Sphingosomes are clinically used delivery systems for chemotherapeutic agents, biomacromolecules, and diagnostic agents. Due to flexibility in size and composition, different types of sphingosomes have been developed.

Protheragen-ING specializes in the development of sphingosomes Drug Delivery Systems (DDS) to revolutionize targeted drug delivery. Our team of experienced scientists and researchers are at the forefront of sphingosomes DDS development, utilizing cutting-edge technologies and industry best practices to deliver innovative solutions for drug delivery challenges.

Sphingosomes as DDS

Sphingosomes are amphiphilic concentric vesicular delivery systems formed from a sphingolipid bilayer that surrounds an aqueous volume and has an acidic internal pH. These vesicles comprise sphingolipids (SL) and cholesterol (Chol) in molar ratios ranging from 75:25 to 30:50, with 55:45 SL/Chol being optimal.

Sphingosomes are advanced DDSs that harness the power of sphingolipids, naturally occurring lipids found in cell membranes, to encapsulate and deliver drugs to specific sites in the body.

Fig. 1 Solubilization of free β-sitosterol in milk sphingomyelin and polar lipid vesicles as carriers. (Lopez C, et al. 2023)

By leveraging the unique properties of sphingolipids, Sphingosomes DDS offer numerous advantages over traditional drug delivery methods, including:

• Provides selective passive targeting of tumor tissue.
• Improve efficacy and therapeutic index.
• Increase stability through encapsulation.
• Reduce the toxicity of the encapsulating agent.
• Improved pharmacokinetic effects (increased circulation time).
• Flexible conjugation with site-specific ligands for active targeting.

Our Expertise

We offer comprehensive sphingosomes DDS development services tailored to meet the specific needs of our clients. Our multidisciplinary team possesses extensive knowledge and expertise in areas such as:

• Formulation Development

We excel in designing and optimizing sphingosomes formulations to encapsulate a wide range of drugs, including small molecules, peptides, proteins, and nucleic acids. Our formulation experts employ state-of-the-art techniques to ensure optimal drug loading, stability, and release characteristics.

• Characterization and Analysis

We employ a variety of advanced analytical techniques to characterize and evaluate the physicochemical properties of sphingosomes DDS. This includes particle size analysis, morphology assessment, drug encapsulation efficiency, drug release kinetics, and stability studies.

• Targeting Strategies

Our team specializes in developing strategies to achieve targeted drug delivery using sphingosomes DDS. We can incorporate ligands, antibodies, or peptides onto the surface of sphingosomes to enhance their affinity for specific cell types or tissues, thereby increasing drug accumulation at the desired site.

• In Vitro and In Vivo Evaluation

We conduct rigorous in vitro and in vivo studies to assess the performance and efficacy of sphingosomes DDS. Our scientists utilize cell-based assays, animal models, and imaging techniques to evaluate drug release profiles, cellular uptake, tissue distribution, pharmacokinetics, and therapeutic outcomes.

Protheragen-ING's Technical Approach

Preparation of Sphingosomes

• Active loading: This method is preferred in many ways, and by using a transmembrane pH gradient, a variety of therapeutics can be loaded into the sheath with close to 100% encapsulation efficiency. The method involves establishing some form of gradient that attracts lipophilic compounds to the interior of the vesicles, where they can reside as long as the gradient is maintained.
• Passive loading: This method typically requires the drug to be added to the buffer during the reconstitution step. This allows the drug to be trapped inside the vesicles, whereas it would be retained if it were not fat-soluble. It is commonly used in sphingosine preparations. Various passive loading methods include the mechanical dispersion method, and thin-film hydration method.

Fig. 2 PE-loaded sphingosome was prepared by an improved thin film hydration method (lipid hydration method). (AlMadalli HJ, et al. 2024)

Reduce the size of Sphingosomes

• Extrusion technology
• Ultrasonic treatment
• Microemulsification technology

Application of Sphingosomes as Carrier

Sphingosomes can be used as vectors to treat proliferative diseases, immune diseases, infectious diseases, vascular diseases, rheumatoid diseases, and inflammatory diseases.

Representative drugs include prostaglandins, amphotericin B, methotrexate, cisplatin, vincristine, vinblastine, doxorubicin, camptothecin, ciprofloxacin, progesterone, testosterone, estradiol, Clomethasone and steroids such as vitamin E esters and dexamethasone.

Are you ready to unlock the full potential of Sphingosomes DDS for your drug delivery needs? Contact us today to discuss your project requirements, explore collaboration opportunities, and embark on a journey toward advanced targeted drug delivery.