A Review on Liposomes as Novel Drug Delivery System
Bharti Choudhary*, Jitendra Banweer
School of Pharmaceutical Sciences, Sanjeev Agrawal Global Educational University,
Bhopal 462022, Madhya Pradesh, India.
*Corresponding Author E-mail: patelbharti90@gmail.com
ABSTRACT:
Liposomes, spherical vesicles made of phospholipids and cholesterol, are a potential drug delivery mechanism due to their large size, hydrophobic and lipophilic properties. They exhibit high biocompatibility and stability, allowing for the encapsulation of both hydrophilic and lipophilic drugs. Their amphiphatic structure allows for regulated drug release within their compartments. Liposomes are used in treating various ailments like tumors and cancer. This comprehensive review of the Liposomal Drug Delivery System explores various aspects related to liposomes.
KEYWORDS: Liposomes, Innovative transportation, Amphiphilic, Regulated discharge.
INTRODUCTION:
Liposomes are circular vesicles with essential properties inferred from the Greek words "lipos" meaning fat and "soma" meaning body. Liposomes were found incidentally by Bangham and colleagues in 1961. Liposomes are valuable since of their capacity to act as carriers for a assortment of drugs, giving helpful or other advantageous properties.1
Liposomes are colloidal particles extending in measure from 0.01 to 5.0ยตm. Liposomes viably typify drugs, permitting them to stay within the body for a long time. In any case, the medicate must to begin with be discharged from the liposomes some time recently it can be metabolized and dispensed with.2 These are little, circular, manufactured vesicles that can be made utilizing cholesterol and phospholipids determined from normal items.3
Liposomes hold incredible guarantee for medicate conveyance since of their expansive measure, combination of hydrophobicity and hydrophilicity, and their offer to natural frameworks.
Liposomes have the one-of-a-kind capacity to typify drugs from both fluid and lipid stages, making them appealing as vehicles for the conveyance of both hydrophilic and hydrophobic therapeutics.
Liposome are a novel course of medicate conveyance frameworks particularly planned to convey drugs straightforwardly to locales of activity.
They have the capacity to adjust to hydrophilic and lipophilic atoms to avoid medicate corruption and discharge dynamic fixings in a controlled manner. Glycerol is considered the most component of the molecule, so glycerol containing phospholipids are considered vital in liposome details. Glycerol accounts for 50% of the lipid weight in this test.4
The structural components consist of phospholipids:
Liposomes, spherical vesicles made of phospholipids and cholesterol, are a potential drug delivery mechanism due to their large size, hydrophobic and lipophilic properties, high biocompatibility, and stability. They are used in treating ailments like tumors and cancer, and their amphiphatic structure allows for regulated drug release.
Phospholipids, including phosphatidylcholine, phosphatidyl ethanolamine, glycerol, inositol, and serine, are charged lipids. Examples include non-ionic lipids, zwitter ionic lipids, and cationic lipids.
Phosphocholine, a hydrophilic polar head group, is found in phosphatidylcholine, an amphipathic particle composed of hydrophobic acyl hydrocarbon chains and a glycerol bridge. This structure, found in naturally occurring phosphatidylcholine, was discovered in 2011.
The way the hydrocarbon chains in the lipid particles behave determines the liposome film's evaluation.(Paecharoenchai and colleagues, 2012) The quality of fatty acids in lipid atoms affects the bilayer's characteristics, including its adaptability and reaction to completely different situations (for example, the number of two sections inside the chain is truncated).(Li and others, 2011) Choline-containing phospholipids may be used to create liposomes, because phospholipids are naturally abundant. Phospholipids are composed of phosphatidylcholine, sometimes shortened to PC and sometimes referred to as lecithin.Chioma (2016) There are three different types of phospholipids: phospholipid glycerol (PG), phospholipid serine (PS), and phospholipid ethanolamine (also known as cephalin). A crucial component of the organization and structure of liposomes is cholesterol.
It could be a widely used sterol. Sterols can change the framework's rigidity and soundness. It does not form a bilayer structure all at once (Dawaba et al. 2016). With a ratio of 1:1 or 2:1 between cholesterol and phosphatidylcholine, cholesterol binds to phospholipids in high quantities. According to Misra et al. (2018), cholesterol in the lipid bilayer promotes healthy skin and tissue organization and increases soundness. Cholesterol can reduce water-soluble compounds while increasing the quality and flexibility of cell films. Great cholesterol foresees disintegration and interaction with liposomes.
