Investigating the Correlation Between Drug Physical Properties and Physical Characteristics and Drug Entrapment Efficiencies of Chitosan-TPP Nanoparticles

Abstract

Chitosan nanoparticles (NPs) have been the subject of intensive research. This study aimed to determine how different drug characteristics such as molecular weights, drug solubility in the processing medium, and drug ionization/charge state affected chitosan NPs particularly their percentage entrapment efficiency (% EE) and mean hydrodynamic diameters (MHDs). Drugs with varying molecular weights but of similar aqueous solubilities were chosen and were dissolved in a 2% chitosan-acetic acid solution. Chitosan NPs were formed using by ionic gelation technique using sodium tripolyphosphate (TPP) at specific concentration and volume ratios of chitosan to TPP. NPs containing Enalapril and Paracetamol displayed better short-term stability in terms of MHDs. A direct relationship between MHDs of NPs and chitosan concentrations was found. In comparison, at both low and high admixed drug concentrations and at high chitosan concentration, larger NPs sizes were associated with the lower molecular weight drug (Paracetamol). However, the study did not demonstrate a direct relationship between NPs characteristics such as MHDs and drugs molecular weights. The ZP of Paracetamol-loaded NPs was lowest at high drug concentrations at all chitosan concentrations compared to other drugs-loaded NPs. When compared to drugs with high and low molecular weights, medium molecular weight Atenolol showed the highest % EE. This clearly indicated that there was no direct correlation between drug molecular weight and % EE, but rather other factors influenced on % EE. Nevertheless, an inverse linear relationship with high correlation coefficients was only found when % EE was plotted against each drug molecular weight divided by the ratio of drugs solubilities in acetic acid to their employed concentrations, however the correlation was inconsistent between drugs of varying molecular weights.