stinging mechanism of the cnidarians is a sophisticated injection system...

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Bibliographic Details
Published in:Marine drugs 2014-01, Vol.12 (2), p.734-745
Main Authors: Tal, Yossi, Ayalon, Ari, Sharaev, Agnesa, Kazir, Zoya, Brekhman, Vera, Lotan, Tamar
Format: Article
Language:English
Subjects:
Administration, Cutaneous
Animals
Bites and Stings - metabolism
Capsules
Chemistry, Pharmaceutical - methods
cnidocyst
diffusion cell
Drug Delivery Systems
hydrophilic drug
Hydrophobic and Hydrophilic Interactions
Lidocaine - administration & dosage
Lidocaine - chemistry
Lidocaine - pharmacokinetics
Marine
Mice
Mice, Nude
Nematostella vectensis
Niacinamide - administration & dosage
Niacinamide - chemistry
Niacinamide - pharmacokinetics
Osmotic Pressure
Sea Anemones - chemistry
Skin - metabolism
Skin Absorption
transdermal
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Summary:Transdermal delivery is an attractive option for drug delivery. Nevertheless, the skin is a tough barrier and only a limited number of drugs can be delivered through it. The most difficult to deliver are hydrophilic drugs. The stinging mechanism of the cnidarians is a sophisticated injection system consisting of microcapsular nematocysts, which utilize built-in high osmotic pressures to inject a submicron tubule that penetrates and delivers their contents to the prey. Here we show, for the first time, that the nematocysts of the starlet sea anemone Nematostella vectensis can be isolated and incorporated into a topical formulation for continuous drug delivery. We demonstrate quantitative delivery of nicotinamide and lidocaine hydrochloride as a function of microcapsular dose or drug exposure. We also show how the released submicron tubules can be exploited as a skin penetration enhancer prior to and independently of drug application. The microcapsules are non-irritant and may offer an attractive alternative for hydrophilic transdermal drug delivery.
ISSN:1660-3397
1660-3397
DOI:10.3390/md12020734