Points of interest of Liposomes Due to their amphipathic nature, two sorts of drugs can adhere together.
1. Water dissolvable or insoluble
2. Superior adequacy and refinement parameters.5
3. Nonionic materials
4. The 6th include is the capacity to specifically and inactively target tumour
5. Liposomes are biodegradable.
6. Liposomes increment sedate solidness.
7. One of the results of this is often the wonder of fashion perception.
8. Give sustained-release medicate formulations.
9. There's a relationship between drugs and cells.
10. The impact of evasion.
11. Enhance the stabilisation of proteins.6
Disadvantages of Liposomes:
1. Low solubility.
2. It includes a brief half-life.
3. The fetched of generation is to some degree impressive.7
4. The plausibility of spillage and combination of the typified pharmaceutical is show.
5. It is conceivable for phospholipids to experience oxidation
6. High production cost
LIPOSOMES: activity Component There are four particular components that are dependable for the action of liposomes. They are as depicted underneath.8
Endocytosis could be a handle that happens when Endothelial system phagocytic cells, including neutrophils are responsible for the method.9
1. Adsorption may be a prepare that takes put on the surface of the cell and can be caused by non-specific electrostatic powers or by contact with components of the cell surface.10
2. Combination may be a handle that takes put when a liposomal bilayer is embedded into the plasma film, and the liposomal fabric is persistently discharged into the cytoplasm.11
3. Lipid trade is the method by which lipids from liposomes are exchanged to the layer of the cell without the substance of the liposomes being related with the exchange.
1. Evaluation of the wrapped-up work Passive stacking method Mechanical scattering methods Lipid hydration strategy is the foremost common strategy utilized to make multilayered vesicles (MLVs). Utilizing this procedure, the lipid arrangement dissipates, shaping a long layer at the foot of a round-bottom jar (RBF). The movies were at that point hydrated by including water-based buffers and mixing utilizing vortexing. The hydration handle happens at the next temperature than the move from the gel to the fluid gem state. Depending on their solvency, the particles to be typified are presented into watery buffers or organic solvents.12 SLV is manufactured using microemulsification innovation. High-pressure homogenizers can be utilized to make tall shear powers to realize micro emulsification of lipid compositions.
Within the handle of drying the reconstituted vesicles, liposomes are combined with water containing appropriate drugs or freeze-dried proteins to make liposomes, which are at that point got dried out. The progressed disintegration framework permits utilizing this innovation for fast freezing of SUVs. Due to this highlight, monolayer formation occurs. A case of a lipid-soluble medicate is ethanol broken up in a lipid dissolvable. The particles are at that point included to the watery stage, coming about within the quick arrangement of multilamellar vesicles (MLVs). Typically a moment handle called dissolvable dispersion-ethanol injection. Ether mixture includes the cautious infusion of a lipid arrangement broken up in ether into a arrangement to be typified. This prepare is carried out at a temperature of 55 to 60 degrees Celsius. As the cleanser is washed out, the concentration of phospholipids within the blend increments, driving to the formation of huge unilamellar vesicles (LUVs).
Strategies for Forerunner Conveyance The liposome antecedent strategy includes the utilize of lipids and drugs blended into a carrier to create a fluid containing forerunner liposomes. The item is at that point hydrated and changed over into an isotonic liposome arrangement as detailed within the writing.
The method of lessening the dampness substance of the cargo, such as by solidifying the cargo to create it less thick. This strategy is called solidify drying. In common, this strategy is utilized to dry items that are inclined to warm degradation.
Liposomes in Commercial Definition In 1995, the US FDA affirmed the utilize of Doxil, a medicate called doxorubicin typified in a PEGylated liposome.
