Mixing lipids to manipulate the ionization status of lipid nanoparticles for specific tissue targeting.

ABSTRACT:

Introduction

The development of targeted drug delivery systems is a rapidly growing area in the field of nanomedicine.

Methods

We report herein on optimizing the targeting efficiency of a lipid nanoparticle (LNP) by manipulating the acid dissociation constant (pKa) value of its membrane, which reflects its ionization status. Instead of changing the chemical structure of the lipids to achieve this, we used a mixture of two types of pH-sensitive cationic lipids that show different pKa values in a single LNP. We mixed various ratios of YSK05 and YSK12-C4 lipids, which have pKa values of 6.50 and 8.00, respectively, in one formulation (referred to as YSK05/12-LNP).

Results

The pKa of the YSK05/12-LNP was dependent not only on the molar ratio of

SUBMITTER: Shobaki N 

PROVIDER: S-EPMC6294068 | biostudies-literature | 2018

REPOSITORIES: biostudies-literature