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Molecules 2017, 22(5), 836; doi:10.3390/molecules22050836

Emulsion-Based Intradermal Delivery of Melittin in Rats

1
Rural Development Administration, National Academy of Agricultural Science, Wanju, Chonbuk 55365, Korea
2
School of Biomedical Sciences, Charles Sturt University, Bathurst, NSW 2795, Australia
*
Author to whom correspondence should be addressed.
Academic Editor: Philippe Bulet
Received: 14 March 2017 / Revised: 16 May 2017 / Accepted: 16 May 2017 / Published: 19 May 2017
(This article belongs to the Special Issue Bioactive Natural Peptides As A Pipeline For Therapeutics)
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Abstract

Bee venom (BV) has long been used as a traditional medicine. The aim of the present study was to formulate a BV emulsion with good rheological properties for dermal application and investigate the effect of formulation on the permeation of melittin through dermatomed rat skin. A formulated emulsion containing 1% (w/v) BV was prepared. The emulsion was compared with distilled water (DW) and 25% (w/v) N-methyl-2-pyrrolidone (NMP) in DW. Permeation of melittin from aqueous solution through the dermatomed murine skin was evaluated using the Franz diffusion cells. Samples of receptor cells withdrawn at pre-determined time intervals were measured for melittin amount. After the permeation study, the same skin was used for melittin extraction. In addition, a known amount of melittin (5 μg/mL) was added to stratum corneum, epidermis, and dermis of the rat skin, and the amount of melittin was measured at pre-determined time points. The measurement of melittin from all samples was done with HPLC-MS/MS. No melittin was detected in the receptor phase at all time points in emulsion, DW, or NMP groups. When the amount of melittin was further analyzed in stratum corneum, epidermis, and dermis from the permeation study, melittin was still not detected. In an additional experiment, the amount of melittin added to all skin matrices was corrected against the amount of melittin recovered. While the total amount of melittin was retained in the stratum corneum, less than 10% of melittin remained in epidermis and dermis within 15 and 30 min, respectively. Skin microporation with BV emulsion facilitates the penetration of melittin across the stratum corneum into epidermis and dermis, where emulsified melittin could have been metabolized by locally-occurring enzymes. View Full-Text
Keywords: bee venom; emulsion; melittin; permeation bee venom; emulsion; melittin; permeation
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Han, S.M.; Kim, S.G.; Pak, S.C. Emulsion-Based Intradermal Delivery of Melittin in Rats. Molecules 2017, 22, 836.

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