Characterization of liposomes:
|
A. Physical Description |
|
|
Parameter of Characterization |
Techniques |
|
Vesicle form and surface characteristics |
Scanning electron microscopy (SEM) and transmission electron microscopy (TEM) |
|
Size distribution of vesicles |
TEM and dynamic light scattering |
|
Charge on the surface |
Electrophoresis by free flow |
|
Surface pH and electrical surface potential |
pH-sensitive probes and zeta potential measuring |
|
The Lamellarity |
Nuclear Magnetic Resonance Spectroscopy of Phosphorus-31 (NMR) |
|
Phase behavior |
Electron microscopy using freeze-fracture and differential scanning calorimetry |
|
Percent capture |
Gel exclusion and mini column centrifugation |
|
Drug release |
Dialysis and diffuse cells |
|
B. Chemical Description |
|
|
Concentration of phospholipids |
HPLC (High Performance Liquid Chromatography) |
|
Concentration of cholesterol |
Cholesterol oxide test with HPLC |
|
concentration of Drug |
Assay technique |
|
Peroxidation of phospholipids |
UV Monitoring |
|
Hydrolysis of phospholipids |
Thin Layer Chromatography, or HPLC/TLC |
|
The auto-oxidation of cholesterol |
High performance liquid chromatography |
|
Degradation of antioxidants |
High Performance Liquid Chromatography/Thin Layer Chromatography |
|
pH |
pH meter |
|
The osmolarity |
An osmometer |
|
C. Biological description |
|
|
Infertility |
Cultures That Are Aerobic or Anaerobic |
|
The pyrogenic nature |
Response to rabbit sickness |
|
The toxicity of animals |
Tracking the survival of rats |
Liposome Stability:
The steadiness of liposomes is vital in deciding the helpful impact of drugs. Steadiness can be separated into two categories:
A. Physical steadiness: It is the capacity of liposome to preserve their shape and properties over time. The rack life of liposomes can be influenced by different physical marvels such as combination, accumulation, shape and measure changes. The most issue that emerges is the spillage of chemical compounds. Shape and estimate ought to be considered as basic characteristics in security safeguards. To guarantee soundness within the body, the wealth of super saturation in phospholipids ought to be decreased. The item ought to be put away at 4 degrees Celsius to anticipate solidifying and secure from light.13
B. Chemical Steadiness: Phospholipids are inclined to hydrolysis due to their unsaturated greasy corrosive composition, which can influence the soundness of the treatment. Cancer prevention agents such as butylated hydroxyl anisole (BHA) can be utilized to avoid oxidative debasement of liposomes.
Liposomes are broadly utilized in quality treatment within the treatment of infections.14
Recent advancements in the field of liposomes as a novel drug delivery system have significantly improved their clinical applications. Liposomes, which are phospholipid-based vesicles, offer unique advantages such as targeted drug delivery, controlled release, and reduced systemic toxicity, making them ideal for treating cancer, fungal infections, and inflammatory diseases.
Targeted and Sustained Delivery:
Liposomes have shown great success in delivering drugs to specific sites in the body, such as tumors, through passive and active targeting mechanisms. This minimizes off-target effects and enhances therapeutic efficacy, as seen with FDA-approved drugs like Doxil and AmBisome, which use liposomal formulations for cancer and fungal infections, respectively.15
Recent Innovations:
Research has focused on multifunctional liposomes, such as PEGylated liposomes, which prolong circulation time and improve drug delivery to tumors. These liposomes are being explored for delivering combinations of drugs, targeting cellular organelles, and integrating diagnostic agents for theranostics (simultaneous therapy and diagnostics)16,17
Ongoing Clinical Trials:
Current trials are exploring liposome-encapsulated drugs for advanced cancer therapies and infectious diseases. Liposomal formulations are also being tested for their ability to deliver genetic material in gene therapy and vaccines, promising new avenues for personalized medicine.18
REFERENCE:
1. Bangham AD, Horne RW. Negative staining of phospholipids and their structural modification by surface-active agents as observed in the electron microscope. Journal of Molecular Biology. 1964; Jan; 8(5): 660-IN10. doi.org/10.1016/s0022-2836(64)80115-7.
2. Lasic D. Novel applications of liposomes. Trends in Biotechnology [Internet]. 1998; Jul 1 [cited 2022 Mar 3]; 16(7): 30721. doi.org/10.1016/s0167-7799(98)01220-7.
3. Mayer LD, Hope MJ, Cullis PR, Janoff AS. Solute distributions and trapping efficiencies observed in freeze-thawed multilamellar vesicles. Biochimica et Biophysica Acta (BBA) - Biomembranes. 1985; Jul 1;817(1):1936. doi.org/10.1016/0005-2736(85)90084-7
4. Fujisawa T, Miyai H, Hironaka K, Tsukamoto T, Tahara K, Yuichi Tozuka, et al. Liposomal diclofenac eye drop formulations targeting the retina: Formulation stability improvement using surface modification of liposomes. International Journal of Pharmaceutics. 2012; Oct 1; 436(1-2): 5647. doi.org/10.1016/j.ijpharm.2012.07.024.
