A Review on Liposomes

Abstract

In the latter part of the 1960s, liposomes sphere-shaped vesicles composed up of one or more membrane bilayers were first identified. In many scientific fields currently, including as mathematics and theoretical physics, biophysics, chemistry, colloid science, biochemistry, and biology, they serve as an immensely helpful reproduction, reagent, and tool. Ever since, liposomes have entered the market. Liposomes are an incredibly successful novel drug delivery system that uses cutting-edge technology to transfer active molecules to the site of action. Currently, a number of formulations of liposomes are being used in clinical settings. Research on liposome technology is moving from traditional vesicles to \"second-generation liposomes,\" which produce long-circulating liposomes by altering the vesicle\'s size, charge, and lipid composition.[1]

Introduction

Liposomes are spherical vesicles made of lipid bilayers that serve as biocompatible drug carriers. They are particularly effective for targeted drug delivery, including chemotherapeutic agents, due to their ability to encapsulate both hydrophilic and hydrophobic drugs. Their structure allows drugs to be delivered locally, reducing systemic toxicity and improving therapeutic efficacy.

Key Advantages of Liposomes

1. Versatility: Can carry both positively and negatively charged substances, including DNA and large molecules.

2. Protection: Shields encapsulated drugs or genes from degradation.

3. Targeted Delivery: Allows delivery to specific cells or tissues.

4. Reduced Toxicity: Minimizes exposure to non-target organs like heart, kidneys, and brain.

5. Enhanced Absorption: Improves drug solubility, tissue penetration, and cellular uptake.

Limitations

1. High Production Cost

2. Drug Leakage or Fusion

3. Instability due to Oxidation or Hydrolysis

4. Short Shelf Life and Low Solubility

Functional Mechanisms

Liposomes improve drug performance through:

• Enhanced solubility of poorly soluble drugs.

• Immune modulation via encapsulated vaccines or immunosuppressants.

• Localized or systemic release of biologics like peptides and hormones.

• Organ avoidance, reducing toxicity in critical systems.

• Ligand-based targeting for diseases like cancer.

• Improved hydrophilic drug transfer (e.g., antibiotics, genes).

• Better dermal penetration for topical drugs.

Types of Liposomes

1. Conventional Liposomes: Early forms using natural phospholipids.

2. pH-sensitive Liposomes: Release drugs in acidic environments like endosomes.

3. Cationic Liposomes: Often used in gene therapy; bind DNA for delivery.

4. Immune Liposomes: Act as adjuvants to stimulate immune responses.

5. Long-circulating Liposomes: PEGylated (coated with PEG) to extend circulation time and avoid immune clearance.

Structural Components

• Phospholipids: Main structural molecules (e.g., phosphatidylcholine).

• Cholesterol: Stabilizes the lipid bilayer and regulates fluidity.

Preparation Methods

1. Thin Film Method: Basic, low-efficiency approach using hydrated lipid films.

2. Reverse Phase Evaporation: Higher encapsulation efficiency, good for macromolecules.

3. Freeze-Thaw Technique: Useful for encapsulating proteins through freeze cycles.

4. Ultrasonic Method: Produces small unilamellar vesicles (SUVs) via sonication.

5. Calcium-Induced Fusion: Creates large unilamellar vesicles (LUVs) using acidic phospholipids and calcium.

Applications

• Cancer therapy (e.g., doxorubicin)

• Gene delivery

• Vaccination and immunotherapy

• Antifungal treatments (e.g., amphotericin B)

• Topical dermatological drugs

Conclusion

Liposomes are shown to be a successful medication delivery method for a number of conditions, include managing pain and cancer treatment. The formation of the biocompatible, biodegradable, and low immunogenicity liposomes improved the pharmacokinetic and pharmacodynamic features of the highly hazardous, water-insoluble, and poorly bioavailable medication. To get beyond their initial weaknesses, liposomes undergo a number of changes in terms of the elements and manufacture method. Several liposomes formulation is now approved in the market to treat various conditions and more than five hundred liposomal formulations are now in different phases of clinical manufacturing.

