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*Corresponding Author: Abbaraju Krishna Sailaja, Department of pharmaceutics, RBVRR Women’s college of pharmacy, Affiliated to Osmania University, Hyderabad.
Citation: PoojaVemula, Abbaraju K, Sailaja, (2023), Transferosomes-A Novel Carrier for Drug Delivery, Dermatology and Dermatitis, 8(5); DOI:10.31579/2578-8949/132
Copyright: © 2023, Abbaraju Krishna Sailaja. This is an open-access article distributed under the terms of The Creative Commons. Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
Received: 10 November 2023 | Accepted: 16 November 2023 | Published: 27 November 2023
Keywords: gerhard Hansen; leprosy; philately; postage stamps; envelopes; numismatics; commemorative medals
Transferosomes are a type of lipid-based drug delivery system that is designed to enhance the delivery of drugs through the skin or other biological barriers. They are composed of phospholipids, surfactants, and sometimes cholesterol, which form a bilayer structure that encapsulates the drug. Additionally, transferosomes can be tailored to target specific tissues or cells, which can increase the efficacy of drugs while reducing the risk of side effects. For example, transferosomes can be designed to deliver drugs to cancer cells, allowing for targeted cancer therapy with fewer side effects than traditional chemotherapy. In this article detailed discussion was made on formulation and applications of transferosomes.
Transferosomes were first introduced in the 1990s as a novel drug delivery system, and they have since been studied extensively for their potential therapeutic applications. One of the key advantages of transferosomes is their ability to improve the bioavailability of drugs that have poor water solubility, which can limit their effectiveness when administered by traditional methods.
Overall, transferosomes are a promising drug delivery system with potential applications in a wide range of therapeutic areas. Ongoing research is focused on improving the stability, efficacy, and safety of transferosomes, as well as exploring new ways to use them in clinical practice.[3]
Figure 1.1 : Structure of transferosomes
| Class | Example | Uses |
| Phospholipids | Soya phosphatidyl choline, Dipalmitoyl phosphatidyl choline, Distearoyl phoshatidyl choline | Vesicles forming component |
| Surfactant | Sod. Cholate, Sod.deoxycholate, tween-80, Span-80 | For providing flexibility |
| Alcohol | Ethanol, methanol | As a solvent |
| Buffering agent | Saline phosphate buffer (pH 6.4) | As a hydrating medium |
| Drug | Fluconazole | A.P. I |
Table 1: Composition of transferosomes
Advantages of Transferosomes:
Enhanced Penetration: Transferosomes possess high deformability and elasticity, allowing them to squeeze through narrow pores and penetrate deep into the skin or mucosal tissues. This property facilitates the efficient delivery of drugs to target sites that are otherwise difficult to reach, including deeper skin layers or systemic circulation.
Increased Drug Bioavailability: The deformability of transferosomes enhances the bioavailability of drugs by promoting their absorption through the skin or mucosal membranes. This is particularly beneficial for drugs with poor oral bioavailability or those that require localized delivery.
Improved Stability: Transferosomes provide improved stability to encapsulated drugs by shielding them from enzymatic degradation, pH variations, and other environmental factors. This helps maintain the integrity and activity of the drug during storage and transportation.
Targeted Drug Delivery: Similar to invasomes, transferosomes can be surface-modified with targeting ligands to achieve targeted drug delivery. These ligands can recognize specific receptors or molecules on the target cells, allowing for precise and localized drug delivery while minimizing off-target effects.
Versatile Formulation: Transferosomes can encapsulate a wide range of drugs, including both hydrophilic and hydrophobic compounds. This versatility makes them suitable for various types of drugs, allowing for flexibility in drug formulation and delivery.[4]
Disadvantages of Transferosomes:
Complex Manufacturing Process: The preparation of transferosomes requires specialized techniques and equipment, which can increase the complexity and cost of manufacturing. This can limit their widespread use and availability, especially for small-scale production or in resource-limited settings.
Stability Challenges: Transferosomes may face stability issues during storage, such as aggregation, leakage of encapsulated drugs, or changes in their physical properties. These challenges need to be addressed to ensure consistent and reliable performance of transferosomes.