5. Mishra H, Chauhan V, Kumar K, Teotia D. A comprehensive review on Liposomes: a novel drug delivery system. Journal of Drug Delivery and Therapeutics. 2018; Nov 25; 8(6): 4004. doi.org/10.22270/jddt.v8i6.2071.
6. Kaur D, Kumar S. NIOSOMES: Present Scenario and Future Aspects. Journal of Drug Delivery and Therapeutics. 2018 Sep 6; 8(5): 3543. doi.org/10.22270/jddt.v8i5.1886
7. Hong MS, Lim SJ, Lee MK, Kim YB, Kim CK. Prolonged blood circulation of methotrexate by modulation of liposomal composition. Drug delivery [Internet]. 2001; 8(4): 2317. doi.org/10.1080/107175401317245912
8. Vemuri S, Rhodes CT. Preparation and characterization of liposomes as therapeutic delivery systems: a review. Pharmaceutica Acta Helvetiae. 1995; Jul; 70(2): 95111. doi.org/10.1016/0031-6865(95)00010-7
9. James ND, Coker RJ, Tomlinson D, Harris JRW, Gompels M, Pinching AJ, et al. Liposomal doxorubicin (Doxil): An effective new treatment for Kaposis sarcoma in AIDS. Clinical Oncology. 1994 Jan;6(5):2946. doi.org/10.1016/s0936-6555(05)80269-9.
10. Laouini A, Jaafar-Maalej C, Limayem-Blouza I, Sfar S, Charcosset C, Fessi H. Preparation, Characterization and Applications of Liposomes: State of the Art. Journal of Colloid Science and Biotechnology. 2012; Dec 1; 1(2): 14768. doi.org/10.1166/jcsb.2012.1020.
11. Gregoriadis G, Davis C. Stability of liposomes invivo and invitro is promoted by their cholesterol content and the presence of blood cells. Biochemical and Biophysical Research Communications. 1979; Aug; 89(4): 128793. doi.org/10.1016/0006-291x(79)92148-x.
12. Ejiogu Deborah Chioma. Formulation And Evaluation Of Etodolac Niosomes By Modified Ether Injection Technique. Universal Journal of Pharmaceutical Research. 2016 Nov 15;1(1):16. doi.org/10.22270/ujpr.v1i1.r1
13. Ugochukwu AE. Preparation and Characterization of Tolterodine Tartrate Proniosomes. Universal Journal of Pharmaceutical Research. 2017 May 15;2(2):225. doi.org/10.22270/ujpr.v2i2.r1
14. Wasan KM, Lopez-Berestein G. The Past, Present, and Future Uses of Liposomes in Treating Infectious Diseases. Immunopharmacology and Immunotoxicology. 1995 Jan;17(1):115. doi.org/10.3109/08923979509052716
15. Allen TM, Cullis PR. Liposomal drug delivery systems: From concept to clinical applications. Advanced Drug Delivery Reviews [Internet]. 2013 Jan [cited 2019 Mar 1];65(1):3648. doi.org/10.1016/j.addr.2012.09.037.
16. Ellens H, Mayhew E, Rustum Y. Reversible depression of the reticuloendothelial system by liposomes. Biochimica et Biophysica Acta (BBA) - General Subjects. 1982; Feb 25; 714(3): 47985. doi.org/10.1016/0304-4165(82)90157-x
17. Nekkanti, Vijaykumar and Kalepu, Sandeep. (2015). Recent Advances in Liposomal Drug Delivery: A Review. Pharmaceutical Nanotechnology. 3. 35-55. doi.org/10.2174/2211738503666150709173905
18. Barenholz Y (Chezy). Doxilฎ The first FDA-approved nano-drug: Lessons learned. Journal of Controlled Release. 2012; Jun; 160(2): 11734. doi.org/10.1016/j.jconrel.2012.03.020.
|
Received on 02.08.2024 Revised on 30.10.2024 Accepted on 03.12.2024 Published on 12.06.2025 Available online from June 14, 2025 Research J. Pharmacy and Technology. 2025;18(6):2864-2867. DOI: 10.52711/0974-360X.2025.00412 ฉ RJPT All right reserved
|
|
|
This work is licensed under a Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License. Creative Commons License. |
|