Total drug quantification in prodrugs using an automated elemental analyzer

Area of Science:

• Pharmaceutical Science
• Analytical Chemistry
• Polymer Chemistry

Background:

• Polymeric prodrugs enhance active pharmaceutical ingredient (API) pharmacokinetics.
• Accurate API quantification is vital for polymeric prodrug development.
• Existing methods like RP-HPLC and SEC are time-consuming and complex.

Purpose of the Study:

• To introduce and evaluate an automated elemental analyzer for API quantification in polymeric prodrugs.
• To compare the elemental analysis method with traditional quantification techniques.
• To establish a facile and sensitive analytical approach for drug loading determination.

Main Methods:

• Preparation of a poly(L-lysine succinylated) (PLS) and lamivudine (LAM) polymeric prodrug.
• Quantification using an automated elemental analyzer.
• Comparative analysis with hydrolysis followed by RP-HPLC and SEC-MALS.

Main Results:

• Elemental analysis demonstrated excellent agreement with conventional methods (RP-HPLC, SEC-MALS).
• The elemental analyzer approach was significantly less laborious than traditional methods.
• The method proved to be rapid and sensitive for drug loading determination.

Conclusions:

• Automated elemental analysis provides a facile and efficient method for quantifying drug loading in polymeric prodrugs.
• This technique offers a valuable alternative to conventional, more labor-intensive analytical approaches.
• The elemental analyzer is a promising tool for the development of polymeric prodrug therapeutics.