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Scale-Independent Microfluidic Production of Cationic Liposomal Adjuvants and Development of Enhanced Lymphatic Targeting Strategies

Mol Pharm. 2019 Oct 7;16(10):4372-4386. doi: 10.1021/acs.molpharmaceut.9b00730. Epub 2019 Sep 6.

Abstract

Cationic liposomes prepared from dimethyldioctadecylammonium bromide (DDAB) and trehalose 6,6'-dibehenate (TDB) are strong liposomal adjuvants. As with many liposome formulations, within the laboratory DDAB:TDB is commonly prepared by the thin-film method, which is difficult to scale-up and gives high batch-to-batch variability. In contrast, controllable technologies such as microfluidics offer robust, continuous, and scale-independent production. Therefore, within this study, we have developed a microfluidic production method for cationic liposomal adjuvants that is scale-independent and produces liposomal adjuvants with analogous biodistribution and immunogenicity compared to those produced by the small-scale lipid hydration method. Subsequently, we further developed the DDAB:TDB adjuvant system to include a lymphatic targeting strategy using microfluidics. By exploiting a biotin-avidin complexation strategy, we were able to manipulate the pharmacokinetic profile and enhance targeting and retention of DDAB:TDB and antigen within the lymph nodes. Interestingly, redirecting these cationic liposomal adjuvants did not translate into notably improved vaccine efficacy.

Keywords: cationic liposomes; lymphatic targeting; manufacture; microfluidics; vaccine adjuvants.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adjuvants, Immunologic / administration & dosage
  • Adjuvants, Immunologic / chemistry*
  • Animals
  • Antigens, Bacterial / administration & dosage
  • Antigens, Bacterial / immunology
  • Cations / chemistry*
  • Female
  • Immunization
  • Liposomes / administration & dosage
  • Liposomes / chemistry*
  • Lymph Nodes / drug effects*
  • Mice
  • Mice, Inbred BALB C
  • Mice, Inbred C57BL
  • Microfluidics*
  • Quaternary Ammonium Compounds / chemistry*
  • Tissue Distribution
  • Tuberculosis / immunology
  • Tuberculosis / prevention & control
  • Tuberculosis Vaccines / administration & dosage*
  • Tuberculosis Vaccines / immunology
  • Tuberculosis Vaccines / pharmacokinetics

Substances

  • Adjuvants, Immunologic
  • Antigens, Bacterial
  • Cations
  • Liposomes
  • Quaternary Ammonium Compounds
  • Tuberculosis Vaccines
  • dimethyldioctadecylammonium