Evaluation of the in vitro bee venom release and skin absorption from bioadhesive gel formulation

Topical and transdermal drug delivery are one of the most suitable alternative, non-invasive routes for administration of drugs in clinical practice mainly due to the increased patient compliance and reduced systemic drug side effects. Many drug products applied to the skin surface may penetrate to some extent into the skin layers, where their effects are expected, as for example, topical formulations for the treatment of different local skin disorders. Also, significant concentrations of drug could be absorbed by the body regions close to the site of delivery, where regional effects are expected, for e.g., in the muscles, local blood vessels and articulations. Arthritis is a systemic, autoimmune disease characterized by inflammation of joints. Inflammatory cytokines cause activation of the macrophages which leads to swelling of joints, damage to cartilage, bone erosion , functional impairment and stiffness. Bee venom (BV) contains a variety of peptides, including melittin, apamin, adolapin, the mast-cell degranulating peptide, enzymes (phospholipase [PL] A2), biologically active amines (histamine and epinephrine) and nonpeptide components with anti�inflammatory, anti-arthritis, anticoagulant, antimicrobial, anticancer and anti-nociceptive properties. Melittin, a major peptide component of BV shown to have anti-inflammatory and anti�arthritis properties and inhibitory activity on nuclear factor kappaB which is involved in the synthesis of inflammatory mediators and may be essential for the treatment of arthritis using BV. The aim of this study was to evaluate the stability of crude BV as an active ingredient, as well as to evaluate the in vitro release and skin absorption of BV from a designed topical gel formulation