Abstract

This study aimed to produce thermosensitive liposomes (TSL) by applying the quality by design (QbD) concept. In this paper, our research group collected and studied the parameters that significantly impact the quality of the liposomal product. Thermosensitive liposomes are vesicles used as drug delivery systems that release the active pharmaceutical ingredient in a targeted way at ~40–42 °C, i.e., in local hyperthermia. This study aimed to manufacture thermosensitive liposomes with a diameter of approximately 100 nm. The first TSLs were made from DPPC (1,2-dipalmitoyl-sn-glycerol-3-phosphocholine) and DSPC (1,2-dioctadecanoyl-sn-glycero-3-phosphocholine) phospholipids. Studies showed that the application of different types and ratios of lipids influences the thermal properties of liposomes. In this research, we made thermosensitive liposomes using a PEGylated lipid besides the previously mentioned phospholipids with the thin-film hydration method.

Highlights

  • Liposomes are spherical formations, vesicles located by a membrane bilayer, in the nanometre size range [1]

  • Phospholipids are important components of liposomes that, due to their hydrophobic tails and hydrophilic heads, are able to form a double membrane layer. One of their crucial pharmaceutical advantages is that these vesicles can incorporate hydrophobic and hydrophilic active pharmaceutical ingredients (APIs) as well

  • The hydrophilic drug is found in the hydrophilic core of the liposomes, while the lipophilic API is in the wall of the vesicles [1]

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Summary

Introduction

Liposomes are spherical formations, vesicles located by a membrane bilayer, in the nanometre size range [1]. The inner phase of liposomes is separated from the dispersed media by a double lipid layer The size of these vesicles can range from 20 nm to some μm. Phospholipids are important components of liposomes that, due to their hydrophobic tails and hydrophilic heads, are able to form a double membrane layer One of their crucial pharmaceutical advantages is that these vesicles can incorporate hydrophobic and hydrophilic active pharmaceutical ingredients (APIs) as well. The developer of the practice [2]—is one of the most frequently used preparation methods This method is still widely used for the typical production of non-phospholipid/phospholipid vesicles located in a membrane bilayer and formed by supramolecular assembly [8,9,10,11]. Its first step is to solve the lipids of the membrane and the hydrophobic API in an organic solvent, which is later removed

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