Gelatin Coating for the Improvement of Stability and Cell Uptake of Hydrophobic Drug-Containing Liposomes.

Gantumur Battogtokh,Yechan Joo,Sharif Md Abuzar,Sung-Joo Hwang,Heejun Park

doi:10.3390/molecules27031041

Gantumur Battogtokh, Yechan Joo + Show 3 more

Open Access

https://doi.org/10.3390/molecules27031041

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Abstract

Purpose: Most therapeutic agents have limitations owing to low selectivity and poor solubility, resulting in post-treatment side effects. Therefore, there is a need to improve solubility and develop new formulations to deliver therapeutic agents specifically to the target site. Gelatin is a natural protein that is composed of several amino acids. Previous studies revealed that gelatin contains arginyl-glycyl-aspartic acid (RGD) sequences that become ligands for the integrin receptors expressed on cancer cells. Thus, in this study, we aimed to increase the efficiency of drug delivery into cancer cells by coating drug-encapsulating liposomes with gelatin (gelatin-coated liposomes, GCLs). Methods: Liposomes were coated with gelatin using electrostatic interaction and covalent bonding. GCLs were compared with PEGylated liposomes in terms of their size, zeta potential, encapsulation efficiency, stability, dissolution profile, and cell uptake. Results: Small-sized and physically stable GCLs were prepared, and they showed high drug-encapsulation efficiency. An in vitro dissolution study showed sustained release depending on the degree of gelatin coating. Cell uptake studies showed that GCLs were superior to PEGylated liposomes in terms of cancer cell-targeting ability. Conclusions: GCLs can be a novel and promising carrier system for targeted anticancer agent delivery. GCLs, which exhibited various characteristics depending on the coating degree, could be utilized in various ways in future studies.

Highlights

There are several types of lipid-based nanoparticles used as drug delivery systems, such as liposomes, lipid nanoparticles, and solid lipid nanoparticles
To enhance the targeting ability of liposomal carrier systems, we developed Gelatin-coated liposomes (GCLs) in this study
The gelatin coating on the liposomes worked as intended, and the GCLs exhibited different properties depending on the coating mechanism, namely electrostatic interaction or covalent bond formation

Summary

Introduction

There are several types of lipid-based nanoparticles used as drug delivery systems, such as liposomes, lipid nanoparticles, and solid lipid nanoparticles. One such example is liposomes, which are a type of nanocarrier consisting of phospholipids and cholesterol. Liposomes can encapsulate both hydrophobic and hydrophilic drugs owing to their amphipathic properties, and the surface of liposomes can be modified using functionalized lipids [1,2]. It has been pointed out that PEGylated liposomes have weak interactions with cancer cells because of the aqueous layers on their surfaces created by the PEG moiety [6]. Other proteins can be promising candidates as next-generation drug carriers

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