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 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.
StarletDerma Ltd., 8 HaEshel St., Caesarea 38900, Israel. Yossi@Starletderma.com.
Yossi
Y
Tal
StarletDerma Ltd., 8 HaEshel St., Caesarea 38900, Israel. Ari@Starletderma.com.
Ari
A
Ayalon
StarletDerma Ltd., 8 HaEshel St., Caesarea 38900, Israel. agnesa@starletderma.com.
Agnesa
A
Sharaev
StarletDerma Ltd., 8 HaEshel St., Caesarea 38900, Israel. zoya@starletderma.com.
Zoya
Z
Kazir
Marine Biology Department, The Leon H.Charney School of Marine Sciences, University of Haifa, Mount Carmel, Haifa 31905, Israel. vbrekhman@univ.haifa.ac.il.
Vera
V
Brekhman
Marine Biology Department, The Leon H.Charney School of Marine Sciences, University of Haifa, Mount Carmel, Haifa 31905, Israel. lotant@univ.haifa.ac.il.
Tamar
T
Lotan
D000279:Administration, Cutaneous; D000818:Animals; D001733:Bites and Stings / Q000378:metabolism; D002214:Capsules; D002626:Chemistry, Pharmaceutical / Q000379:methods; D016503:Drug Delivery Systems; D057927:Hydrophobic and Hydrophilic Interactions; D008012:Lidocaine / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D051379:Mice; D008819:Mice, Nude; D009536:Niacinamide / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D009997:Osmotic Pressure; D012615:Sea Anemones / Q000737:chemistry*; D012867:Skin / Q000378:metabolism; D012869:Skin Absorption
D002214:Capsules; D009536:Niacinamide; D008012:Lidocaine