Solid-State and Solution Characterization of Myricetin

Journal Title: AAPS PharmSciTech - Year 2015, Vol 16, Issue 6

Abstract

Myricetin (MYR) is a natural compound that has been investigated as a chemopreventative agent. MYR has been shown to suppresses ultraviolet B (UVB)-induced cyclooxygenase-2 (COX-2) protein expression and reduce the incidence of UVB-induced skin tumors in mice. Despite MYR’s promise as a therapeutic agent, minimal information is available to guide the progression of formulations designed for future drug development. Here, data is presented describing the solid-state and solution characterization of MYR. Investigation into the solid-state properties of MYR identified four different crystal forms, two hydrates (MYR I and MYR II) and two metastable forms (MYR IA and MYR IIA). From solubility studies, it was evident that all forms are very insoluble (<5 μg/ml) in pure water. MYR I was found to be the most stable form at 23, 35, and 56°C. Stability determination indicated that MYR undergoes rapid apparent first-order degradation under basic pH conditions, and that degradation was influenced by buffer species. Apparent first-order degradation was also seen when MYR was introduced to an oxidizing solution. Improved stability was achieved after introducing 0.1% antioxidants to the solution. MYR was found to have good stability following exposure to ultraviolet radiation (UVR), which is a consideration for topical applications. Finally, a partitioning study indicated that MYR possess a log P of 2.94 which, along with its solid-state properties, contributes to its poor aqueous solubility. Both the solid-state properties and solution stability of MYR are important to consider when developing future formulations.

Authors and Affiliations

Stephen J. Franklin, Paul B. Myrdal

Keywords

Related Articles

Dissolution Testing for Bioavailability of Over-the-Counter (OTC) Drugs—a Technical Note

Thermoforma Orbital Shaker (420-4, Waltham, MA) was used to shake sample solutions at 100 RPM and 37°C. Orion pH Meter (710-1, Pittsburgh, PA) was used to measure solution pH. Two-point calibration with p...

Comparative Pharmacokinetic Study of Mangiferin After Oral Administration of Pure Mangiferin and US Patented Polyherbal Formulation to Rats

The online version of this article (doi:10.1208/s12249-014-0206-8) contains supplementary material, which is available to authorized users.

A Co-blended Locust Bean Gum and Polymethacrylate-NaCMC Matrix to Achieve Zero-Order Release via Hydro-Erosive Modulation

Locust bean gum (LBG) was blended with a cellulose/methacrylate-based interpolyelectrolyte complex (IPEC) to assess the hydro-erosive influence of addition of a polysaccharide on the disposition and drug delivery propert...

The Effect of Moisture on the Flowability of Pharmaceutical Excipients

The effect of moisture content on flowability of six pharmaceutical powders (microcrystalline cellulose (MCC), hydroxypropyl methylcellulose (HPMC), carboxymethyl cellulose (CMC), polyvinylpyrrolidone (PVP), corn starch,...

Development of Novel Ionic Liquid-Based Microemulsion Formulation for Dermal Delivery of 5-Fluorouracil

The present study was aimed at synthesizing an imidazole-based ionic liquid 1-butyl-3-methylimidazolium bromide (BMIMBr) and subsequent development of a novel ionic liquid-in-oil (IL/o) microemulsion (ME) system for derm...

Download PDF file
  • EP ID EP682314
  • DOI  10.1208/s12249-015-0329-6
  • Views 82
  • Downloads 0

How To Cite

Stephen J. Franklin, Paul B. Myrdal (2015). Solid-State and Solution Characterization of Myricetin. AAPS PharmSciTech, 16(6), -. https://europub.co.uk/articles/-A-682314