Vaccine adjuvant platform and fluorescence imaging of amphiphilic γ-PGA-IMQ-LA-FL conjugates

Abstract

Adjuvants have proven to be integral components in most vaccines for promoting appropriate immune responses at both innate and adaptive levels. Imiquimod (IMQ, R837), an agonist for Toll-like receptors 7...

Formulation and Evaluation of Lipidized Imiquimod as an Effective Adjuvant

“…Undoubtedly, the safety issue of IMQ-Chol is a prerequisite for its biomedical applications as a good adjuvant. However, our previous research indicated that pristine IMQ was found to be more cytotoxic and triggered different degrees of toxic side effects after subcutaneous injection in mice. Considering animal ethics and its poor solubility, we did not use IMQ as a control in our following experiment.…”

“…FMDV-specific IgG (Lanzhou Shouyan Biotechnology, Co., Ltd.) and subtypes (IgG1, IgG2a) in the serum of the immunized mice were detected by mouse IgG1 and IgG2a ELISA kit (Multi Sciences (LIANKE) Biotech, Co., Ltd.) 2−12 weeks after immunization according to a previous study. 15 The absorbance was calculated at 450 nm using a microplate reader (Bio-Rad), and all samples were measured in quadruplicate.…”

“…In addition, IMQ has low solubility both in water and in most common organic solvents (such as dichloromethane and ethanol) or mineral oil, which poses challenges for adjuvant development. To circumvent these drawbacks, IMQ was encapsulated in nanomaterials − or covalent-conjugated to polymers. , …”

“…To circumvent these drawbacks, IMQ was encapsulated in nanomaterials 12−14 or covalent-conjugated to polymers. 11,15 Lipidation is another important modification strategy for bioactive molecules to improve their pharmacokinetic properties, which has shown exceptional promise in pharmaceutical applications such as self-adjuvant vaccines. 16 Based on these grounds, the practical applications of small-molecule synthetic TLR7 adju vants from the covalent attachment of lipophilic groups have impeded the advancement of the field.…”