Advances in oncology drug discovery continue to produce highly potent compounds. However, many of these therapies face significant barriers in clinical translation due to poor solubility, limited bioavailability, high required doses, and systemic toxicity of molecules. Drug delivery remains a critical factor in determining whether an oncology therapy can achieve its intended therapeutic efficacy.
Lipid-based nanotechnology has emerged as an effective strategy to address those challenges. Ascendia Pharmaceutical Solutions developed the LipidSol® platform to enable higher drug payloads, improved tumor targeting, reduced dosing requirements, and mitigate toxicity across a broad range of oncology drugs.
Many oncology drugs exhibit poor aqueous solubility and low bioavailability, requiring high doses to achieve therapeutic exposure. These high doses often increase systemic toxicity, as conventional formulations are non-specific, leading to indiscriminate distribution of the drug across healthy and diseased tissues.
A lack of effective targeting further compounds this issue. When drugs are unable to preferentially accumulate in tumor tissue, exposure to normal cells leads to dose-limiting side effects. As a result, highly potent oncology drugs may fail to reach their full therapeutic potential despite strong therapeutic activity at the molecular target level.
LipidSol® is Ascendia Pharmaceutical Solutions’ proprietary lipid nanoparticle and liposomal technology platform. The platform encompasses both traditional liposome systems and advanced lipid nanoparticles, including architectures like lipoplexes, as those used in nucleic acid delivery.
LipidSol® is supported by a library of proprietary ionizable lipid materials in addition to off-the-shelf conventional phospholipids and long-circulating PEGylated lipids. This flexibility allows formulation scientists to tailor lipid composition, structure, and surface characteristics to the specific requirements of an oncology payload, including small molecules, peptides, RNA, and other biologics.
A core advantage of LipidSol® is its ability to achieve high encapsulation efficiency. By incorporating oncology drugs within lipid nanoparticles, LipidSol® enhances solubility and stabilizes payloads by customized formulations.
Optimized lipid composition and structural stability allow for higher drug loading compared to conventional formulations. Improved encapsulation efficiency ensures that a greater proportion of the administered dose remains associated with the delivery system, supporting more predictable pharmacokinetics and therapeutic exposure by a controlled release mechanism.
Controlled release from lipid nanoparticles further supports dose reduction. By avoiding rapid bolus exposure and lowering peak plasma concentrations, LipidSol® formulations can reduce Cmax-related toxicity while maintaining sustained therapeutic levels.
Systemic toxicity remains a major limitation for many oncology therapies. LipidSol® addresses this challenge through controlled drug release and selective tissue distribution.
Encapsulation within lipid nanoparticles reduces off-target exposure by shielding healthy tissues from immediate drug contact. Extended circulation time increases the likelihood of tumor accumulation while minimizing exposure to non-diseased organs. Together, these mechanisms contribute to improved tolerability without compromising therapeutic efficacy.
LipidSol® supports both passive and active targeting strategies. Passive targeting is achieved by optimizing particle size, surface charge, and circulation time to enhance tumor penetration and retention.
Active targeting can be incorporated through surface functionalization, such as antibody or ligand conjugation. These modifications promote selective binding to tumor-associated markers, increasing drug accumulation at the tumor site. Lipid composition can also be engineered to enhance cellular uptake and intracellular delivery, improving payload transport and distribution across the cell membrane.
Lipid nanoparticle technology has been validated in nucleic acid delivery, including RNA-based therapies. Encapsulation stabilizes sensitive payloads in circulation and enables effective intracellular delivery.
Ascendia Pharmaceutical Solutions has applied LipidSol® to a wide range of payloads, including small molecules, peptides, RNA, and larger biologics. Programs span preclinical and clinical development stages, demonstrating the platform’s adaptability across oncology modalities.
Ascendia Pharmaceutical Solutions provides integrated development and manufacturing support for LipidSol® programs. In-house capabilities include formulation design, analytical characterization, and scalable manufacturing using advanced technologies such as precision microfluidics and high-shear homogenization.
These process technologies enable tight control over particle size, drug loading, and batch consistency while supporting rapid scale-up from early development through cGMP production. Lyophilization strategies further enhance stability and enhanced shelf life for lipid nanoparticle formulations..
LipidSol® enables oncology developers to overcome key delivery challenges by increasing payload capacity, improving tumor targeting, reducing required doses, and lowering systemic toxicity. Combined with Ascendia Pharmaceutical Solutions’ development expertise and state-of-the-art manufacturing capabilities, the platform supports efficient translation from concept to clinical evaluation.
Oncology drug developers seeking to improve therapeutic index, enhance delivery performance, or address formulation limitations are encouraged to engage with Ascendia Pharmaceutical Solutions. To discuss how LipidSol® can support current and future oncology programs, contact Ascendia Pharmaceutical Solutions to schedule a meeting with the formulation and development team.