Development of liposomal drug formulations: quality attributes and methods for quality control

E.V Melnikova,A.R Sayfutdinova,M.A Vodyakova,V.A Merkulov,D.V Goryachev,A.A Chaplenko

doi:10.24075/brsmu.2018.092

Abstract

The use of nanostructured components in drug manufacturing and, more specifically, targeted drug delivery has recently become a major trend in the pharmaceutical industry. Nanodrugs encompass a wide range of pharmaceutical agents containing dendrimers, nanocrystals, micelles, liposomes, and polymer nanoparticles. Liposomes are the most well-studied nanoparticles and effective drug carriers. However, the more complex their structure is, the more process controls are needed and the more quality attributes have to be monitored, including the chemical properties of the liposomal fraction such as the shape, size and charge of the nanoparticle, conjugation efficacy, and distribution of the active ingredient. We believe that quality control of key liposome characteristics should rely on dynamic and laser light scattering coupled with electrophoresis, differential scanning calorimetry, cryo-electron microscopy, nuclear magnetic resonance, laser diffraction analysis, and gel filtration chromatography.

Highlights

The use of nanostructured components in drug manufacturing and, targeted drug delivery has recently become a major pharmacy trend
Russian legislation does not describe the concepts of “nanopreparations” or “nanodrugs”; in reality, all drugs that are nanoparticles or contain them are considered to be such. This definition mainly applies to the drugs based on liposomes and micelles, where nanostructures enable transportation of the active pharmaceutical ingredient inside the body, prolong its absorption, increase stability, etc. Another case are drugs considered to be nanostructured due to the physicochemical characteristics of their active ingredients, an example of which are antianemic iron preparations that may contain iron (III) atoms stabilized by a carbohydrate complex, which defines their nanocolloidal structure
We are developing quality assessment and research guidelines applicable to drugs based on liposomes and micelles, as well as containing nanoparticles

Summary

Introduction

The use of nanostructured components in drug manufacturing and, targeted drug delivery has recently become a major pharmacy trend. Controlled parameters: amount of residual organic solvents in the lipid film; active pharmaceutical ingredient integration rate and size of the liposomes after lipid film dispersion; stability; pH value.

Results

Conclusion