Preformulation Studies of Bee Venom for the Preparation of Bee Venom-Loaded PLGA Particles

Abstract

It is known that allergic people was potentially vulnerable to bee venom (BV), which can induce an anaphylactic shock, eventually leading to death. Up until recently, this kind of allergy was treated only by venom immunotherapy (VIT) and its efficacy has been recognized worldwide. This treatment is practiced by subcutaneous injections that gradually increase the doses of the allergen. This is inconvenient for patients due to frequent injections. Poly (D,L-lactide-co-glycolide) (PLGA) has been broadly studied as a carrier for drug delivery systems (DDS) of proteins and peptides. PLGA particles usually induce a sustained release. In this study, the physicochemical properties of BV were examined prior to the preparation of BV-loaded PLGA nanoparticles NPs). The content of melittin, the main component of BV, was 53.3%. When protected from the light BV was stable at 4 °C in distilled water, during 8 weeks. BV-loaded PLGA particles were prepared using dichloromethane as the most suitable organic solvent and two min of ultrasonic emulsification time. This study has characterized OPEN ACCESSMolecules 2015, 20 15073 the physicochemical properties of BV for the preparation BV-loaded PLGA NPs in order to design and optimize a suitable sustained release system in the future.

Bee Venom: From Venom to Drug

“…Therapy by direct sting using honeybees is considered as a traditional method of treatment. It has multiple disadvantages like pain and inflammation caused by the sting, difficulty for maintaining its regular concentrations in blood, the need for long-term administration of a series of stings or injections because of the short half-life of melittin, and the inconvenience to patients [89]. The relatively short plasma half-life of bee venom and the problematic nature of determining its definite dose have led investigators and practitioners to promote and develop other alternatives, such as the combination with polymers or nanoparticles (NPs) [90].…”

“…The degradation time for NPs can be controlled from days to years by altering the type and amount of polymers, the polymer molecular weights, or the NPs' structures. Bee venom can maintain sustained release and efficacy for a long time using such polymer NPs, which reduces the administration interval and patient compliance [89,103].…”

Application of Fundamental Techniques for Physicochemical Characterizations to Understand Post-Formulation Performance of Pharmaceutical Nanocrystalline Materials

“…SEM is an analytical technique used for the characterization of surface morphology of API and excipients microscopically, in particular, differences in crystal habits and the shape of the samples [128,129]. SEM does not convey any information in respect of the chemical structure and/or thermal behaviour of compounds, and is used with other thermal and spectroscopic methods such as DSC, TGA, and FTIR to identify incompatibilities between API and excipients [129].…”

Melittin-loaded Iron Oxide Nanoparticles Prevent Intracranial Arterial Dolichoectasia Development through Inhibition of Macrophage-mediated Inflammation

“…To address this shortcoming, we engineered a MeLioN by loading melittin on the surface of an L-arginine-coated iron oxide nanoparticle (LION) as a core-shell structure. As observed from various melittin nanoparticle formulations to neutralize its toxicity [42][43][44][45][46][47], we further tested the hypothesis that nanoparticlemediated targeted delivery of melittin would circumvent this side effect and attenuate IADE development by targeting inflammatory cells and cytokines (Figure 1).…”