References

[1] Sahoo SK, Labhasetwar V: Drug delivery and imaging using nanoparticles. DDT 2003, 8:24. [2] In 1995, Bennett and O\'Brien authored Biochemistry 34, 3102-3113. [3] Biochemistry 35, 11782-11790; Miller, C. R., Chang, D. Y., Bennett, D. E., and O\'Brien, D. F. (1996) [4] Proc. Natl. Acad. Sci. U.S.A. 85, 8067-8071; Allen, T. M., Williamson, P., & Schlegel, R. A. (1988). [5] Papahadjopoulos D., Allen, T., Gabizon, A., Mayhew, E., Matthay, K., Huang, S. K., Lee, K.-D., Woodle, M. C., Lasic, D. D., Redemann, C., and Martin, F. J. (1991) Proc. Natl. Acad. Sci. U.S.A. 88, 11460-11464. [6] Nir, S., Papahadjopoulos D., and Lee, K.-D. (1993) Biological Chemistry, 32, 889-899. [7] Rodríguez JA, Bernabeu E, Daniels TR, et al. Targeted delivery of anti-cancer treatments and the transferrin receptor. Gen Subj. Biochim Biophys Acta 2012;1820:291–317. 10.1016/j.bbagen.2011.07.016 is the doi. [8] Barenholz Y, Stuart MC, Lasic DD, Frederik PM, and McIntosh TJ. 1992. internal liposome gelation. An innovative system for drugs encapsulation. Journal of FEBS 312:255–258 [9] Phosphatodylethanolamine liposomes: drug transport, gene transfer, and immunodiagnostic applications Litzinger DC, Huang L. 1992. 201–227 in Biochim Biophys Acta, 1113 [10] Stealth liposomes: a review of the science, explanation, and current and prospective therapeutic applications by Immordino ML, Dosio F, and Cattel L. Int J Nanomedicine 1(3), 2006, 297-315 NCBI/PubMed [11] Wang CY, Huang L. pH-sensitive immunoliposomes enhance controlling the expression of a foreign gene in mice and its transport to particular target cells. Proc 7851-7855 in Natl Acad Sci U S A 1987;84(22) View the PubMed/NCBI article [12] Karlsson G, Gustafsson J, Arvidson G, and Almgren M. Cryo-TEM characterisation of cationic liposome-DNA complexes. Biochim Biophys Acta 1995;1235(2):305-312 View the PubMed/NCBI articl [13] SJ LeGrue. Adjuvant and carrier characteristics of tumor-specific antigens administered by liposomes. Immunother Cancer 1984;17(2):135-141 View the PubMed/NCBI articl [14] Alving CR. Liposomes as adjuvant and antigen carriers. 1991, J Immunol Methods, 140(1), 1–13 View the PubMed/NCBI articl [15] Chonn A, Allen TM. Low consumption into the reticuloendothelial system of large unilamellar liposomes. 1987;223(1):42–46; FEBS Lett View a PubMed/NCBI article. [16] De Gennes PG. A simplified perspective on polymers at an interface. Research in Interface Science and Colloids 1987;27(1):189–209 [17] Platzgummer M, Wagner A, Quendler H, Stiegler G, Ferko B, Kreismayr G, et al. GMP liposome production: a novel approach to production. 16(3), J Liposome Res 2006, 311-319 [18] Akbarzadeh A, Hanifehpour Y, Zarghami N, Rezaei-Sadabady R, Davaran S, Joo SW, et al. Classification, production, and uses of liposomes. 2013\'s Nanoscale Res Lett 8(1):102 [19] Takahashi J, Tsuji Y, Ogata A, Konno Y, Watanabe Y, Aramaki K. cholesterol\'s capability to improve the charge of cationic liposomes. Surface A Colloid 2016;506:732-738 [20] Bhandari AK, Rana AC, and Dua JS. Al pharmacokinetic investigation, Clin. Transl. Sci. 14(2021) 132–136; IJPSR 2012; 3(2): 14–20 [21] Pakistan Review of Pharmaceutical Science 1996; 19(1): 65-77; Riaz M. [22] Sultana Y, Aqil M, Samad A. Recent Drug Delivery 2007; 4: 297-305 [23] Biochem J 1993; 295: 221-225; Onaderra M, Mancheno JM, Gasset M, Lacadena J, Schiavo G, Pozo AMD, Gavilanes G [24] Kuboi R, Shimanouchi T, Umakoshi H, & Tuan LQ. 2009; 44: 101-106; Enzyme and Microbial Technology. [25] Y.C. Tsai, H.T. Wang, A.M. Wang, S.F. Shih, Y.C. Chen, T.T. Tai, T.J. Wu, H.D. Wu, Y.C. Tsai, [26] C. Constantin, A. Pisani, G. Bardi, and then M. Neagu, Nano-carriers of COVID-19 vaccines: the main pillars of efficacy, Nanomedicine 16 (2021) 2377–2387, A preclinical pharmacokinetic study, Targeted delivery of inhalable liposomal hydroxychloroquine as a treatment for COVID-19 disease, Clin. Transl. Sci. 14(2021) 132–136.

Copyright

Copyright © 2025 Ms. Supriya B Chavan , Ms. Harshada S Shelke, Dr. Nitin M Gawai, Rushali S Bedjawalge. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.