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Review
. 2022 Jan 27;14(2):308.
doi: 10.3390/pharmaceutics14020308.

Liposomal-Based Formulations: A Path from Basic Research to Temozolomide Delivery Inside Glioblastoma Tissue

Roxana-Maria Amarandi  1 , Alina Ibanescu  1 , Eugen Carasevici  1 , Luminita Marin  2 , Brindusa Dragoi  1
Affiliations
Review

Liposomal-Based Formulations: A Path from Basic Research to Temozolomide Delivery Inside Glioblastoma Tissue

Roxana-Maria Amarandi et al. Pharmaceutics. .

Abstract

Glioblastoma (GBM) is a lethal brain cancer with a very difficult therapeutic approach and ultimately frustrating results. Currently, therapeutic success is mainly limited by the high degree of genetic and phenotypic heterogeneity, the blood brain barrier (BBB), as well as increased drug resistance. Temozolomide (TMZ), a monofunctional alkylating agent, is the first line chemotherapeutic drug for GBM treatment. Yet, the therapeutic efficacy of TMZ suffers from its inability to cross the BBB and very short half-life (~2 h), which requires high doses of this drug for a proper therapeutic effect. Encapsulation in a (nano)carrier is a promising strategy to effectively improve the therapeutic effect of TMZ against GBM. Although research on liposomes as carriers for therapeutic agents is still at an early stage, their integration in GBM treatment has a great potential to advance understanding and treating this disease. In this review, we provide a critical discussion on the preparation methods and physico-chemical properties of liposomes, with a particular emphasis on TMZ-liposomal formulations targeting GBM developed within the last decade. Furthermore, an overview on liposome-based formulations applied to translational oncology and clinical trials formulations in GBM treatment is provided. We emphasize that despite many years of intense research, more careful investigations are still needed to solve the main issues related to the manufacture of reproducible liposomal TMZ formulations for guaranteed translation to the market.

Keywords: characterization; chitosan; glioblastoma; liposome; synthesis; temozolomide.

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Conflict of interest statement

The authors declare no conflict of interest.

Figures

Figure 1
Figure 1
Schematic representation of a liposome.
Figure 2
Figure 2
Main types of liposomes.
Figure 3
Figure 3
Chemical formula of PEG.
Figure 4
Figure 4
Chemical structure of chitosan.
Figure 5
Figure 5
Strategies for TMZ-liposomes crossing the BBB and BTB.
Figure 6
Figure 6
Common phospholipids used for liposomal formulations.
Figure 7
Figure 7
Main conventional techniques used for liposome preparation.
Figure 8
Figure 8
Types of liposomes based on structure and size.
Figure 9
Figure 9
Main methods for large-scale production of liposomes.
Figure 10
Figure 10
Physico-chemical properties (4S) influencing the fate of NPs after intravenous administration.
Figure 11
Figure 11
Physico-chemical characterization of liposomes: methodologies and assays/techniques.
Figure 12
Figure 12
Clinical trials on TMZ and liposomes.
See this image and copyright information in PMC

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