Synthesis of Polymer Conjugates of Efavirenz, Tenofovir and Dolutegravir

Background and purpose: Chitosan and alginate are examples of biodegradable polymers which have the advantage of controlled drug delivery, prevent overdose and toxicity. The aim of the study is to synthesize the three anti-retroviral drug-polymer conjugates of chitosan and alginate. Method: The synthetic pathways involved the synthesis of three different conjugates labelled as, A, B and C through a Schiff process reaction, Diazotization reaction and esterification reaction, respectively. After synthesis, the products were purified by recrystallisation and preparative TLC. The calibration curve data and IR analyses were conducted. Result: The synthetic yield for the drug conjugates was 85%, 75% and 82% for efavirenz-chitosan (A) Tenofovir-chitosan (B) and dolutegravir-alginate (C), respectively. The drug conjugates obeyed Beer–Lambert's law and showed linear response in the concentration range of 5–40 μg/mL with a 2 correlation coefficient (R ) of 0.999 for all three drug-polymer conjugates. The IR spectra of conjugate -1 A with the functional group (C=N) appeared at 1997.96 cm , B Conjugate with functional group -1 - (N=N) appeared at 2303.5 cm and C conjugate with functional group (COO-) appeared at 1736.3 cm 1, respectively. Conclusion: The Synthesis of Polymer Conjugates of Efavirenz, Tenofovir and Dolutegravir was achieved through different synthetic pathways and monitored by Thin-layer chromatography, melting point and UV and then confirmed by Fourier Transform infra-red (FTRI) spectroscopy.