Polysorbate 80 is one of the most commonly used surfactants in the formulation of biotherapeutics, particularly those administered intravenously. It comprises a mixture of fatty acids but is not a precisely defined chemical entity. Hence, there are a range of different grades available in the market, all meeting compendial specifications. Polysorbate 80 is known to undergo auto degradation producing protein-damaging by-products, and to contain residual impurities that can have an impact on the stability and integrity of the active ingredients in the formulation. Given the variety of chemical compositions that polysorbate 80 can comprise, the degradation pathway and extent could vary depending on the grade used in the formulation. This study compared the physical and chemical properties of four commercially available polysorbate 80 grades with different degrees of purity and oleic acid content and investigated their degradation profiles. This study did not find any significant differences between the properties or degradation profiles of the four grades investigated. Further studies are underway to understand the formation of other reactive impurities and their impact on the model protein formulations.
Welcome to the 15th volume of the Journal of Excipients and Food Chemicals (JEFC) 2024. It is my pleasure to introduce myself as the new Editor for this publication. To quote the ubiquitous Taylor Swift on X (2015); “This is a new year. A new beginning. And things will change”. For The Journal of Excipients and Food Chemicals (JEFC), this means a new perspective that stems from my thirty-plus year career in the pharmaceutical industry, working on new product development and drug delivery.
The objective of the work presented here was to assess the feasibility of using glucosamine HCl as a solid-dispersion (SD) carrier to enhance the biopharmaceutical properties of a BCS class III/IV drug, acyclovir (ACV). The solid-dispersions of acyclovir and glucosamine HCl were prepared by an ethanol-based solvent evaporation method. The prepared formulations characterized by photomicroscopy, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), Fourier transform infrared spectrophotometry (FTIR), powder x-ray diffractometry (PXRD) and drug content analysis. The functional characterization of ACV-SD was performed by aqueous solubility evaluation, dissolution studies, fasted versus fed state dissolution comparison, ex vivo permeability, and stability studies. Photomicroscopy and SEM analysis showed different surface morphologies for pure ACV, glucosamine HCl and ACV-SD. The physical-chemical characterization studies supported the formation of ACV-SD. A 12-fold enhancement in the aqueous solubility of ACV was observed in the prepared solid dispersions, compared to pure ACV. Results from in vitro dissolution demonstrated a significant increase in the rate and extent of ACV dissolution from the prepared ACV-SD formulations, compared to pure ACV. The rate and extent of ACV permeability across everted rat intestinal membrane were also found to be significantly increased in the ACV-SD formulations. Under fed conditions, the rate and extent of the in vitro dissolution of ACV from the formulation was appreciably greater compared to fasted conditions. Overall, the results from the study suggest the feasibility of utilizing glucosamine HCl as a solid dispersion carrier/excipient for enhancement of biopharmaceutical properties of acyclovir, and similar drugs with low solubility/permeability characteristics.
The developments in pharmaceutical excipient science and technology since 1995 have been reviewed. The field of excipients science and technology has changed and continues to change. Some good progress has been made in such areas as harmonization of excipient pharmacopeial monographs, and the application of new analytical methods to better characterize excipients
