Liposomes for drug delivery: review of vesicular composition, factors affecting drug release and drug loading in liposomes

Figures & data

Table

Advantages of Liposomes Liposomes are biocompatible and completely biodegradable. They are also non-toxic and non-immunogenic. Liposomes can encapsulate and deliver both hydrophobic and hydrophilic drugs. They possess flexibility to couple with site-specific ligands to achieve active targeting. Liposomes can provide sustained drug release. They protect the entrapped drugs from degradation in hostile environments. Liposomes can modulate the pharmacokinetic and pharmacodynamics of encapsulated drugs.

Disadvantages of Liposomes Liposomes have low stability. They possess a short half-life. The carrier lipids can undergo hydrolysis and oxidation. Leakage and fusion of encapsulated drug/molecules. Their production cost is high.

Figure 1. General structure of liposomes (own work).

Figure 2. Drug loading techniques in liposomes [92].

Table 1. Liposomal formulations available commercially.

Formulation	Therapeutic uses	Active ingredient	Company	References
Doxil®	Ovarian cancer and AIDS-related Kaposi’s Sarcoma	Doxorubicin	Sequus Pharmaceuticals	[130, 37]
Daunoxome®	AIDS-related Kaposi’s Sarcoma	Daunorubicin	NeXstar Pharmaceuticals	[131]
Depocyt®	Neoplastic meningitis	Cytarabine/Ara-C	Sky Pharmaceuticals	[132]
Myocet®	Combination with Cyclophosphamide for Metastatic Breast Cancer	Doxorubicin	Elan Pharmaceuticals	[133, 37]
Marqibo®	Acute lymphoblastic leukaemia	Vincristine	Talon Therapeutics	[134]
Onivyde®	Combination with Fluorouracil and Leucovorin in Metastatic adenocarcinoma of pancreas	Irinotecan	Merrimack Pharmaceuticals	[58, 37]
Ambisome®	Fungal infections	Amphoteracin B	Astellas Pharmaceuticals	[135]

Pauli G, Tang WL, Li SD. Development and characterization of the solvent-assisted active loading technology (SALT) for liposomal loading of poorly water-soluble compounds. Pharmaceutics. 2019;11(9):465. doi: 10.3390/pharmaceutics11090465.

 PubMed Web of Science ®Google Scholar

Zhao Y, Alakhova DY, Kim JO, et al. A simple way to enhance doxil® therapy: drug release from liposomes at the tumor site by amphiphilic block copolymer. J Control Release. 2013;168(1):61–69. doi: 10.1016/j.jconrel.2013.02.026.

 PubMed Web of Science ®Google Scholar

Bulbake U, et al. Liposomal formulations in clinical use: an updated review. Pharmaceutics. 2017;9(2):12. doi: 10.3390/pharmaceutics9020012.

 PubMed Web of Science ®Google Scholar

O’Byrne KJ, et al. A phase I dose-escalating study of daunoxome, liposomal daunorubicin, in metastatic breast cancer. Br J Cancer. 2002;87(1):15–20.

 PubMed Web of Science ®Google Scholar

Salehi B, et al. Liposomal cytarabine as cancer therapy: from chemistry to medicine. Biomolecules. 2019;9(12):773. doi: 10.3390/biom9120773.

 PubMed Web of Science ®Google Scholar

Batist G, Barton J, Chaikin P, et al. Myocet (liposome-encapsulated doxorubicin citrate): a new approach in breast cancer therapy. Expert Opin Pharmacother. 2002;3(12):1739–1751. doi: 10.1517/14656566.3.12.1739.

 PubMedGoogle Scholar

Silverman JA, Deitcher SR. Marqibo® (vincristine sulfate liposome injection) improves the pharmacokinetics and pharmacodynamics of vincristine. Cancer Chemother Pharmacol. 2013;71(3):555–564. doi: 10.1007/s00280-012-2042-4.

 PubMed Web of Science ®Google Scholar

Zhang W, Falconer JR, Baguley BC, et al. Improving drug retention in liposomes by aging with the aid of glucose. Int J Pharm. 2016;505(1-2):194–203. doi: 10.1016/j.ijpharm.2016.03.044.

 PubMedGoogle Scholar

Adler-Moore J, Proffitt RT. AmBisome: liposomal formulation, structure, mechanism of action and pre-clinical experience. J Antimicrob Chemother. 2002;49 Suppl 1(Suppl. S1):21–30. doi: 10.1093/jac/49.suppl_1.21.

 PubMedGoogle Scholar

Data availability statement

The data that support the findings of this review article are available in PubMed Central [PMC] at [https://pubmed.ncbi.nlm.nih.gov/] and Scopus [https://www.scopus.com/home.uri]. These data were cited from the following resources available in the public domain: [https://pubmed.ncbi.nlm.nih.gov/https://www.scopus.com/home.uri]