Variable Performance: The performance of transferosomes can be influenced by various factors, including the physicochemical properties of the drug, formulation parameters, and the site of application. Achieving consistent and predictable performance across different drug molecules and conditions may require optimization and customization for each specific application.
Regulatory Considerations: Like other novel drug delivery systems, transferosomes may require specific regulatory considerations for approval and commercialization. Compliance with regulatory standards, safety assessments, and demonstrating the efficacy of transferosomes may add complexity and time to the development process.
Limited Drug Loading Capacity: Transferosomes may have a limited drug-loading capacity due to their vesicular structure. This can be a
drawback when delivering drugs with high dosage requirements or large molecular sizes, potentially requiring higher doses or more frequent administration.[5]
Mechanism of transport:
The mechanism of transport involves the generation of an "osmotic gradient" resulting from water evaporation when a lipid suspension, known as transferosomes, is applied to the skin surface. The transport of these elastic vesicles is not dependent on concentration. The process relies on trans-epidermal hydration as the driving force for vesicle transport. Due to their elasticity, the vesicles can pass through the pores in the corneum, although these pores are smaller in diameter compared to the vesicles. When transferosomes are applied to an open biological surface, such as non-occluded skin, they tend to penetrate the barrier and migrate into the water-rich deeper layers to maintain sufficient hydration [6,7].
During penetration through the corneum, reversible deformation of the bilayer occurs. However, it is crucial to ensure that vesicle integrity, gradient, and barrier properties for underlying hydration affinity are not compromised during this deformation.
Since transferosomes are too large to diffuse through the skin, they need to identify and establish their own pathway through the organ. The effectiveness of transferosomes in drug delivery relies on their ability to expand and overcome hydrophilic pores within the skin. Intracellular drug transportation may involve diffusion of the vesicle lipid bilayer with the skin, similar to normal endocytosis involving the diffusion of vesicles through cytomembrane. The mechanism is intricate and incorporates advanced principles of elasto-mechanics, combined with material transport and hydration/osmotic forces [7,8].
Methods to prepare transferosomes:
1. Ethanol Injection Method
2. Thin Film Hydration Method
3. Reverse Phase Evaporation
4. Ether Injection
5. Solvent Injection Method. [6]
There are several methods used to prepare transferosomes. Here are some commonly employed techniques:
Thin Film Hydration Method: this technique has 3 steps:
Modified hand shaking method:
The selection of the drug's effectiveness is prioritized to enhance the specified parameters. While maintaining consistency with other factors during the preparation of a particular system, the selection and utilization of edge activators become pivotal, influencing the surface charge and thereby contributing to the advancement of highly flexible vesicles, enhancing the drug delivery system.
Reverse Phase Evaporation Method: In this method, a water-in-oil (W/O) emulsion is formed by dissolving lipids and the drug in an organic solvent and then adding an aqueous phase. The resulting W/O emulsion is subjected to high-speed homogenization, leading to the formation of a water-rich vesicle system, which is subsequently converted into transferosomes.
Ether Injection Method: Lipids and the drug are dissolved in an organic solvent mixture containing ether. The organic phase is then rapidly injected into an aqueous medium under high-speed homogenization or sonication, resulting in the formation of transferosomes.
Ethanol Injection Method: Similar to the ether injection method, lipids and the drug are dissolved in an organic solvent mixture containing ethanol. The organic phase is rapidly injected into an aqueous medium under high-speed homogenization or sonication, leading to transferosome formation.
Dehydration-Rehydration Vesicle Method: This method involves the dehydration of preformed liposomes or multilamellar vesicles (MLVs) followed by rehydration with an aqueous medium containing the drug. The dehydration process can be achieved using freeze-drying, spray-drying, or other techniques, and the resulting dehydrated vesicles are subsequently rehydrated to form transferosomes [13,14].
Lipid Film and Remote Loading Method: This method combines the lipid film hydration technique with remote loading of the drug. Lipids are dissolved in an organic solvent to form a lipid film, which is then hydrated with an aqueous medium containing a pH gradient or an ion gradient. The pH or ion gradient drives the active ingredient into the vesicles during hydration, resulting in remote loading of the drug. [ 15,16]
Characterization of Transferosomes:
Application of transfersomes:
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